CH5132799 selectively inhibits class I PI3Ks, such as PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ with IC50 values of 0.014, 0.12, 05.0, and 0.36 μM, respectively. CH5132799 shows less inhibition of class II PI3Ks, class III PI3ks, and mTOR. CH5132799 suppresses phosp
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
PI3-kinase class I inhibitor
Product Description
CH5132799 inhibits class I PI3Ks, particularly PI3Kα with IC50 of 14 nM; less potent to PI3Kβδγ, while sensitive in PIK3CA mutations cell lines. A PI3K and FRAP inhibitor
1.Ohwada J, Ebiike H, Kawada H, Tsukazaki M, Nakamura M, Miyazaki T, Morikami K, Yoshinari K, Yoshida M, Kondoh O et al.. (2011) Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799.. Bioorg Med Chem Lett, 21 (6):(1767-72). [PMID:21316229][10.1021/op500134e]
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