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JNK Inhibitor VIII JNK inhibitor

Name: JNK Inhibitor VIII
Brand: Selleck Chemicals
SKU: S7794
Rating: 5 (5 reviews)

Cat.No.S7794

JNK Inhibitor VIII (TCS JNK 6o) is an inhibitor of c-Jun N-terminal kinases with IC50 of 45 nM and 160 nM for JNK-1 and JNK-2, respectively. This compound inhibits JNK-1, JNK-2, and JNK-3 with Ki of 2 nM, 4 nM and 52 nM, respectively.

Chemical Structure

Molecular Weight: 356.38

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Quality Control

Batch: S779401 DMSO]71 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.77%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.77

Related Targets	ERK p38 MAPK Raf MEK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase
Other JNK Inhibitors	CC-90001 SP600125 JNK-IN-8 Anisomycin (Flagecidin) JNK Inhibitor IX Tanzisertib Hydrochloride (CC-930) Polyphyllin I DTP3 BI-78D3 Bentamapimod (AS602801)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description	PMID
NB7	Growth inhibition assay	Inhibition of human NB7 cell growth in a cell viability assay, IC50=2.27473μM	SANGER
LB2241-RCC	Growth inhibition assay	Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50=6.57739μM	SANGER
NCI-H1299	Growth inhibition assay	Inhibition of human NCI-H1299 cell growth in a cell viability assay, IC50=13.2019μM	SANGER
BV-173	Growth inhibition assay	Inhibition of human BV-173 cell growth in a cell viability assay, IC50=14.0505μM	SANGER
HPAF-II	Growth inhibition assay	Inhibition of human HPAF-II cell growth in a cell viability assay, IC50=14.5873μM	SANGER
RS4-11	Growth inhibition assay	Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=16.6795μM	SANGER
EW-1	Growth inhibition assay	Inhibition of human EW-1 cell growth in a cell viability assay, IC50=17.1883μM	SANGER
NCI-H1581	Growth inhibition assay	Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50=17.2588μM	SANGER
SK-PN-DW	Growth inhibition assay	Inhibition of human SK-PN-DW cell growth in a cell viability assay, IC50=17.9485μM	SANGER
KP-4	Growth inhibition assay	Inhibition of human KP-4 cell growth in a cell viability assay, IC50=19.1087μM	SANGER
DU-145	Growth inhibition assay	Inhibition of human DU-145 cell growth in a cell viability assay, IC50=19.8748μM	SANGER
ACHN	Growth inhibition assay	Inhibition of human ACHN cell growth in a cell viability assay, IC50=20.6213μM	SANGER
A172	Growth inhibition assay	Inhibition of human A172 cell growth in a cell viability assay, IC50=21.263μM	SANGER
HuO-3N1	Growth inhibition assay	Inhibition of human HuO-3N1 cell growth in a cell viability assay, IC50=21.4318μM	SANGER
QIMR-WIL	Growth inhibition assay	Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=22.3274μM	SANGER
NCI-H1650	Growth inhibition assay	Inhibition of human NCI-H1650 cell growth in a cell viability assay, IC50=22.7873μM	SANGER
SW1088	Growth inhibition assay	Inhibition of human SW1088 cell growth in a cell viability assay, IC50=23.1641μM	SANGER
Mewo	Growth inhibition assay	Inhibition of human Mewo cell growth in a cell viability assay, IC50=23.3997μM	SANGER
NCI-H1355	Growth inhibition assay	Inhibition of human NCI-H1355 cell growth in a cell viability assay, IC50=24.6365μM	SANGER
SK-LU-1	Growth inhibition assay	Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50=27.058μM	SANGER
KYSE-70	Growth inhibition assay	Inhibition of human KYSE-70 cell growth in a cell viability assay, IC50=27.125μM	SANGER
KP-N-YS	Growth inhibition assay	Inhibition of human KP-N-YS cell growth in a cell viability assay, IC50=27.5706μM	SANGER
HTC-C3	Growth inhibition assay	Inhibition of human HTC-C3 cell growth in a cell viability assay, IC50=27.7345μM	SANGER
NB17	Growth inhibition assay	Inhibition of human NB17 cell growth in a cell viability assay, IC50=27.9113μM	SANGER
GOTO	Growth inhibition assay	Inhibition of human GOTO cell growth in a cell viability assay, IC50=27.9415μM	SANGER
BEN	Growth inhibition assay	Inhibition of human BEN cell growth in a cell viability assay, IC50=29.865μM	SANGER
HMV-II	Growth inhibition assay	Inhibition of human HMV-II cell growth in a cell viability assay, IC50=30.1553μM	SANGER
SF295	Growth inhibition assay	Inhibition of human SF295 cell growth in a cell viability assay, IC50=32.156μM	SANGER
MPP-89	Growth inhibition assay	Inhibition of human MPP-89 cell growth in a cell viability assay, IC50=33.5199μM	SANGER
LCLC-103H	Growth inhibition assay	Inhibition of human LCLC-103H cell growth in a cell viability assay, IC50=34.2223μM	SANGER
MN-60	Growth inhibition assay	Inhibition of human MN-60 cell growth in a cell viability assay, IC50=36.0139μM	SANGER
BB65-RCC	Growth inhibition assay	Inhibition of human BB65-RCC cell growth in a cell viability assay, IC50=36.1528μM	SANGER
BHY	Growth inhibition assay	Inhibition of human BHY cell growth in a cell viability assay, IC50=36.9645μM	SANGER
SK-MEL-3	Growth inhibition assay	Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=37.7324μM	SANGER
NY	Growth inhibition assay	Inhibition of human NY cell growth in a cell viability assay, IC50=37.7592μM	SANGER
CAL-72	Growth inhibition assay	Inhibition of human CAL-72 cell growth in a cell viability assay, IC50=37.9289μM	SANGER
ES3	Growth inhibition assay	Inhibition of human ES3 cell growth in a cell viability assay, IC50=38.1949μM	SANGER
NBsusSR	Growth inhibition assay	Inhibition of human NBsusSR cell growth in a cell viability assay, IC50=39.3132μM	SANGER
NB10	Growth inhibition assay	Inhibition of human NB10 cell growth in a cell viability assay, IC50=40.1731μM	SANGER
ChaGo-K-1	Growth inhibition assay	Inhibition of human ChaGo-K-1 cell growth in a cell viability assay, IC50=41.1576μM	SANGER
KYSE-450	Growth inhibition assay	Inhibition of human KYSE-450 cell growth in a cell viability assay, IC50=41.4514μM	SANGER
SK-MEL-1	Growth inhibition assay	Inhibition of human SK-MEL-1 cell growth in a cell viability assay, IC50=41.9927μM	SANGER
PC-3	Growth inhibition assay	Inhibition of human PC-3 cell growth in a cell viability assay, IC50=42.2752μM	SANGER
KARPAS-299	Growth inhibition assay	Inhibition of human KARPAS-299 cell growth in a cell viability assay, IC50=44.5948μM	SANGER
DBTRG-05MG	Growth inhibition assay	Inhibition of human DBTRG-05MG cell growth in a cell viability assay, IC50=44.6546μM	SANGER
HCC1806	Growth inhibition assay	Inhibition of human HCC1806 cell growth in a cell viability assay, IC50=45.2169μM	SANGER
NCI-H2009	Growth inhibition assay	Inhibition of human NCI-H2009 cell growth in a cell viability assay, IC50=45.2843μM	SANGER
HCC2157	Growth inhibition assay	Inhibition of human HCC2157 cell growth in a cell viability assay, IC50=45.7976μM	SANGER
EM-2	Growth inhibition assay	Inhibition of human EM-2 cell growth in a cell viability assay, IC50=47.4011μM	SANGER
DOK	Growth inhibition assay	Inhibition of human DOK cell growth in a cell viability assay, IC50=48.3877μM	SANGER
HepG2	Function assay	Inhibition of cJun phosphorylation in HepG2 cell line, Ki=0.004μM	16759099
HepG2	Function assay	Inhibition of cJun phosphorylation in HepG2 cell line, EC50=0.92μM	16759099
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	356.38	Formula	C₁₈H₂₀N₄O₄	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	894804-07-0	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	TCS JNK 6o			Smiles	CCOC1=C(C(=CC(=N1)NC(=O)CC2=C(C=CC(=C2)OC)OC)N)C#N

Solubility

In vitro
Batch:

DMSO : 71 mg/mL (199.22 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.
	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.	3.550mg/ml (9.96mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.700mg/ml (4.77mM)

In vivo Formulation Calculator (Clear solution)

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

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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.
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Mechanism of Action

Targets/IC₅₀/Ki	JNK1 (Cell-free assay) 2 nM(Ki) JNK2 (Cell-free assay) 4 nM(Ki) JNK1 (Cell-free assay) 45 nM JNK3 (Cell-free assay) 52 nM(Ki) JNK2 (Cell-free assay) 160 nM
In vitro	JNK Inhibitor VIII (TCS-JNK-6a) binds competitively and reversibly to the ATP site. This compound demonstrates a remarkable selectivity profile. Additionally, it shows some inhibition of c-Jun phosphorylation in hepG2 cells. TCS-JNK-6o is a 2,5-dimethoxy analogue of this chemical with the dimethoxy substitution of the phenyl ring. This compound shows further gains in potency.
Kinase Assay	Ser/Thr-kinase
Kinase Assay	Ser/Thr-kinase assays are performed using a radioactive FlashPlate-based assay platform. In this format, biotinylated substrate peptide (2 μM), γ-[³³P]-ATP (5 μM, 2 mCi/μmol), this compound (3-10000 nM in 2% DMSO), and enzyme are incubated for 1 h in buffer containing 25 mM Hepes, pH 7.5, 1 mM DTT, 10 mM MgCl2, 100 μM Na3VO4, and 0.075 mg/mL Triton X-100, stopped with 80 μL of stop buffer containing 100 mM EDTA and 4 M NaCl, transferred to streptavidin-coated 384-well FlashPlates, which are then washed 3 times and read using a TopCount microplate reader.
In vivo	Pharmacokinetic profiles are determined for JNK Inhibitor VIII (TCS-JNK-6o) in Sprague-Dawley rats. This compound shows a short half-life of roughly 1 h, with rapid clearance and barely measurable bioavailability. Microsomal incubation studies revealed that oxidative metabolism is very rapid with this compound.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16759099/

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