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Merck
CN

528117

PI 3-K抑制剂IX,PIK-90

The PI 3-K inhibitor IX, PIK-90, also referenced under CAS 677338-12-4, controls the biological activity of PI 3-K. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

别名:

PI 3-K抑制剂IX,PIK-90

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关于此项目

经验公式(希尔记法):
C18H17N5O3
化学文摘社编号:
分子量:
351.36
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
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InChI key

ZJAVHOMVDCMAMF-UHFFFAOYSA-N

InChI

1S/C18H17N5O3/c1-25-13-6-5-12-14(15(13)26-2)21-18(23-9-8-20-16(12)23)22-17(24)11-4-3-7-19-10-11/h3-7,10H,8-9H2,1-2H3,(H,21,22,24)

SMILES string

[n]21[c](c3c(nc2NC(=O)c4cnccc4)c(c(cc3)OC)OC)=NCC1

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

pale yellow

solubility

DMSO: 0.5 mg/mL

shipped in

wet ice

storage temp.

−20°C

Quality Level

General description

一种具有细胞渗透性的咪唑喹唑啉化合物,可作为一种针对全部三类PI 3-K激酶(p110α,p110γ、PI 3-KC2α,p110δ,PI 3-KC2β,p110β和hsVPS34的IC50 分别为11,18、47、58、64、350和830 nM)以及几种PIKK(DNA-PK,ATM和mTORC1的IC50 分别为13、610和1050 nM)和PI 4-KIIIα(IC50 =830 nM)的强效、可逆的ATP竞争性抑制剂,同时对PI 4-KIIIβ和ATR的效价大大降低(分别为IC50 =3.1和15 µM),对PI 4-KIIα,PIPK(IC50 >100 µM)以及一组36种常用研究的蛋白激酶(在2.5 µM时为<15% inhibition at 10 µM). Effectively suppreses insulin-stimulated phosphorylations of Akt and rpS6 in 3T3-L1 adipocytes and L6 myotubes in a dose-dependent manner in vitro (by >90%)的活性很小或没有活性,并完全防止小鼠体内胰岛素诱导的血糖下降(10 mg/ml,i.p.)。

Packaging

用惰性气体包装

Preparation Note

复溶后,等分并冷冻保存(-20°C)。贮备液在-20°C下可稳定保存至多3个月。
完全溶解可能需要轻微加热。

Other Notes

Fan, Q.W., et al. 2007.Cancer Res.67, 7960.
Fan, Q.W., et al. 2006.Cancer Cell9, 341.
Knight, Z.A., et al. 2006.Cell125, 733.

Legal Information

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

Disclaimer

毒性:标准处理(A)

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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