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Merck
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主要文件

528108

Sigma-Aldrich

PI 3-Kγ Inhibitor II

The PI 3-Kγ Inhibitor II, also referenced under CAS 648449-76-7, controls the biological activity of PI 3-Kγ. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

别名:

PI 3-Kγ Inhibitor II, 5-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethylene)-thiazolidine-2,4-dione, PI 3-K Inhibitor II

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About This Item

经验公式(希尔记法):
C11H5F2NO4S
分子量:
285.22
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77

质量水平

方案

≥98% (HPLC)

表单

solid

效能

180 nM Ki

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

off-white

溶解性

DMSO: 10 mg/mL
ethanol: 5 mg/mL

运输

ambient

储存温度

2-8°C

SMILES字符串

FC1(Oc2c(ccc(c2)\C=C3\SC(=O)NC\3=O)O1)F

InChI

1S/C11H5F2NO4S/c12-11(13)17-6-2-1-5(3-7(6)18-11)4-8-9(15)14-10(16)19-8/h1-4H,(H,14,15,16)/b8-4+

InChI key

SRLVNYDXMUGOFI-XBXARRHUSA-N

一般描述

A cell-permeable thiazolidinedione compound that acts as a potent and ATP-competitive inhibitor of PI 3-Kγ (Ki = 180 nM; IC50 = 250 nM). Exhibits great selectivity over PI 3-Kα (IC50 = 4.5 µM), PI 3-Kβ and δ (IC50 >20 µM), and shows little effect towards a large panel of receptors, unrelated enzymes, ion channels, and 38 commonly studied kinases. Shown to block MCP-1-mediated monocyte chemotaxis in vitro and exhibit better in vivo efficacy than LY294002 (Cat. No. 440202 and 440204) in blocking RANTES- or thioglycollate-induced peritoneal neutrophil recruitment by oral administration in a murine peritonitis model.

生化/生理作用

Cell permeable: yes
Primary Target
PI 3-Kγ
Product competes with ATP.
Reversible: no
Target IC50: 250 nM against PI 3-Kγ

包装

Packaged under inert gas

警告

Toxicity: Irritant (B)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Bilancio, A., et al. 2006. Blood107, 642.
Camps, M., et al. 2005. Nat. Med.11, 936.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

储存分类代码

11 - Combustible Solids

WGK

WGK 3


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Manoj K Rathinaswamy et al.
eLife, 10 (2021-03-05)
Class I Phosphoinositide 3-kinases (PI3Ks) are master regulators of cellular functions, with the class IB PI3K catalytic subunit (p110γ) playing key roles in immune signalling. p110γ is a key factor in inflammatory diseases and has been identified as a therapeutic

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