616452
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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关于此项目
经验公式（希尔记法）:
C17H13N5
化学文摘社编号:
分子量:
287.32
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
产品名称
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).
SMILES string
[nH]1ncc(c1c4nc(ccc4)C)c2nc3c(nccc3)cc2
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 key
LBPKYPYHDKKRFS-UHFFFAOYSA-N
assay
≥95% (HPLC)
form
solid
potency
23 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 5 mg/mL, methanol: 5 mg/mL
shipped in
ambient
Quality Level
storage temp.
2-8°C
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General description
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。
Biochem/physiol Actions
主靶
ALKS结合
ALKS结合
产物与ATP竞争。
次级靶标
ALK 5自身磷酸化(IC₅₀= 4 nM)
ALK 5自身磷酸化(IC₅₀= 4 nM)
细胞可渗透性：是
Packaging
用惰性气体包装
Preparation Note
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。
Other Notes
Gellibert, F., et al. 2004.J. Med. Chem.47, 4494.
Ichida, J. K., et al. 2009.Cell Stem Cell 5, 491.
Ichida, J. K., et al. 2009.Cell Stem Cell 5, 491.
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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