Home MAPK JNK inhibitor JNK Inhibitor VIII For research use only.

JNK Inhibitor VIII

Synonyms: TCS JNK 6o

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. JNK Inhibitor VIII (TCS JNK 6o) inihibits JNK-1, JNK-2, and JNK-3 with Ki of 2 nM, 4 nM and 52 nM, respectively.

JNK Inhibitor VIII Chemical Structure

JNK Inhibitor VIII Chemical Structure

CAS No. 894804-07-0

Purity & Quality Control

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

JNK Inhibitor VIII Related Products

Signaling Pathway

JNK Signaling Pathways

JNK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation 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

Biological Activity

Description 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. JNK Inhibitor VIII (TCS JNK 6o) inihibits JNK-1, JNK-2, and JNK-3 with Ki of 2 nM, 4 nM and 52 nM, respectively.
Targets
JNK1 [1]
(Cell-free assay)		 JNK2 [1]
(Cell-free assay)		 JNK1 [1]
(Cell-free assay)		 JNK3 [1]
(Cell-free assay)		 JNK2 [1]
(Cell-free assay)
2 nM(Ki) 4 nM(Ki) 45 nM 52 nM(Ki) 160 nM
In vitro
In vitro

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 TCS-JNK-6a with the dimethoxy substitution of the phenyl ring. TCS-JNK-6o shows further gains in potency.[1]
Kinase Assay Ser/Thr-kinase
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), inhibitors (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.
Cell Research Cell lines hepG2 cells
Concentrations Serial concentrations
Incubation Time 1 h
Method

HepG2 human hepatoma cells (ATCC) are cultured in low glucose MEM supplemented with 1×NEAA, 1×sodium pyruvate, and 10% FBS. For P-c-Jun assays, cells are plated at 5×104 cells/well in 500 μL of complete media on 24-well collagen-coated plates and incubated overnight. Serial compound dilutions are made in DMSO at 100×, and then 5 μL is added directly to the media on the cells to provide the final inhibitor concentrations. After 1 h, cells are stimulated with vehicle control or TNFR for 30 min and harvested in 70μL of lysis buffer (TBS (54 mM Tris-HCl, pH 7.6, 150 mM NaCl), 1% TritonX-100,0.5% Nonidet P-40, 0.25% sodium deoxycholate, 1 mM EDTA, 1 mM EGTA, 0.5 mM sodium fluoride, 1 mM pervanadate, 1 μM microcystin, 1 mM AEBSF, 1 tablet of complete EDTA Free-Mini inhibitor cocktail) and frozen at -80 °C prior to use in the P-c-Jun assay.
In Vivo
In vivo

Pharmacokinetic profiles are determined for JNK Inhibitor VIII (TCS-JNK-6o) in Sprague-Dawley rats. JNK Inhibitor VIII (TCS-JNK-6o) showes 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.[1]
Animal Research Animal Models Sprague-Dawley rat
Dosages 5 mg/kg
Administration IV, Oral gavage

Chemical Information & Solubility

Molecular Weight 356.38 Formula

C18H20N4O4
CAS No. 894804-07-0 SDF --
Smiles CCOC1=C(C(=CC(=N1)NC(=O)CC2=C(C=CC(=C2)OC)OC)N)C#N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 71 mg/mL ( (199.22 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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