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Merck
CN

528108

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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关于此项目

经验公式（希尔记法）:
C11H5F2NO4S
化学文摘社编号:
648449-76-7
分子量:
285.22
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD19705528

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color

off-white

SMILES string

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

assay

≥98% (HPLC)

form

solid

potency

180 nM Ki

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

solubility

DMSO: 10 mg/mL, ethanol: 5 mg/mL

shipped in

ambient

Quality Level

100

相关类别

General description

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.

Biochem/physiol Actions

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

Packaging

Packaged under inert gas

Preparation Note

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

Other Notes

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

Legal Information

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

Disclaimer

Toxicity: Irritant (B)

存储类别

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

相关内容

Human Kinome & InhibitorSelect™ Libraries

Human Kinome Poster: The InhibitorSelect™ Protein Kinase Inhibitor Libraries provide broad coverage of the human kinome as shown here. The depicted human kinome dendrogram of 518 kinases are classified into five broad groups, 90 families, and 145 subfamilies. Inhibitor coverage was assigned based upon published data related to potency (IC50, EC50, Kd, etc.) for individual kinases harvested from the literature. Colored dots denote which library contains an inhibitor with demonstrated potent activity against the designated kinase and do not necessarily reflect known specificity of the inhibitor. Coverage of lipid and atypical kinases are depicted as a separate dendrogram. As shown, Calbiochem® Protein Kinase Inhibitor Libraries cover all major kinase families including TK, CMGC, CAMK, AGC, CK1, STE, TKL, as well as Lipid or Atypical kinase families.

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