产品描述: | ITD-1是有效的TGF-β抑制剂。它不抑制TGFBR1或TGFBR的激酶活性,但能够有效地抑制TGFβ2诱导的效应因子SMAD2/3磷酸化,对Activin A的影响甚微 |
靶点: |
TGF-β;TGF-beta/Smad |
体外研究: |
ITD-1, a small molecule inhibitor of TGF-β signaling, can partially induce proteasomal degradation of the TβR232,33, and blocks Smad and MAPK activation |
体内研究: |
ITD-1 partially inhibits TGF-β signaling and renal fibrosis in unilateral ischemia-reperfusion injury (UIRI) mice |
细胞实验: |
Cell lines: NRK-49F cells Concentrations: 3 μM Incubation Time: 1 h Method: NRK-49F cells are pre-incubated with KP1 (10 µg/ml, 3 μM) or ITD-1 (3 μM) for 1 h, and then treated with TGF-β1 (2 ng/ml) for 45 min. Western blot analyses the protein levels of p-Smad3 and p-p38. |
参考文献: |
1. Erik Willems, et al. Small molecule-mediated TGF-β type II receptor degradation promotes cardiomyogenesis in embryonic stem cells. Cell Stem Cell. 2012, 11(2):242-52. 2. Yuan Q, et al. A Klotho-derived peptide protects against kidney fibrosis by targeting TGF-β signaling. Nat Commun. 2022 Jan 21;13(1):438. |
溶解性: |
soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.407 ml |
12.033 ml |
24.066 ml |
5 mM |
0.481 ml |
2.407 ml |
4.813 ml |
10 mM |
0.241 ml |
1.203 ml |
2.407 ml |
50 mM |
0.048 ml |
0.241 ml |
0.481 ml |
|
注意: |
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