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PR-171 (Carfilzomib) Proteasome inhibitor

Name: PR-171 (Carfilzomib)
Brand: Selleck Chemicals
SKU: S2853
Rating: 5 (249 reviews)

Cat.No.S2853

Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival autophagy and induces cell apoptosis.

Chemical Structure

Molecular Weight: 719.91

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Quality Control

Batch: Purity: 99.75%

99.75

Related Targets	HDAC Caspase Secretase MMP HCV Protease Cysteine Protease DPP Tyrosinase HIV Protease Serine Protease
Other Proteasome Inhibitors	MG132 Celastrol Epoxomicin (BU-4061T) ONX-0914 (PR-957) Oprozomib Delanzomib VR23 Marizomib (Salinosporamide A) PI-1840 KSQ-4279 (USP1-IN-1)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
MM.1S	Growth Inhibition Assay	0-100 nM	48 h	IC50 = 10 nM	25312543
NCI-H929	Growth Inhibition Assay	0-100 nM	48 h	IC50 = 14 nM	25312543
SUDHL16	Apoptosis Asssay	2.5–3.5 nM	48 h	enhances the cell death co-treatment with ACY1215	25239935
SUDHL14	Apoptosis Asssay	2.5–3.5 nM	48 h	enhances the cell death co-treatment with ACY1215	25239935
U2932	Apoptosis Asssay	2.5–3.5 nM	48 h	enhances the cell death co-treatment with ACY1215	25239935
P-UMSCC-1	Growth Inhibition Assay			IC50=11.2 nM	24915039
R-UMSCC-1	Growth Inhibition Assay			IC50=2294 nM	24915039
P-Cal33	Growth Inhibition Assay			IC50=17.3 nM	24915039
R-Cal33	Growth Inhibition Assay			IC50=1112 nM	24915039
Jurkat	Growth Inhibition Assay	1-11nM	48 h	inhibits the cell proliferation co-treatment with vorinostat	24801128
Jurkat	Apoptosis Asssay	8 nM	24/48 h	induces apoptosis, caspase activation, and PARP cleavage co-treatment with vorinostat	24801128
UMSCC-22A	Apoptosis Asssay	200 nM	24 h	induce the cell apoptosis co-treatment with ONX 0912	22929803
UMSCC-22B	Apoptosis Asssay	200 nM	24 h	induce the cell apoptosis co-treatment with ONX 0912	22929803
1483	Apoptosis Asssay	200 nM	24 h	induce the cell apoptosis co-treatment with ONX 0912	22929803
UMSCC-1	Apoptosis Asssay	200 nM	24 h	induce the cell apoptosis co-treatment with ONX 0912	22929803
UMSCC-22A	Growth Inhibition Assay			IC50=38.7 ± 1.0 nM	22929803
UMSCC-22B	Growth Inhibition Assay			IC50=30.7 ± 9.3 nM	22929803
1483	Growth Inhibition Assay			IC50=50.5 ± 11.9 nM	22929803
UMSCC-1	Growth Inhibition Assay			IC50=34.6 ± 2.6 nM	22929803
Cal33	Growth Inhibition Assay			IC50=49.3 ± 8.9 nM	22929803
PCI-15A	Growth Inhibition Assay			IC50=70.4 ± 22.6 nM	22929803
PCI-15B	Growth Inhibition Assay			IC50=39.5 ± 11.0 nM	22929803
OSC-19	Growth Inhibition Assay			IC50=18.3 ± 4.2 nM	22929803
SUDHL16	Apoptosis Asssay	2.0-4.0 nM	48 h	induces cell death co-treatment with obatoclax	22411899
SUDHL16	Function Assay	2.5 nM	24 h	activates JNK, inactivates AKT, up-regulates Noxa, and induces γH2A.X co-treatment with obatoclax	22411899
Granta	Growth Inhibition Assay	0-4 nM	48 h	induce cell death co-treatment with HADCIs	21750224
SUDHL16	Growth Inhibition Assay	1-4 nM	36 h	induce cell death co-treatment with HADCIs	20233973
MOLT4	Function assay		1 hr	Inhibition of chymotrypsin-like activity of 20S proteasome in human MOLT4 cells after 1 hr by CellTiter-Glo luminescent assay, IC50 = 0.0051 μM.	19348473
MESSA	Cytotoxicity assay		72 hrs	Cytotoxicity against human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay, IC50 = 0.018 μM.	19348473
MESSA	Cytotoxicity assay		72 hrs	Cytotoxicity against multidrug resistance transporter expressing doxorubicin resistant human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay, IC50 = 0.413 μM.	19348473
RPMI8226	Cytotoxicity assay		72 hrs	Cytotoxic activity against human RPMI8226 cells after 72 hrs by MTS assay, IC50 = 0.01319 μM.	24767818
NCI-H929	Cytotoxicity assay		72 hrs	Cytotoxic activity against human NCI-H929 cells after 72 hrs by MTS assay, IC50 = 0.02132 μM.	24767818
CCRF-CEM	Antiproliferative assay		72 hrs	Antiproliferative activity against human CCRF-CEM cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0061 μM.	26231162
RPMI8266	Antiproliferative assay		72 hrs	Antiproliferative activity against human RPMI8266 cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0139 μM.	26231162
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0193 μM.	26231162
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0238 μM.	26231162
TOV21G	Antiproliferative assay		72 hrs	Antiproliferative activity against human TOV21G cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0238 μM.	26231162
RKO	Antiproliferative assay		72 hrs	Antiproliferative activity against human RKO cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0271 μM.	26231162
MM1S	Antiproliferative assay		72 hrs	Antiproliferative activity against human MM1S cells measured after 72 hrs by MTS assay, IC50 = 0.0015 μM.	27765408
RPMI8226	Antiproliferative assay		72 hrs	Antiproliferative activity against human RPMI8226 cells measured after 72 hrs by MTS assay, IC50 = 0.0132 μM.	27765408
LCL	Cytotoxicity assay		48 hrs	Cytotoxicity against human LCL cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.03 μM.	27994734
RD-ES	Cytotoxicity assay		48 hrs	Cytotoxicity against human RD-ES cells harboring p53 mutant assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.043 μM.	27994734
U266	Cytotoxicity assay		48 hrs	Cytotoxicity against human U266 cells harboring mutant p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.06 μM.	27994734
WE68	Cytotoxicity assay		48 hrs	Cytotoxicity against human WE68 cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.08 μM.	27994734
IMR90	Cytotoxicity assay		48 hrs	Cytotoxicity against human IMR90 cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.13 μM.	27994734
MCF10A	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF10A cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.32 μM.	27994734
SKOV3	Cytotoxicity assay		48 hrs	Cytotoxicity against p53 deficient human SKOV3 cells assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.32 μM.	27994734
MDA-MB-468	Cytotoxicity assay		48 hrs	Cytotoxicity against human MDA-MB-468 cells harboring mutant p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.33 μM.	27994734
HNDF	Cytotoxicity assay		48 hrs	Cytotoxicity against HNDF cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.35 μM.	27994734
KGN	Cytotoxicity assay		48 hrs	Cytotoxicity against human KGN cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.45 μM.	27994734
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 4.5 μM.	27994734
MCF7	Function assay	35 nM	4 hrs	Inhibition of 26S proteasome in human MCF7 cells assessed as accumulation of high molecular weight polyubiquitin-conjugated proteins at 35 nM after 4 hrs by Western blot analysis	27994734
MDA-MB-468	Function assay	35 nM	4 hrs	Inhibition of 26S proteasome in human MDA-MB-468 cells assessed as accumulation of high molecular weight polyubiquitin-conjugated proteins at 35 nM after 4 hrs by Western blot analysis	27994734
MM1S	Cytotoxicity assay		72 hrs	Cytotoxicity against human MM1S cells measured after 72 hrs by MTS assay, IC50 = 0.0015 μM.	28027531
RPMI8226	Cytotoxicity assay		72 hrs	Cytotoxicity against human RPMI8226 cells measured after 72 hrs by MTS assay, IC50 = 0.0132 μM.	28027531
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
fibroblast cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
fibroblast cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells	29435139
Daoy	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for Daoy cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D caspase screen for TC32 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for MG 63 (6-TG R) cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for RD cells	29435139
ANBL-6	Function assay			Inhibition of 20S proteasome activity in human ANBL-6 cells, IC50 = 0.01 μM.	29652143
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.0041 μM.	30165344
MDA-MB-231	Cytotoxicity assay		48 hrs	Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 0.0044 μM.	30165344
RPMI8226	Cytotoxicity assay		48 hrs	Cytotoxicity against human RPMI8226 cells after 48 hrs by MTT assay, IC50 = 0.0067 μM.	30165344
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	719.91	Formula	C₄₀H₅₇N₅O₇	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	868540-17-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C)CC(C(=O)C1(CO1)C)NC(=O)C(CC2=CC=CC=C2)NC(=O)C(CC(C)C)NC(=O)C(CCC3=CC=CC=C3)NC(=O)CN4CCOCC4

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (138.9 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 50 mg/mL

Water : 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.
Clear solution	2%DMSO 1 30%PEG300 2 2%TWEEN80 3 66%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (1.39mM)	Taking the 1 mL working solution as an example, add 20 μL of 50 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 660 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.
Clear solution	2%DMSO 1 30%PEG300 2 2%Tween80 3 66%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (1.39mM)	Taking the 1 mL working solution as an example, add 20 μL of 50 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 660 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:

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% 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	Proteasome (ANBL-6 cells) 5 nM
In vitro	Carfilzomib (PR-171) inhibits proliferation in a variety of cell lines and patient-derived neoplastic cells, including multiple myeloma, and induced intrinsic and extrinsic apoptotic signaling pathways and activation of c-Jun-N-terminal kinase (JNK). It reveals enhanced anti-MM activity, overcomes resistance to other agents, and acts synergistically with (Dex). This compound shows preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, with over 80% inhibition at doses of 10 nM. Short exposure to low-dose Carfilzomib leads to preferential binding specificity for the β5 constitutive 20S proteasome and the β5i immunoproteasome subunits. Measurement of caspase activity in ANBL-6 cells pulsed with it reveals substantial increases in caspase-8, caspase-9, and caspase-3 activity after 8 hours, giving a 3.2-, 3.9- and 6.9-fold increase, respectively, over control cells after 8 hours. In carfilzomib pulse-treated cells, the mitochondrial membrane integrity is decreased to 41% (Q1 + Q2), compared with 75% in vehicle-treated control cells. In another study, it has also shown preclinical effectiveness against hematological and solid malignancies. It directly inhibits osteoclasts formation and bone resorption.
Kinase Assay	Enzyme-linked immunosorbent assay for subunit profiling of carfilzomib
Kinase Assay	ANBL-6 cells (2 × 10⁶/well) are plated in 96-well plates and treated with Carfilzomib (PR-171) doses from 0.001 to 10 μM for 1 hour. Cells are then lysed (20 mM Tris-HCl, 0.5 mM EDTA), and cleared lysates are transferred to polymerase chain reaction (PCR) plates. A standard curve is generated using untreated ANBL-6 cell lysates starting at a concentration of 6 μg protein/μL. The active site probe [biotin-(CH2)4-Leu-Leu-Leu-epoxyketone; 20 μM] is added and incubated at room temperature for 1 hour. Cell lysates are then denatured by adding 1% sodium dodecyl sulfate (SDS) and heating to 100°C, followed by mixing with 20 μL per well streptavidin-sepharose high-performance beads in a 96-well multiscreen DV plate and incubated for 1 hour. These beads are then washed with enzyme-linked immunosorbent assay (ELISA) buffer (PBS, 1% bovine serum albumin, and 0.1% Tween-20), and incubated overnight at 4°C on a plate shaker with antibodies to Proteasome subunits. Antibodies used included mouse monoclonal anti-β1, anti-β2, anti-β1i, and anti-β5i, goat polyclonal anti-β2i, and rabbit polyclonal anti-β5 (affinity-purified antiserum against KLH-CWIRVSSDNVADLHDKYS peptide). The beads are washed and incubated for 2 hours with horseradish peroxidase-conjugated secondary goat antirabbit, goat antimouse or rabbit antigoat antibodies. After washing, the beads are developed using the supersignal ELISA picochemiluminescence substrate. Luminescent detection is performed. Raw luminescence is converted to μg/mL by comparison with the standard curve and expressed as the % inhibition relative to vehicle control. Curve fits are generated using the following nonsigmoidal dose-response equation: Y = Bottom + (Top-Bottom)/(1 + 10̂((LogEC50 − X) × HillSlope)), where X is the logarithm of concentration, Y is the % inhibition, and EC50 is the dose of this compound showing 50% effect.
In vivo	Carfilzomib (PR-171) moderately reduces tumor growth in an in vivo xenograft model. It effectively decreases multiple myeloma cell viability following continual or transient treatment mimicking. This compound also increases trabecular bone volume, decreases bone resorption and enhances bone formation in non-tumor bearing mice.
References	[1] https://pubmed.ncbi.nlm.nih.gov/17591945/ [2] https://pubmed.ncbi.nlm.nih.gov/21247387/ [3] https://pubmed.ncbi.nlm.nih.gov/22763387/ [4] https://pubmed.ncbi.nlm.nih.gov/21750224/

Applications

Methods	Biomarkers	Images	PMID
Western blot	pERK / ERK / pSTAT5 / STAT5 / pPI3K / PI3K caspase-9 / caspase-8 c-PARP / PARP / caspase-3 Bcl-2 / Bcl-Xl / Mcl-1 / Bik / Bim / Bax / Bak Atg5 / Atg12 / Beclin-1 / LC3-II Noxa / Bik / Puma / Mcl-1 EGFR / HER2 / ER alpha / p-Akt(Ser473) / Akt / p-ERK / ERK / p53 BDP1 / HER2(Tyr1248) / HER2(Tyr1221/Tyr1222) / PARP1 / caspase-7 / p53 Mut HLA class I		24590311
Growth inhibition assay	Cell viability		27655642

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05552976	Recruiting	Relapsed or Refractory Multiple Myeloma	Bristol-Myers Squibb	January 10 2023	Phase 3
NCT05675449	Recruiting	Multiple Myeloma	Pfizer	December 14 2022	Phase 1
NCT05041933	Unknown status	Hematological Diseases	University Hospital Limoges	September 15 2021	--

Tech Support

Handling Instructions

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Frequently Asked Questions

Question 1:
How should I prepare a solution of it for an ongoing in vivo study?

Answer:
It can be dissolved in 2% DMSO/30% PEG 300/dd H₂O at 10 mg/ml as a suspension, and can be dissolved in 2% DMSO/castor oil at 10 mg/ml as a clear solution.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):