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375645

Sigma-Aldrich

HePTP Inhibitor, ML119

The HePTP Inhibitor, ML119 controls the biological activity of HePTP. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

别名:

HePTP Inhibitor, ML119, (Z)-2-(5-(7-Bromo-3-oxo[1,3]thiazolo(2ʹ,3ʹ:2,3)imidazo[4,5-b]pyridin-2(3H)-ylidene)methyl)furan-2-yl)benzoic acid, PTPN7 Inhibitor, ML119, CID1357397, CD45 Inhibitor IV, Dusp6/MKP3 Inhibitor II, EC-PTP/PCPTP1 Inhibitor II, Lyp Inhibitor II, PTP Inhibitor XXX, PTP-SL Inhibitor II, PTP1B Inhibitor VIII, PTPN2/TCPTP Inhibitor III, SHP1 Inhibitor VIII, SHP2 Inhibitor V, STEP Inhibitor, VHR Inhibitor III, CD45 Inhibitor IV, Dusp6/MKP3 Inhibitor II, EC-PTP/PCPTP1 Inhibitor II, Lyp Inhibitor II, PTP Inhibitor XXX, PTP-SL Inhibitor II, PTP1B Inhibitor VIII, PTPN2/TCPTP Inhibitor III, SHP1 Inhibitor VIII, SHP2 Inhibitor V, STEP Inhibitor, VHR Inhibitor III, (<

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About This Item

经验公式（希尔记法）:
C20H10BrN3O4S
CAS号:
357302-57-9
分子量:
468.28
MDL编号:
MFCD01470958
UNSPSC代码:
12352200
NACRES:
NA.28

质量水平

100

方案

≥98% (HPLC)

表单

solid

效能

210 nM IC50

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

green-yellow

溶解性

DMSO: 10 mg/mL

运输

ambient

储存温度

2-8°C

SMILES字符串

BrC1=CC2=C(N(C(/C(S3)=C/C4=CC=C(C5=CC=CC=C5C(O)=O)O4)=O)C3=N2)N=C1

InChI

1S/C20H10BrN3O4S/c21-10-7-14-17(22-9-10)24-18(25)16(29-20(24)23-14)8-11-5-6-15(28-11)12-3-1-2-4-13(12)19(26)27/h1-9H,(H,26,27)/b16-8-

InChI key

NMLOLMOZTQCQJF-PXNMLYILSA-N

一般描述

A cell-permeable oxothiazolo-imidazo-pyridinylidene-benzoate that competitively blocks the activity of hematopoietic protein tyrosine phosphatase (HePTP) (IC50 = 210 nM; Ki = 211 nM) and thereby induces sustained hyperactivation of ERK1/2 and p38 MAP kinase (in OKT3-stimulated Jurkat TAg T cells at 4 µM, and in mouse leukocytes (3 mg/kg, i.p.)) without affecting MEK and Akt. Shown to interact with the catalytic pocket of HePTP loop and act as a pTyr mimetic. Displays adequate selectivity over HePTP-H237A, MKP-3, VHR, STEP, PTP-SL, PTP1B, LYP, TCPTP, SHP1, SHP2, CD45 and PAR phosphatases (IC50 = 2.8, 5.2, 1.9, 6.3, 1.1, 1.7, 1.9, 1.0, 2.5, 1.1, 3.1 and 73 µM, respectively). Exhibits greater microsomal stability (t1/2 = 50 min in rat liver microsomes).

生化/生理作用

Cell permeable: yes
Primary Target
HePTP/PTPN7
Reversible: yes
Secondary Target
other phosphatases
Target Ki: 211 nM for HePTP

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Sergienko, E., et al. 2012. ACS Chem. Biol.7, 367.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

储存分类代码

11 - Combustible Solids

WGK

WGK 2

闪点(°F)

Not applicable

闪点(°C)

Not applicable

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