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Staurosporine (STS) Protein Kinase inhibitor

Name: Staurosporine (STS)
Brand: Selleck Chemicals
SKU: S1421
Rating: 5 (189 reviews)

Cat.No.S1421

Staurosporine (STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. This compound also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.

Chemical Structure

Molecular Weight: 466.53

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Quality Control

Batch: Purity: 99.61%

99.61

Products Often Used Together with Staurosporine (STS)

Z-VAD-FMK

Z-VAD-FMK inhibits cell death induced by this compound in SJG2/MT330 cells.

Related Targets	TGF-beta/Smad PKC ROCK Bcr-Abl
Other Antineoplastic and Immunosuppressive Antibiotics Inhibitors	Cyclosporin A Oligomycin A (MCH 32) Puromycin Dihydrochloride Nigericin sodium salt Geldanamycin (NSC 122750) Honokiol Streptozotocin (STZ) Sodium Monensin (NSC 343257) Cephalomannine Pirarubicin

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
human colon carcinoma cell line HCT116	Function assay			Concentration required for growth inhibition of human colon carcinoma cell line HCT116, IC50=6 nM.	15537345
human PBMC	Function assay		24 h	Suppression of IL2 production in human PBMC after 24 hrs by ELISA, IC50=16 nM.	18585046
endothelial cells	Function assay			Effective dose against plasminogen activator activity stimulated by phorbol ester in endothelial cells, ED50 = 7.5 μM.	8709095
Sf9 insect cells	Function assay			Inhibition of protein kinase C(1:1mixture of PKC alpha & beta) expressed in Sf9 insect cells, IC50 = 0.02 μM.	9873605
LoVo cells	Antiproliferative activity assay			Antiproliferative activity against human colon cancer cell line (LoVo cells) using MTT assay, IC50 = 0.001 μM.	11591505
umbilical vein endothelial cells	Antiproliferative activity assay			Antiproliferative activity against human umbilical vein endothelial cells (HUVECs) using MTT assay, IC50 = 0.004 μM.	11591505
ST-486 cells	Antiproliferative activity assay			Antiproliferative activity against burkit lymphoma cell line (ST-486 cells) using MTT assay, IC50 = 0.007 μM.	11591505
DLD-1 cells	Antiproliferative activity assay			Antiproliferative activity against human colon cancer cell line (DLD-1 cells) using MTT assay, IC50 = 0.009 μM.	11591505
HEK293 cells	Function assay			Inhibition of PKC-beta II mediated IL-8 release from HEK293 cells by ELISA, IC50 = 0.077 μM.	12941331
P19 cells	Function assay			Inhibition of Platelet-derived growth factor receptor in P19 cells, IC50 = 0.002 μM.	15771419
P19 cells	Function assay			Inhibition of Platelet-derived growth factor receptor in P19 cells, IC50 = 0.002 μM.	15771419
P19 cells	Function assay			Inhibition of Protein Kinase A in P19 cells, IC50 = 0.004 μM.	15771419
P19 cells	Function assay			Inhibition of Calcium/calmodulin-dependent protein kinase type II in P19 cells, IC50 = 0.006 μM.	15771419
P19 cells	Function assay			Inhibition of Cyclin-dependent kinase 1 in P19 cells, IC50 = 0.008 μM.	15771419
P19 cells	Function assay			Inhibition of Vascular endothelial growth factor receptor in P19 cells, IC50 = 0.014 μM.	15771419
HEK293 cells	Function assay			Inhibition of IL-8 release by HEK293 cells expressing PKC-beta2, IC50 = 0.077 μM.	15771419
P19 cells	Function assay			Inhibition of Insulin receptor kinase in P19 cells, IC50 = 0.2 μM.	15771419
P19 cells	Function assay			Inhibition of Casein kinase 1 in P19 cells, IC50 = 1.4 μM.	15771419
FL5.12-Akt1 cells	Antiproliferative activity assay			Antiproliferative activity against FL5.12-Akt1 cells by MTT assay, IC50 = 0.29 μM.	16403626
MiaPaCa-2 cells	Antiproliferative activity assay			Antiproliferative activity against MiaPaCa-2 cells by MTT assay, IC50 = 0.37 μM.	16403626
FL5.12-Akt1 cells	Function assay			Activity against GSK3 in FL5.12-Akt1 cells, EC50 = 0.46 μM.	16403626
MiaPaCa-2 cells	Antiproliferative activity assay			Antiproliferative activity against human MiaPaCa-2 cells, IC50 = 0.37 μM.	16413780
FL5.12-Akt1 cells	Function assay			Activity against GSK3 phosphorylation in FL5.12-Akt1 cells, EC50 = 0.46 μM.	16413780
Sf21 cells	Function assay			Inhibition of JAK3 expressed in Sf21 cells, IC50 = 0.006 μM.	17088059
U937 cells	Cytotoxicity assay			Cytotoxicity against human U937 cells, IC50 = 2 μM.	17088067
Sf9 cells	Function assay		1 min	Inhibition of human Fyn expressed in Sf9 cells after 1 min by ELISA in presence of 1 umol/L ATP, IC50 = 0.005 μM.	17315853
Sf9 cells	Function assay		20 mins	Inhibition of human Fyn expressed in Sf9 cells after 20 mins by ELISA in presence of 1 umol/L ATP, IC50 = 0.015 μM.	17315853
Sf9 cells	Function assay		1 min	Inhibition of human Fyn expressed in Sf9 cells after 1 min by ELISA in presence of 10 umol/L ATP, IC50 = 0.036 μM.	17315853
Sf9 cells	Function assay		20 mins	Inhibition of human Fyn expressed in Sf9 cells after 20 mins by ELISA in presence of 10 umol/L ATP, IC50 = 0.083 μM.	17315853
Sf9 cells	Function assay		1 min	Inhibition of human Fyn expressed in Sf9 cells after 1 min by ELISA in presence of 100 umol/L ATP, IC50 = 0.27 μM.	17315853
Sf9 cells	Function assay		20 mins	Inhibition of human Fyn expressed in Sf9 cells after 20 mins by ELISA in presence of 100 umol/L ATP, IC50 = 0.51 μM.	17315853
A549 cells	Cytotoxicity assay		72 h	Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B method, GI50 = 0.0024 μM.	18484775
MDA-MB-231 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B method, GI50 = 0.0071 μM.	18484775
HT29 cells	Cytotoxicity assay		72 h	Cytotoxicity against human HT29 cells after 72 hrs by sulforhodamine B method, GI50 = 0.0109 μM.	18484775
MCF7 cells	Function assay			Inhibition of PKA in human MCF7 cells by array-based fluorescence assay, Ki = 0.005 μM.	18656369
MCF7 cells	Function assay			Inhibition of PKA in human MCF7 cells by array-based fluorescence assay, IC50 = 2 μM.	18656369
Sf9 cells	Function assay			Inhibition of human Syk expressed in Sf9 cells, IC50 = 0.003 μM.	18823784
Sf9 cells	Function assay			Inhibition of human ZAP70 expressed in Sf9 cells, IC50 = 0.053 μM.	18823784
insect cells	Function assay			Inhibition of human recombinant Pim1 expressed in insect cells by HTRF, IC50 = 0.01 μM.	19179076
HT-29 cells	Apoptosis assay		2 h	Induction of apoptosis in human HT-29 cells assessed as change in mitochondrial transmembrane potential after 2 hrs by JC1 staining based fluorescence assay, ED50 = 0.0026 μM.	19422206
insect Sf21 cells	Function assay			Inhibition of JAK3 expressed in insect Sf21 cells assessed as inhibition of biotinylated substrate phosphorylation, IC50 = 0.006 μM.	19427203
Jurkat cells	Antiproliferative activity assay			Antiproliferative activity against JAK3 expressing IL2-stimulated human Jurkat cells, IC50 = 0.071 μM.	19427203
Jurkat cells	Antiproliferative activity assay			Antiproliferative activity against JAK3 expressing human resting Jurkat cells, IC50 = 0.311 μM.	19427203
HUE cells	Function assay		90 mins	Inhibition of VEGFR2 in HUE cells assessed as inhibition of VEGF-induced autophosphorylation treated for 90 mins before VEGF challenge by ELISA, IC50 = 0.07 μM.	20170163
Sf9 cells	Function assay		60 mins	Inhibition of human recombinant GST-fused NIK expressed in Sf9 cells after 60 mins by radiometric protein kinase assay, IC50 = 2.3 μM.	20580552
Sf21 cells	Function assay	30 uM		Inhibition of human CHK2 kinase expressed in insect Sf21 cells using phospho-CREBtide as substrate at 30 uM, IC50 = 0.027 μM.	21334796
Sf21 cells	Function assay	30 uM		Inhibition of human recombinant IKK-alpha expressed in insect Sf21 cells using phospho-Ulight-IkappaB-alpha as substrate at 30 uM, IC50 = 0.039 μM.	21334796
Sf21 cells	Function assay	30 uM		Inhibition of human recombinant IKK-beta expressed in insect Sf21 cells using phospho-Ulight-IkappaB-alpha as substrate at 30 uM, IC50 = 0.49 μM.	21334796
HeLa cells	Cytotoxicity assay		48 h	Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.000004 μM.	21388191
MCF7 cells	Cytotoxicity assay		48 h	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.05 μM.	21388191
HT-29 cells	Function assay		2 h	Effect on mitochondrial membrane potential in human HT-29 cells after 2 hrs using JC-1 staining by fluorescence assay, IC50 = 0.002 μM.	21428375
HeLa cells	Cytotoxicity assay		48 h	Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.000004 μM.	21488655
MCF7 cells	Cytotoxicity assay		48 h	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.05 μM.	21488655
HT-29 cells	Function assay			Inhibition of mitochondrial membrane potential in human HT-29 cells using JC1 dye staining by fluorescence plate reader assay, IC50 = 0.0025 μM.	21513293
SF268 cells	Cytotoxicity assay		48 h	Cytotoxicity against human SF268 cells after 48 hrs by SRB assay, GI50 = 0.044 μM.	21513294
CHOK1 cells	Cytotoxicity assay		48 h	Cytotoxicity against human CHOK1 cells after 48 hrs by SRB assay, GI50 = 0.13 μM.	21513294
H460 cells	Cytotoxicity assay		48 h	Cytotoxicity against human H460 cells after 48 hrs by SRB assay, GI50 = 3.6 μM.	21513294
HT-29 cells	Cytotoxicity assay		48 h	Cytotoxicity against human HT-29 cells after 48 hrs by SRB assay, GI50 = 3.6 μM.	21513294
MCF7 cells	Cytotoxicity assay		48 h	Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay, GI50 = 11 μM.	21513294
SW1116 cells	Function assay		24 h	Inhibition of telomerase in human SW1116 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 8.32 μM.	21962523
HT-29 cells	Apoptosis assay		2 h	Induction of apoptosis in human HT-29 cells assessed reduction of mitochondrial membrane potential after 2 hrs by using JC1 staining by fluorescence cell-based assay, ED50 = 0.0026 μM.	21973101
LoVo cells	Antiproliferative activity assay		48 to 72 h	Antiproliferative activity against human LoVo cells after 48 to 72 hrs by MTT assay, IC50 = 0.001 μM.	22182929
ST486 cells	Antiproliferative activity assay		48 to 72 h	Antiproliferative activity against human ST486 cells after 48 to 72 hrs by MTT assay, IC50 = 0.007 μM.	22182929
DLD1 cells	Antiproliferative activity assay		48 to 72 h	Antiproliferative activity against human DLD1 cells after 48 to 72 hrs by MTT assay, IC50 = 0.009 μM.	22182929
B16F10 cells	Antiproliferative activity assay		48 h	Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay, IC50 = 2.82 μM.	22503364
MCF7 cells	Antiproliferative activity assay		48 h	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 3.07 μM.	22503364
A431 cells	Cytotoxicity assay		24 h	Cytotoxicity against human A431 cells after 24 hrs using Annexin VeFITC/propidium iodide staining by MTT assay, IC50 = 0.07 μM.	22541051
MCF7 cells	Cytotoxicity assay		24 h	Cytotoxicity against human MCF7 cells after 24 hrs using Annexin VeFITC/propidium iodide staining by MTT assay, IC50 = 0.18 μM.	22541051
BJ cells	Cytotoxicity assay		72 h	Cytotoxicity against human BJ cells after 72 hrs by Calcein AM assay, IC50 = 0.002 μM.	22921081
CEM cells	Cytotoxicity assay		72 h	Cytotoxicity against human CEM cells after 72 hrs by Calcein AM assay, IC50 = 0.023 μM.	22921081
MCF7 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MCF7 cells after 72 hrs by Calcein AM assay, IC50 = 0.064 μM.	22921081
HeLa cells	Cytotoxicity assay		72 h	Cytotoxicity against human HeLa cells after 72 hrs by Calcein AM assay, IC50 = 0.175 μM.	22921081
HepG2 cells	Function assay		24 h	Inhibition of telomerase in human HepG2 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 4.14 μM.	23018096
SW1116 cells	Antiproliferative activity assay		48 h	Antiproliferative activity against human SW1116 cells after 48 hrs by MTT method, IC50 = 4.95 μM.	23018096
HepG2 cells	Antiproliferative activity assay		48 h	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT method, IC50 = 6.73 μM.	23018096
BGC823 cells	Antiproliferative activity assay		48 h	Antiproliferative activity against human BGC823 cells after 48 hrs by MTT method, IC50 = 6.83 μM.	23018096
HeLa cells	Antiproliferative activity assay		48 h	Antiproliferative activity against human HeLa cells after 48 hrs by MTT method, IC50 = 9.12 μM.	23018096
HCT116 cells	Function assay			Inhibition of TNIK-mediated TCF4/beta-casein transcription in human HCT116 cells by beta-lactamase reporter gene assay, IC50 = 0.039 μM.	23232060
HepG2 cells	Function assay		48 h	Inhibition of telomerase in human HepG2 cells after 48 hrs by TRAP-PCR-ELISA, IC50 = 8.3 μM.	23279864
SW1116 cells	Function assay		24 h	Inhibition of telomerase in human SW1116 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 4.18 μM.	24286761
KE-97 cells	Cytotoxicity assay		72 h	Cytotoxicity against human KE-97 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.13 μM.	24328283
Jurkat cells	Cytotoxicity assay		72 h	Cytotoxicity against human Jurkat cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.14 μM.	24328283
HuH7 cells	Cytotoxicity assay		72 h	Cytotoxicity against human HuH7 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.23 μM.	24328283
BGC823 cells	Cytotoxicity assay		72 h	Cytotoxicity against human BGC823 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.38 μM.	24328283
MCF7 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MCF7 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.52 μM.	24328283
NIH/3T3 cells	Cytotoxicity assay		96 h	Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by SRB assay, IC50 = 0.2 μM.	24361521
A2780 cells	Cytotoxicity assay		96 h	Cytotoxicity against human A2780 cells after 96 hrs by SRB assay, IC50 = 0.2 μM.	24361521
HT-29 cells	Cytotoxicity assay		96 h	Cytotoxicity against human HT-29 cells after 96 hrs by SRB assay, IC50 = 0.2 μM.	24361521
8505C cells	Cytotoxicity assay		96 h	Cytotoxicity against human 8505C cells after 96 hrs by SRB assay, IC50 = 0.2 μM.	24361521
518A2 cells	Cytotoxicity assay		96 h	Cytotoxicity against human 518A2 cells after 96 hrs by SRB assay, IC50 = 0.2 μM.	24361521
MCF7 cells	Cytotoxicity assay		96 h	Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay, IC50 = 0.4 μM.	24361521
A549 cells	Cytotoxicity assay		96 h	Cytotoxicity against human A549 cells after 96 hrs by SRB assay, IC50 = 0.6 μM.	24361521
V79 MZ cells	Function assay			Inhibition of human aldosterone synthase expressed in V79 MZ cells assessed as inhibition of aldosterone synthesis, IC50 = 0.011 μM.	24422519
HEK293 cells	Cytotoxicity assay		72 h	Cytotoxicity against HEK293 cells after 72 hrs by CellTiterGlo assay, IC50 = 0.056 μM.	24763262
HeLa cells	Antiproliferative activity assay		24 to 48 h	Antiproliferative activity against human HeLa cells after 24 to 48 hrs by CCK-8 assay, IC50 = 2.72 μM.	24792811
A549 cells	Antiproliferative activity assay		24 to 48 h	Antiproliferative activity against human A549 cells after 24 to 48 hrs by CCK-8 assay, IC50 = 3.05 μM.	24792811
HepG2 cells	Cytotoxicity assay			Cytotoxicity against human HepG2 cells, EC50 = 2 μM.	25316317
Raji cells	Cytotoxicity assay			Cytotoxicity against human Raji cells, EC50 = 2 μM.	25316317
BJ cells	Cytotoxicity assay			Cytotoxicity against human BJ cells, EC50 = 2 μM.	25316317
HEK293 cells	Cytotoxicity assay			Cytotoxicity against HEK293 cells, EC50 = 2 μM.	25316317
A549 cells	Cytotoxicity assay		48 h	Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50 = 0.02 μM.	25825934
HeLa cells	Cytotoxicity assay		48 h	Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.025 μM.	25825934
PC3 cells	Cytotoxicity assay		48 h	Cytotoxicity against human PC3 cells after 48 hrs by MTT assay, IC50 = 0.031 μM.	25825934
MGC-803 cells	Function assay		24 h	Inhibition of telomerase in human MGC-803 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 8.97 μM.	26900656
Sf9 insect cells	Function assay		10 mins	Inhibition of N-terminal GST tagged recombinant full-length human CHK1 expressed in baculovirus Sf9 insect cells after 10 mins by luminescent ADP-Glo assay, IC50 = 0.0012 μM.	27089211
Sf21 cells	Function assay		60 mins	Inhibition of human recombinant JAK2 expressed in Sf21 cells assessed as reduction in Ulight-CAGAGAIETDKEYYTVKD phosphorylation pre-incubated before substrate addition and measured after 60 mins by LANCE detection method, IC50 = 0.002 μM.	27137359
Neuro2a cells	Cytotoxicity assay		72 h	Cytotoxicity against mouse Neuro2a cells assessed as cell viability after 72 hrs by MTT assay, IC50 = 0.0113 μM.	28152427
MDA-MB-231 cells	Function assay		16 h	Inhibition of retinoblastoma protein phosphorylation in human MDA-MB-231 cells after 16 hrs by Hoechst 33342 staining based fluorescence assay, IC50 = 0.066 μM.	28431342
Sf9 insect cells	Function assay		20 mins	Inhibition of recombinant human N-terminally GST-tagged EGFR L858R/T790M/C797S triple mutant expressed in baculovirus in Sf9 insect cells preincubated for 20 mins followed by addition of [33P]-ATP measured after 2 hrs by filter-binding method, IC50 = 0.00029 μM.	28482151
HEK293 cells	Cytotoxicity assay		72 h	Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 72 hrs by CellTiter Glo luminescent assay, CC50 = 0.00354 μM.	28624701
BT549 cells	Cytotoxicity assay		24 h	Cytotoxic activity against human BT549 cells incubated for 24 hrs by MTT assay, IC50 = 0.08 μM.	28705432
MDA-MB-468 cells	Cytotoxicity assay		24 h	Cytotoxic activity against human MDA-MB-468 cells incubated for 24 hrs by MTT assay, IC50 = 0.15 μM.	28705432
MDA-MB-231 cells	Cytotoxicity assay		24 h	Cytotoxic activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay, IC50 = 0.24 μM.	28705432
Vero cells	Cytotoxicity assay		2 days	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 2 days by cell-titer-glo luminescent assay, TC50 = 0.0024 μM.	28763645
L929 cells	Antiproliferative activity assay		5 days	Antiproliferative activity against mouse L929 cells after 5 days by WST-1 assay, IC50 = 0.2 μM.	28956915
KB-3-1 cells	Antiproliferative activity assay		5 days	Antiproliferative activity against human KB-3-1 cells after 5 days by WST-1 assay, IC50 = 0.2 μM.	28956915
MCF7 cells	Antiproliferative activity assay		5 days	Antiproliferative activity against human MCF7 cells after 5 days by WST-1 assay, IC50 = 1.8 μM.	28956915
FS4-LTM cells	Antiproliferative activity assay		24 h	Antiproliferative activity against human FS4-LTM cells after 24 hrs by WST-1 assay, IC50 = 2.8 μM.	28956915
Vero cells	Cytotoxicity assay		2 days	Cytotoxicity against African green monkey Vero cells after 2 days by CellTiter-Glo luminescent cell viability assay, IC50 = 0.0024 μM.	28993106
HepG2 cells	Cytotoxicity assay	100 uM	3 days	Cytotoxicity against human HepG2 cells at 100 uM after 3 days by CellTiter-Glo luminescent cell viability assay, IC50 = 0.018 μM.	28993106
NIH/3T3 cells	Cytotoxicity assay		96 h	Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by SRB assay, EC50 = 0.008 μM.	29197730
518A2 cells	Cytotoxicity assay		96 h	Cytotoxicity against human 518A2 cells after 96 hrs by SRB assay, EC50 = 0.03 μM.	29197730
A549 cells	Cytotoxicity assay		96 h	Cytotoxicity against human A549 cells after 96 hrs by SRB assay, EC50 = 0.04 μM.	29197730
MCF7 cells	Cytotoxicity assay		96 h	Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay, EC50 = 0.1 μM.	29197730
A2780 cells	Cytotoxicity assay		96 h	Cytotoxicity against human A2780 cells after 96 hrs by SRB assay, EC50 = 0.12 μM.	29197730
HT-29 cells	Cytotoxicity assay		96 h	Cytotoxicity against human HT-29 cells after 96 hrs by SRB assay, EC50 = 0.15 μM.	29197730
PC3 cells	Cytotoxicity assay			Cytotoxicity against human PC3 cells by sulforhodamine B assay, IC50 = 0.017 μM.	29389122
HCT116 cells	Cytotoxicity assay			Cytotoxicity against human HCT116 cells by sulforhodamine B assay, IC50 = 0.055 μM.	29389122
insect cells	Function assay		30 mins	Inhibition of recombinant human PDGFRbeta expressed in insect cells using Ulight-Poly GAT[EAY(1:1:1)]n as substrate after 30 mins by LANCE method, IC50 = 0.00076 μM.	29549836
Sf9 insect cells	Function assay		60 mins	Inhibition of recombinant human KDR expressed in Sf9 insect cells using Ulight-CAGAGAIETDKEYYTVKD as substrate after 60 mins by LANCE method, IC50 = 0.0021 μM.	29549836
insect cells	Function assay		10 mins	Inhibition of recombinant human Src expressed in insect cells using Ulight-Poly GAT[EAY(1:1:1)]n as substrate after 10 mins by LANCE method, IC50 = 0.005 μM.	29549836
insect cells	Function assay		15 mins	Inhibition of recombinant human CDK1/Cyclin B expressed in insect cells using Ulight-CFFKNIVTPRTPPPSQGK-amide as substrate after 15 mins by LANCE method, IC50 = 0.025 μM.	29549836
insect cells	Function assay		15 mins	Inhibition of recombinant human CDK1/Cyclin B expressed in insect cells using Ulight-CFFKNIVTPRTPPPSQGK-amide as substrate after 15 mins by LANCE method, IC50 = 0.025 μM.	29549836
Sf9 insect cells	Function assay		15 mins	Inhibition of recombinant human Flt1 expressed in Sf9 insect cells using Ulight-TK peptide as substrate after 15 mins by LANCE method, IC50 = 0.035 μM.	29549836
Sf21 insect cells	Function assay		15 mins	Inhibition of recombinant human Aurora-A expressed in Sf21 insect cells using Ulight-RRRSLLE as substrate after 15 mins by LANCE method, IC50 = 0.039 μM.	29549836
insect cells	Function assay		60 mins	Inhibition of recombinant human AKT1 expressed in insect cells using CREBtide as substrate after 60 mins by LANCE method, IC50 = 0.056 μM.	29549836
Sf9 insect cells	Function assay		60 mins	Inhibition of recombinant human FAK expressed in Sf9 insect cells using Ulight-TK peptide as substrate after 60 mins by LANCE method, IC50 = 0.062 μM.	29549836
insect cells	Function assay		60 mins	Inhibition of recombinant human ABL expressed in insect cells using Ulight-TK peptide as substrate after 60 mins by LANCE method, IC50 = 0.29 μM.	29549836
insect cells	Function assay		60 mins	Inhibition of recombinant human c-MET expressed in insect cells using Ulight-CAGAGAIETDKEYYTVKD as substrate after 60 mins by LANCE method, IC50 = 0.31 μM.	29549836
PC3 cells	Cytotoxicity assay		72 h	Cytotoxicity against human PC3 cells after 72 hrs by SRB assay, IC50 = 0.039 μM.	29558119
Sf9 cells	Function assay		45 mins	Inhibition of recombinant human C-terminal His-tagged/N-terminal GST-tagged EGFR (668 to 1210 residues) expressed in baculovirus infected Sf9 cells using Poly-(Glu, Tyr) as substrate measured after 45 minutes by Kinase-Glo luminescent assay, IC50 = 0.047 μM.	29902719
Sf9 cells	Function assay		45 mins	Inhibition of recombinant human N-terminal GST-tagged HER2 (679 to 1255 residues) expressed in baculovirus infected Sf9 cells using Poly-(Glu, Tyr) as substrate measured after 45 minutes by Kinase-Glo luminescent assay, IC50 = 0.0608 μM.	29902719
HT-29 cells	Function assay		3 h	Inhibition of mitochondrial membrane potential in human HT-29 cells after 3 hrs by JC-1 staining based fluorescence assay, IC50 = 0.02 μM.	30057155
Sf9 cells	Function assay			Inhibition of N-terminal FLAG-tagged human full-length CDK12 (1 to 1490 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.053 μM.	30067358
Sf9 cells	Function assay			Inhibition of N-terminal FLAG-tagged human full-length CDK12 (1 to 1490 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.053 μM.	30067358
Sf9 cells	Function assay			Inhibition of N-terminal FLAG-tagged human full-length CDK13 (1 to 1512 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.057 μM.	30067358
Sf9 cells	Function assay			Inhibition of N-terminal FLAG-tagged human full-length CDK13 (1 to 1512 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.057 μM.	30067358
HCT116 cells	Cytotoxicity assay		48 h	Cytotoxicity against human HCT116 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 0.03 μM.	30106291
Huh7.5 cells	Cytotoxicity assay		48 h	Cytotoxicity against human Huh7.5 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 0.6 μM.	30106291
K562 cells	Cytotoxicity assay		48 h	Cytotoxicity against human K562 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 1.7 μM.	30106291
LO2 cells	Cytotoxicity assay		48 h	Cytotoxicity against human LO2 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 9.5 μM.	30106291
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Chemical Information, Storage & Stability

Molecular Weight	466.53	Formula	C₂₈H₂₆N₄O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	62996-74-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	AM-2282，Antibiotic AM-2282			Smiles	CC12C(C(CC(O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)NC)OC

Solubility

In vitro
Batch:

DMSO : 46 mg/mL (98.6 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (10.72mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	PKCα (Cell-free assay) 2 nM c-Fgr (Cell-free assay) 2 nM phosphorylase kinase (Cell-free assay) 3 nM PKCη (Cell-free assay) 4 nM PKCγ (Cell-free assay) 5 nM S6 kinase (Cell-free assay) 5 nM v-Src (Cell-free assay) 6 nM Cdc2 (Cell-free assay) 9 nM Cdc2 (Cell-free assay) 9 nM PKA (Cell-free assay) 15 nM Syk (Cell-free assay) 16 nM PKG (Cell-free assay) 18 nM PKCδ (Cell-free assay) 20 nM CaMKII (Cell-free assay) 20 nM Lyn (Cell-free assay) 20 nM MLCK (Cell-free assay) 21 nM PKCε (Cell-free assay) 73 nM
In vitro	Staurosporine (STS), a microbial alkaloid, significantly inhibits protein kinase C from rat brain with IC50 of 2.7 nM. It also displays strong inhibitory effect against HeLa S3 cells with IC50 of 4 nM. This compound inhibits a variety of other protein kinases, including PKA, PKG, phosphorylase kinase, S6 Kinase, Myosin light chain kinase (MLCK), CAM PKII, cdc2, v-Src, Lyn, c-Fgr, and Syk with IC50 of 15 nM, 18 nM, 3 nM, 5 nM, 21 nM, 20 nM, 9 nM, 6 nM, 20 nM, 2 nM, and 16 nM, respectively. At 1 μM, it induces >90% apoptosis in PC12 cells. Consistently, this treatment induces a rapid and prolonged elevation of intracellular free calcium levels [Ca²⁺]_i, accumulation of mitochondrial reactive oxygen species (ROS), and subsequent mitochondrial dysfunction. The apoptosis of MCF7 cells induced by STS can be enhanced by the expression of functional caspase-3 via caspase-8 activation and Bid cleavage. Treatment at 1 μM only partially inhibits IL-3-stimulated Bcl2 phosphorylation but completely blocks PKC-mediated Bcl2 phosphorylation. It induces apoptosis of human foreskin fibroblasts AG-1518, depending on the lysosomal cathepsins D mediated cytochrome c release and caspase activation. In addition to activating the classical mitochondrial apoptosis pathway, STS triggers a novel intrinsic apoptosis pathway, relying on the activation of caspase-9 in the absence of Apaf-1.
Kinase Assay	Enzyme assay and binding assay
Kinase Assay	Protein kinase C is assayed in a reaction mixture (0.25 mL) containing 5 μmol of Tris/HCl, pH 7.5, 2.5 μmol of magnesium acetate, 50 μg of histone II S, 20 μg of phosphatidylserine, 0.88 μg of diolein, 125 nmol of CaCl₂, 1.25 nmol of [γ-³²]ATP (5-10 × 10⁴ cpm/nmol) and 5 μg of partially purified enzyme. The binding of [³H]PDBu to protein kinase C is determined: Reaction mixture (200 μL) contained 4 μmol of Tris/malate, pH 6.8, 20 μmol of KCl, 30 nmol of CaCl₂, 20 μg of phosphatidylserine, 5 μg of partially purified protein kinase C, 0.5% (final concentration) of DMSO, 10 pmol of [³H]PDBu (1-3 × 10⁴ cpm/pmol) and 10 μL of various amounts of Staurosporine (STS).
In vivo	In the gerbil and rat ischemia models, pretreatment with Staurosporine (STS) (0.1–10 ng) before ischemia prevents neuronal damage in a dose-dependent manner, suggesting the involvement of PKC in CA1 pyramidal cell death after ischemia.
References	[1] https://pubmed.ncbi.nlm.nih.gov/3457562/ [2] https://pubmed.ncbi.nlm.nih.gov/8529658/ [3] https://pubmed.ncbi.nlm.nih.gov/9486765/ [4] https://pubmed.ncbi.nlm.nih.gov/10734071/ [5] https://pubmed.ncbi.nlm.nih.gov/10677502/ [6] https://pubmed.ncbi.nlm.nih.gov/14576777/ [7] https://pubmed.ncbi.nlm.nih.gov/21659556/ [8] https://pubmed.ncbi.nlm.nih.gov/2384538/

Applications

Methods	Biomarkers	PMID
Western blot	p-Akt / Akt / PARP /Cleaved PARP FAK / RIP Ambra1	24174874
Growth inhibition assay	Cell viability	25215174
Immunofluorescence	Tubulin / Actin Phalloidin / Type II collagen Pyk2 Annexin cleaved-caspase 3 FAK 4.47	25215174

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05209347	Withdrawn	Ankle Fractures\|Post-traumatic Osteoarthritis\|Osteoarthritis Ankle	University of Iowa	December 2024	Not Applicable
NCT05956990	Not yet recruiting	Colorectal Cancer Survivor\|Rehabilitation\|Quality of Life	Qu Shen\|The First Affiliated Hospital of Xiamen University\|Xiamen University	July 1 2024	Not Applicable
NCT05957289	Not yet recruiting	Rehabilitation\|Colorectal Cancer Survivor\|Quality of Life\|Pilot Study	Qu Shen\|The First Affiliated Hospital of Xiamen University\|Xiamen University	June 1 2024	Not Applicable
NCT06245135	Not yet recruiting	Mobility Limitation	University of Toronto\|University Health Network Toronto\|March of Dimes Canada\|Heart and Stroke Foundation of Canada\|University of Alberta\|University of Manitoba\|Bruyere Research Institute	June 2024	Not Applicable
NCT06374108	Not yet recruiting	Multiple Sclerosis	University of Aarhus\|Aarhus University Hospital\|University of Copenhagen	May 1 2024	Not Applicable

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