JNK Inhibitor VIII

別名: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化学構造

CAS No. 894804-07-0

サイズ 価格(税別) 在庫状況
JPY 37500 国内在庫あり
JPY 73500 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(4)

製品安全説明書

現在のバッチを見る: S779401 DMSO] 71 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false 純度: 99.77%
99.77

JNK Inhibitor VIII関連製品

シグナル伝達経路

JNK阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 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
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生物活性

製品説明 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.
細胞実験 細胞株 hepG2 cells
濃度 Serial concentrations
反応時間 1 h
実験の流れ

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]

動物実験 動物モデル Sprague-Dawley rat
投与量 5 mg/kg
投与経路 IV, Oral gavage

化学情報

分子量 356.38 化学式

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
保管 3 years -20°C powder

In vitro
Batch:

DMSO : 71 mg/mL ( (199.22 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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