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CAS No.: 1099644-42-4

ITD-1 Catalog No. CSN17464

Synonyms: ITD-1

ITD-1 is a selective TGFβ pathway inhibitor with IC50 of 0.85 μM and can act as an inducer of TGFβ type II receptor degradation.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 TGF-beta

IC50:0.85μM
描述TGF betas are members of a much larger gene family and are produced by a variety of cells and tissues which include T-cells, macrophages, platelets and bone^[1]. ITD-1 is the first selective TGFβ inhibitor and reveals an unexpected role for TGFβ signaling in controlling cardiomyocyte differentiation from multipotent cardiovascular precursors ^[3]. ITD-1 optimally promoted cardiogenesis and beating cell clusters when added from day 3-5 of differentiation. In contrast, ITD-1 completely abolished cardiogenesis when added before mesoderm induction, i.e. day 1-3 of differentiation, suggesting a bi-phasic effect of ITD-1 during differentiation of mESC, inhibiting mesoderm early and inducing cardiac fate later. Additionally, ITD-1 stimulated cardiomyocyte differentiation from uncommitted mesodermal progenitors in mouse and human ESCs, indicating that TGFβ represses cardiac fate at this developmental stage and it specifically stimulated cardiac differentiation from a cardiovascular progenitor ^[3].
作用机制ITD-1 is an inducer of TGFβ type II receptor degradation-1, is a potent and highly selective TGFβ pathway inhibitor (IC50 = 0.85 μM). It does not block the kinase activity of either type I (TGFBR1) or type II (TGFBR2) TGFβ receptors but potently blocks phosphorylation of the effector SMAD2/3 proteins induced by TGFβ2, and only minimally in response to Activin A.
参考文献

[1] Sun Z, Ettensohn CA. TGF-β sensu stricto signaling regulates skeletal morphogenesis in the sea urchin embryo. Dev Biol. 2017 Jan 15;421(2):149-160.
[2] Willems E, Cabral-Teixeira J, et al. Small molecule-mediated TGF-β type II receptor degradation promotes cardiomyogenesis in embryonic stem cells. Cell Stem Cell. 2012 Aug 3;11(2):242-52.
[3] Willems E, Cabral-Teixeira J, Schade D, Cai W, Reeves P, Bushway PJ, Lanier M, Walsh C, Kirchhausen T, Izpisua Belmonte JC, Cashman J, Mercola M. Small molecule-mediated TGF-β type II receptor degradation promotes cardiomyogenesis in embryonic stem cells. Cell Stem Cell. 2012 Aug 3;11(2):242-52. doi: 10.1016/j.stem.2012.04.025. PMID: 22862949; PMCID: PMC3419596.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4066 mL
- 12.0330 mL
- 24.0660 mL
- 5 mM
- 0.4813 mL
- 2.4066 mL
- 4.8132 mL
- 10 mM
- 0.2407 mL
- 1.2033 mL
- 2.4066 mL

技术信息

CAS号

1099644-42-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H29NO3

运输

蓝冰

分子量

415.52

别名

ITD-1

溶解度

DMSO	83.0 mg/mL (199.7 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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