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PIK-75 (PI3K inhibitor)

产品价格: ¥890.00

最小起订量:暂无 可售数量:999盒

发货时限:
暂无
所在地区:
中国浙江杭州市
有效期至:
长期有效
最后更新:
2021-05-31 01:30:04
浏览次数:
221

产品详情

品牌名称:
Gene Operation
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.

StorageStore 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.

温馨提示:不可用于临床治疗。

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