| A cell-permeable oxothiazolo-imidazo-pyridinylidene-benzoate that competitively blocks the activity of hematopoietic protein tyrosine phosphatase (HePTP) (IC50=210nM, Ki=211nM) and thereby induces sustained hyperactivation of ERK1/2 and p38 MAP kinase (in OKT3-stimulated Jurkat TAg T cells at 4uM, and in mouse leukocytes (3mg/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 73uM, respectively). Exhibits greater microsomal stability (t1/2=50 min in rat liver microsomes). Synonyms: HePTP Inhibitor, ML119, (Z)-2-(5-(7-Bromo-3-oxo[1,3]thiazolo(2,3:2,3)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 Molecular Formula: C20H10BrN3O4S Molecular Weight: 468.3 Purity: 98% (HPLC) Appearance: Greenish-yellow solid Solubility: DMSO (10mg/ml) Method for Determining Identity: Proton NMR Spectroscopic and Mass Spectrometric Analysis Primary Target: HePTP/PTPN7 Primary Target IC50: 210nM Primary Target Ki: 211nM for HePTP Storage and Stability: Store at 4C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Following reconstitution, aliquot and store at -20C. Stock solutions are stable for 6 months after receipt at -20C. Light sensitive. |
