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| 货号： | IPA1007-0005MG |
| 保存条件： | -20℃ |
| CAS号： | 372196-67-3 |
| 供应商： | 上海伟进生物科技有限公司 |
| 数量： | 10 |
| 英文名： | PIK-75 |
| 保质期： | 2 years |
| 规格： | 5mg |
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 IC50s 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.
[VIP第1年] 指数:2
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