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.

• Synonym(s): 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, (<
• Empirical Formula (Hill Notation): C₂₀H₁₀BrN₃O₄S
• CAS Number: 357302-57-9
• Molecular Weight: 468.28
• MDL number: MFCD01470958
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: solid
• potency: 210 nM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: green-yellow
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: BrC1=CC2=C(N(C(/C(S3)=C/C4=CC=C(C5=CC=CC=C5C(O)=O)O4)=O)C3=N2)N=C1

Description

General description

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).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
HePTP/PTPN7

Reversible: yes

Secondary Target
other phosphatases

Target K_i: 211 nM for HePTP

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable