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Merck
CN

616461

TGF-β RI激酶抑制剂VI，SB431542

TGF-β RI Kinase Inhibitor VI, SB431542, CAS 301836-41-9, is a cell-permeable inhibitor of SMAD2 phosphorylation. Inhibits the activity of ALK4 and ALK5 (IC50 = 140 nM and 94 nM, respectively).

别名:

TGF-β RI激酶抑制剂VI，SB431542, 4-[4-（3,4-亚甲二氧基苯基）-5-（2-吡啶基）-1H-咪唑-2-基]苯甲酰胺，二水合物，4-[4-（1,3-苯并二唑-5-基）-5-（2-吡啶基）-1H-咪唑-2-基]苯甲酰胺，二水合物，SB-431542

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关于此项目

化学文摘社编号:
301836-41-9
MDL number:
MFCD27976360
UNSPSC Code:
51111800
NACRES:
NA.77

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产品名称

TGF-β RI激酶抑制剂VI，SB431542, TGF-β RI Kinase Inhibitor VI, SB431542, CAS 301836-41-9, is a cell-permeable inhibitor of SMAD2 phosphorylation. Inhibits the activity of ALK4 and ALK5 (IC50 = 140 nM and 94 nM, respectively).

SMILES string

[nH]1c(nc(c1c4cc5c(cc4)OCO5)c3ncccc3)c2ccc(cc2)C(=O)N

InChI

1S/C22H16N4O3/c23-21(27)13-4-6-14(7-5-13)22-25-19(20(26-22)16-3-1-2-10-24-16)15-8-9-17-18(11-15)29-12-28-17/h1-11H,12H2,(H2,23,27)(H,25,26)

InChI key

FHYUGAJXYORMHI-UHFFFAOYSA-N

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

ethanol: 10 mg/mL
DMSO: 100 mg/mL

shipped in

ambient

Quality Level

300

storage temp.

2-8°C

Disclaimer

毒性：标准处理（A）

General description

一种细胞渗透性三芳基咪唑化合物，经证明可有效抑制NIH 3T3细胞中组成性活性ALK4、ALK5或ALK7的载体介导表达后的细胞Smad2磷酸化（10 µM抑制剂抑制>90%），而在表达活性ALK1、2、3或6的NIH 3T3培养物中，TGF-βⅠ型受体的其他成员对Smad1磷酸化几乎没有影响。当在无细胞激酶分析中直接测试时，SB431542被证明能有效抑制ALK4和ALK5的活性（IC50分别为140 nM和94 nM），而对包括ALK2和ALK6在内的24种其他激酶（IC50在10 µM ATP存在下为≥10 µM）没有效力或大大降低效力。据报道，当与PD0325901（目录号444966）和噻唑维文（目录号420220）一起使用时，4-TF诱导的成纤维细胞培养产生人类IPSC的效率提高了>200倍。

Packaging

用惰性气体包装

Legal Information

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

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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