| Bioactivity | PF-06260933 is an orally active and highly selective inhibitor of MAP4K4 with IC50s of 3.7 and 160 nM for kinase and cell, respectively. | ||||||||||||
| Invitro | PF-06260933 treatment of human aortic endothelial cell (EC) robustly prevents TNF-α-mediated endothelial permeability in vitro, similar to MAP4K4 knockdown[2]. | ||||||||||||
| In Vivo | In the mice model, PF-06260933 treatment does not alter plasma lipid content, although reductions in glucose levels are observed, which is consistent with whole-body-inducible Map4k4 knockout animals. PF-06260933 administration ameliorates further plaque development and/or promotes plaque regression in this animal model (46.0% versus 25.5%), and a reduction in plasma glucose as well as lipid content is also observed[2]. | ||||||||||||
| Name | PF-06260933 | ||||||||||||
| CAS | 1811510-56-1 | ||||||||||||
| Formula | C16H13ClN4 | ||||||||||||
| Molar Mass | 296.75 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Ammirati M, 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. [2]. Roth Flach RJ, et al. Endothelial protein kinase MAP4K4 promotes vascular inflammation and atherosclerosis. Nat Commun. 2015 Dec 21;6:8995. |
PF-06260933
CAS: 1811510-56-1 F: C16H13ClN4 W: 296.75
PF-06260933 is an orally active and highly selective inhibitor of MAP4K4 with IC50s of 3.7 and 160 nM for kinase and cel
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