For research use only. Not for therapeutic Use.
Potent and selective MAP4K4 inhibitor (IC50 value 3.7 nM for MAP4K4 a.k.a. HGK or ZC1) with suitable PK properties in mouse to be used as a tool in an in vivo model of diabetes, vascular inflammation and atherosclerosis. Robustly prevented TNF-α-mediated endothelial permeability in vitro, similar to MAP4K4 knockdown, and without alteration of plasma lipid content.
Keywords: PF 06260933 dihydrochloride | supplier | MAP4K4 inhibitor | PF06260933 | PF-06260933 | CAS [1883548-86-4] | [1811510-56-1] | MAPK | MAP4K | Inhibitor | HGK | ZC1 | mitogen activated | endothelial | diabetes | vascular inflammation | atherosclerosis | TNF | NF-κB | Enzymes
Catalog Number | I011985 |
CAS Number | 1883548-86-4 |
Molecular Formula | C16H13ClN4.2HCl |
Purity | ≥95% |
IUPAC Name | 5-(6-aminopyridin-3-yl)-3-(4-chlorophenyl)pyridin-2-amine;dihydrochloride |
InChI | InChI=1S/C16H13ClN4.2ClH/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);2*1H |
SMILES | C1=CC(=CC=C1C2=C(N=CC(=C2)C3=CN=C(C=C3)N)N)Cl.Cl.Cl |
Reference | M. Ammirati et al. Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment. ACS Med Chem Lett. 2015 Oct 6;6(11):1128-33.
R.J. Roth Flach et al. Endothelial protein kinase MAP4K4 promotes vascular inflammation and atherosclerosis. Nat Commun. 2015 Dec 21;6:8995. |