375645

HePTP Inhibitor, ML119

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

• 別名: 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, (<
• 実験式（ヒル表記法）: C₂₀H₁₀BrN₃O₄S
• CAS番号: 357302-57-9
• 分子量: 468.28
• MDL番号: MFCD01470958
• UNSPSCコード: 12352200
• NACRES: NA.28

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• 形状: solid
• 有効性: 210 nM IC₅₀
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: green-yellow
• 溶解性: DMSO: 10 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C
• SMILES記法: BrC1=CC2=C(N(C(/C(S3)=C/C4=CC=C(C5=CC=CC=C5C(O)=O)O4)=O)C3=N2)N=C1

詳細

詳細

A cell-permeable oxothiazolo-imidazo-pyridinylidene-benzoate that competitively blocks the activity of hematopoietic protein tyrosine phosphatase (HePTP) (IC₅₀ = 210 nM; K_i = 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 (t_1/2 = 50 min in rat liver microsomes).

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
HePTP/PTPN7

Reversible: yes

Secondary Target
other phosphatases

Target K_i: 211 nM for HePTP

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 2
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable