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经验公式(希尔记法):
C28H27N3O3
化学文摘社编号:
分子量:
453.53
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.28
产品名称
Smad3抑制剂,SIS3, Smad3 Inhibitor, SIS3, CAS 1009104-85-1, is a cell-permeable, selective inhibitor of TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated signaling. Does not affect Smad2, MAPK, ERK, or PI3-K.
SMILES string
[n]1(c2ncccc2c(c1c5ccccc5)C=CC(=O)N3CCc4c(cc(c(c4)OC)OC)C3)C
InChI
1S/C28H27N3O3/c1-30-27(19-8-5-4-6-9-19)22(23-10-7-14-29-28(23)30)11-12-26(32)31-15-13-20-16-24(33-2)25(34-3)17-21(20)18-31/h4-12,14,16-17H,13,15,18H2,1-3H3
InChI key
IJYPHMXWKKKHGT-UHFFFAOYSA-N
assay
≥90% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white
solubility
DMSO: 15 mg/mL
ethanol: 5 mg/mL
shipped in
ambient
storage temp.
2-8°C
Quality Level
Application
Smad3(SIS3)的特异性抑制剂已被用于阻断转化生长因子(TGF)-β/母体十肽同系物3 (SMAD3)信号转导,以表征肺成纤维细胞中有助于信号转导子和转录激活子3(STAT3)活化的信号转导途径 。它也可用作无血清培养基中的SMAD3 抑制剂,用于评估其预防ARPE-19细胞中丙烯醛作用的能力。
Biochem/physiol Actions
Smad3(SIS3)的特异性抑制剂是一种吡咯并吡啶化合物。它选择性阻断转化生长因子(TGF)-β1-依赖型母体十肽同系物3 (Smad3) 磷酸化和Smad3介导的细胞途径,但是不影响Smad2, p38分裂素活化的蛋白质激酶(MAPK)、胞外信号调节激酶(ERK)或磷酸肌醇3-激酶(PI3K)信号传导。 通过其抑制功能, SIS3调节小鼠单侧输尿管梗阻(UUO)肾的纤维化、细胞凋亡和炎症。因此,SIS3可用作肾病抗纤维化治疗的有效药物。
主要靶标
TGF-β1依赖性Smad3磷酸化和Smad3介导的细胞信号转导
TGF-β1依赖性Smad3磷酸化和Smad3介导的细胞信号转导
Disclaimer
毒性:刺激性(B)
Other Notes
可逆:否
产物不与ATP竞争。
细胞可渗透性:是
Jinnin, M., et al. 2006.Mol.Pharmacol.69, 597.
产物不与ATP竞争。
细胞可渗透性:是
Jinnin, M., et al. 2006.Mol.Pharmacol.69, 597.
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3个月。
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
General description
Smad3 inhibitor is a cell-permeable pyrrolopyridine compound that selectively inhibits TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated cellular signaling with no effect on Smad2, p38 MAPK, ERK, or PI 3-K signaling.
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Xingli Ji et al.
Medical science monitor : international medical journal of experimental and clinical research, 24, 1633-1641 (2018-03-21)
BACKGROUND Fibrosis is the common pathological feature in most kinds of chronic kidney disease (CKD). TGF-β/Smads signaling is the master pathway regulating kidney fibrosis pathogenesis, in which Smad3 acts as the integrator of various pro-fibrosis signals. In this study, we
Yi Luo et al.
Stem cell research & therapy, 15(1), 4-4 (2024-01-04)
TMC1 is one of the most common deafness genes causing DFNA36. Patient-derived human induced pluripotent stem cells (iPSCs) provide an opportunity to modelling diseases. TMC1 p.M418K mutation in human is orthologous to Beethoven mice. Here, we investigated the differentiation, morphology
Jeffery Grigsby et al.
Current eye research, 37(11), 1045-1053 (2012-08-22)
Acrolein has been implicated in retinal pigment epithelium (RPE) cell death, and has been associated with diabetic retinopathy. Our purpose was to investigate the potential effect of high glucose in influencing acrolein-mediated RPE cytokine production and cell death. We investigated
Chaitali Chakraborty et al.
Nature communications, 14(1), 6446-6446 (2023-10-14)
Chromatin organization controls transcription by modulating 3D-interactions between enhancers and promoters in the nucleus. Alterations in epigenetic states and 3D-chromatin organization result in gene expression changes contributing to cancer. Here, we map the promoter-enhancer interactome and regulatory landscape of glioblastoma
Masatoshi Jinnin et al.
Molecular pharmacology, 69(2), 597-607 (2005-11-17)
This is the first report that characterizes specific inhibitor of Smad3 (SIS3) as a potent and selective inhibitor of Smad3 function. In the reporter assay, the increased luciferase activity of p3TP-lux by the overexpression of constitutively active form of ALK-5
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