PIK-75 (PI3K inhibitor）

Biological Activity

PIK-75 is a preferential inhibitor of p110α/γ forms of phosphatidylinositol 3-kinase (PI3K), which inhibits p110α, -γ,–δ and –β with IC_50s of 5.8 nM, 76 nM, 0.51 μM and 1.3 μM, respectively. The compound potently inhibits PI_(3,4)P₂ and PIP₃ production in adipocytes, and PIP₃ production in myotubes ^[1], as well as blocks insulin-induced PKB phosphorylation on both Ser⁴⁷³ and Thr³⁰⁸ in CHO-IR cells (IC₅₀ = 78 nM ) and 3T3-L1 cells ^[2],all results show that p110α is the major PI3K isoform responsible for insulin signaling. PIK-75 completely suppresses adipocyte differentiation ^[3]. PIK-75 possesses anti-inflammatory potentiality. It potently and dose-dependently inhibits in vitro and in vivo production of TNF-α and IL-6,diminishes the induced expression of endothelial cell adhesion molecules (E-selectin, ICAM-1 and VCAM-1) and blocks monocyte-endothelial cell adhesion. Orally administration of PIK-75 significantly suppresses the macroscopic and histologic abnormalities associated with dextran sulfate sodium-induced murine colitis ^[4]. PIK-75 has been demonstrated to be a competitive inhibitor with respect to a substrate, phosphatidylinositol (PI) in contrast to most other PI3K inhibitors, which bind at or near the ATP site ^[5].

Chemical Properties

Cas No.: 372196-67-3	M. Wt.: 452.28
Formula: C16H14BrN5O4S	Purity: >99%
Synonym: PIK75, PI3-Kinase α Inhibitor VIII
Chemical Name: 2-methyl-5-nitro-2-[(6-bromoimidazo[1,2-α]pyridin-3-yl)methylene]-1-methylhydrazide-benzenesulfonic acid
Appearance: A crystalline solid
Solubility: Soluble in DMSO, very poorly soluble in water.
Storage：Store solid at -20 ºC for the stability up to two years.

Application Concentration (Just for reference)

The appropriate working concentration of PIK-75 depends on cell types, cell culture properties and specific applications. It is recommended that researchers start with optimal experiments for first use.