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Merck
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文件

616452

Sigma-Aldrich

RepSox

≥95% (HPLC), solid, TGF-β RI kinase inhibitor, Calbiochem

别名:

TGF-β RI激酶抑制剂II, ALK5抑制剂II,转化生长因子-βI型受体激酶抑制剂II,2-(3-(6-甲基吡啶-2-基)-1H-吡唑-4-基)-1,5-萘啶

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About This Item

经验公式(希尔记法):
C17H13N5
分子量:
287.32
MDL號碼:
分類程式碼代碼:
51111800
NACRES:
NA.77

product name

TGF-β RI激酶抑制剂II, TGF-β RI Kinase Inhibitor II, CAS 446859-33-2, is a cell-permeable, potent, reversible, ATP-competitive inhibitor of TGF-β R1 kinase (IC₅₀ = 23 nM and 4 nM for ALK5 binding & auto-phosphorylation).

品質等級

化驗

≥95% (HPLC)

形狀

solid

效力

23 nM IC50

製造商/商標名

Calbiochem®

儲存條件

OK to freeze
protect from light

顏色

yellow

溶解度

DMSO: 5 mg/mL
methanol: 5 mg/mL

運輸包裝

ambient

儲存溫度

2-8°C

InChI

1S/C17H13N5/c1-11-4-2-5-16(20-11)17-12(10-19-22-17)13-7-8-14-15(21-13)6-3-9-18-14/h2-10H,1H3,(H,19,22)

InChI 密鑰

LBPKYPYHDKKRFS-UHFFFAOYSA-N

一般說明

TGF-βⅠ型受体的细胞渗透性、有效性、选择性、可逆性和ATP竞争性抑制剂(ALK5;ALK5结合、ALK5自动磷酸化和HepG2细胞中TGF-β细胞分析的IC50分别为23 nM、4 nM和18 nM)。对包括p38 MAPK(IC50 >16 µM)在内的9种密切相关的激酶组的影响最小。
一种细胞渗透性萘啶基吡唑化合物,可作为TGF-βⅠ型受体的有效、选择性、可逆和ATP竞争性抑制剂(ALK5;ALK5结合、ALK5自动磷酸化和HepG2细胞中TGF-β细胞分析的IC50分别为23 nM、4 nM和18 nM)。对9种密切相关的激酶的影响最小,包括IC50 >16 µM的p38 MAPK。也可作为50 mM的DMSO溶液(目录号508158)提供。

生化/生理作用

主靶
ALKS结合
产物与ATP竞争。
次级靶标
ALK 5自身磷酸化(IC₅₀= 4 nM)
细胞可渗透性:是

包裝

用惰性气体包装

警告

毒性:标准处理(A)

重構

复溶后,等分并冷冻保存(-20°C)。贮备溶液在-20°C下可稳定保存至多6个月。

其他說明

Gellibert, F., et al. 2004.J. Med. Chem.47, 4494.
Ichida, J. K., et al. 2009.Cell Stem Cell 5, 491.

法律資訊

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

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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