|
HePTP Inhibitor, ML119
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).
产品信息
Form Greenish-yellow solid
Primary Target HePTP/PTPN7
Primary Target IC50 210 nM
Primary Target Ki 211 nM for HePTP
Secondary target other phosphatases
Molar mass 468.3
Protect from Light 是的
Packaged under inert gas 是的
Cell permeable 是的
Reversible 是的
Purity ≥98% by HPLC
Solubility DMSO
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Standard Handling |