HePTP Inhibitor, ML119 - Calbiochem (C15-1303-108)

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

Molecular Weight: 468.28. Empirical Formula: C₂₀H₁₀BrN₃O₄S. 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 2. Flash Point(F): Not applicable. Flash Point(C): Not applicable.