PP1 (Src Inhibitor)

PP1 is a potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases. It inhibits p56lck (IC50 = 5 nM), p59fynT (IC50 = 6 nM), Hck (IC50 = 20 nM), and Src (IC50 = 170 nM) without significantly affecting the activity of EGFR kinase (IC50 = 250 nM), JAK2 (IC50 = 50 µM), or ZAP-70 (IC50 > 0.6 µM). PP1 inhibits anti-CD3-induced tyrosine phosphorylation of human T cells with an IC50 value of 600 nM. It exhibits antitumor activity by antagonizing both proliferation and the inhibition of apoptosis mediated by a stem cell factor/mast cell growth factor in hematopoietic and small cell lung cancer cell lines. PP1 also blocks TGF-beta-mediated cellular responses by directly inhibiting type I TGF-beta receptors (IC50 = 50 nM) in a manner unrelated to Src signaling.Formal Name: 1-(1,1-dimethylethyl)-3-(4-methylphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine. CAS Number: 172889-26-8. Synonyms: AGL 1872, EI 275. Molecular Formula: C16H19N5. Formula Weight: 281.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMF:PBS (pH 7.2) (1:9): 0.1 mg/ml, DMSO: 1 mg/ml, Ethanol: 0.1 mg/ml. lambdamax: 254, 284 nm. SMILES: CC(C=C1)=CC=C1C2=NN(C(C)(C)C)C3=NC=NC(N)=C32. InChi Code: InChI=1S/C16H19N5/c1-10-5-7-11(8-6-10)13-12-14(17)18-9-19-15(12)21(20-13)16(2,3)4/h5-9H,1-4H3,(H2,17,18,19). InChi Key: ZVPDNRVYHLRXLX-UHFFFAOYSA-N.