ITD-1
ITD-1 是第一个选择性的 TGFβ 受体抑制剂,IC50 为 460 nM。
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货号:
TK0483 -
规格:
- 1mg
- 5mg
- 10mg
- 50mg
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价格:
¥0.00
ITD-1 是第一个选择性的 TGFβ 受体抑制剂,IC50 为 460 nM。
| CAS No. | 1099644-42-4 |
| 生物活性 | ITD-1 is the first selective TGFβ receptor inhibitor with an IC50 of 460 nM. |
| 分子式 | C27H29NO3 |
| 分子量 | 415.52 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | Powder -20°C 3 years |
| 溶解性数据 | DMSO : 28 mg/mL (67.39 mM; Need ultrasonic and warming) |
| 体外研究 | ITD-1 potently blocks phosphorylation of the effector SMAD2/3 proteins induced by TGFβ2, and only minimally in response to Activin A. HEK293T cells are transfected with a Smad4 response element driving luciferase (SBE4-Luc) to test whether ITD-1 blocks Activin A/Nodal and/or TGFβ signaling, which utilize the same intracellular signaling cascade through Smad4. ITD-1 strongly inhibits TGFβ2 signaling with similar efficacy (92% vs. 99% respectively), but with lower potency compared to SB-431542, an ACVR1B/TGFBR1 kinase inhibitor (IC50= 850nM vs. 70nM respectively), and is a weak and partial inhibitor of Activin A signals. ITD-1 selectively enhances the differentiation of uncommitted mesoderm to cardiomyocytes, but not to vascular smooth muscle and endothelial cells. ITD-1 reveals an unexpected role for TGFβ signaling in controlling cardiomyocyte differentiation from multipotent cardiovascular precursors. |
| 文献 | •ACS Comb Sci. 2019 Dec 9;21(12):805-816. •Oncotarget. 2017 Dec 14;9(3):3188-3197. |
| 纯度及产品资料 | 98% |