PF-6260933

PF-6260933 is an inhibitor of mitogen-activated protein kinase kinase kinase kinase 4 (MAP4K4, IC50 = 3.7 nM). It is selective for MAP4K4 over a panel of 41 kinases at 1 µM but also inhibits TRAF2- and NCK-interacting kinase (TNIK) and misshapen-like kinase 1 (MINK1, IC50s = 15 and 8 nM, respectively). PF-6260933 inhibits the replication of CMV strains AD169 and Merlin(R1111) strains in human foreskin fibroblast (HFF) cells (EC50s = 9.6 and 13.3 µM, respectively). It inhibits collagen- or thrombin-induced aggregation of isolated human platelets by 70.9 and 61.2%, respectively, when used at a concentration of 20 µM. It decreases plaque formation in ApoE-/- mice fed a Western diet in a model of atherosclerosis when administered at a dose of 10 mg/kg. PF-6260933 (15 mg/kg) decreases LPS-induced increases in TNF-alpha levels in wild-type mice and fasting blood glucose levels in ob/ob mice.Formal Name: 5-(4-chlorophenyl)-3,3'-bipyridine]-6,6'-diamine. CAS Number: 1811510-56-1. Synonyms: PF-06260933. Molecular Formula: C16H13ClN4. Formula Weight: 296.8. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 1 mg/ml, DMSO: 1 mg/ml, Ethanol: insol, PBS (pH 7.2): insol. lambdamax: 222, 283 nm. SMILES: ClC1=CC=C(C2=C(N)N=CC(C3=CN=C(N)C=C3)=C2)C=C1. InChi Code: InChI=1S/C16H13ClN4/c17-13-4-1-10(2-5-13)14-7-12(9-21-16(14)19)11-3-6-15(18)20-8-11/h1-9H,(H2,18,20)(H2,19,21). InChi Key: KHPCIHZXOGHCLY-UHFFFAOYSA-N.