product name
TGF-β RI 激酶抑制剂 IV, TGF-β RI Kinase Inhibitor IV, CAS 909910-43-6, is a cell-permeable, selective inhibitor of ALK-4/5/7-mediated signaling (IC₅₀ = 45, 12, and 7.5 nM, respectively).
质量水平
检测方案
≥97% (HPLC)
形式
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
pale yellow
溶解性
DMSO: 20 mg/mL
运输
ambient
储存温度
2-8°C
InChI
1S/C25H19N5S/c1-17-8-7-13-23(27-17)24-21(19-14-15-26-22-12-6-5-11-20(19)22)16-30(29-24)25(31)28-18-9-3-2-4-10-18/h2-16H,1H3,(H,28,31)
InChI key
HIJMSZGHKQPPJS-UHFFFAOYSA-N
一般描述
一种细胞渗透性三取代吡唑化合物，已显示在表达单个I型TGF-β受体的Mv1Lu R4-2转染子中选择性抑制ALK-4/5/7介导（荧光素酶转录活性测定中IC50分别为45、12和7.5 nM），但不抑制ALK-1/2/3/6介导的细胞信号。在浓度为1 µM的情况下，抑制HaCaT细胞中TGF-β-诱导的Smad2磷酸化和NMuMG细胞中的上皮间质转化。
生化/生理作用
主要靶标
ALK-4/5/7
ALK-4/5/7
产物不与ATP竞争。
可逆：否
细胞可渗透性：是
靶标IC50：抑制ALK-4/5/7介导的荧光素酶转录活性测定分别为45、12和7.5 nM
包装
用惰性气体包装
警告
毒性：有害（C）
重悬
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3个月。
其他说明
Tojo, M., et al. 2005.Cancer Sci.96, 791.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 3
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