ITD-1
ITD-1
CAS: 1099644-42-4
Molecular Formula: C27H29NO3
ITD-1 - Names and Identifiers
| Name | ITD-1 |
| Synonyms | ITD1 ITD 1 ITD-1 AOB6123 CS-1731 SCHEMBL3239096 ETHYL 4-{[1,1'-BIPHENYL]-4-YL}-2,7,7-TRIMETHYL-5-OXO-1,4,6,8-TETRAHYDROQUINOLINE-3-CARBOXYLATE 4-[1,1'-Biphenyl]-4-yl-1,4,5,6,7,8-hexahydro-2,7,7-trimethyl-5-oxo-3-quinolinecarboxylic acid ethyl ester 3-Quinolinecarboxylic acid, 4-[1,1'-biphenyl]-4-yl-1,4,5,6,7,8-hexahydro-2,7,7-trimethyl-5-oxo-, ethyl ester |
| CAS | 1099644-42-4 |
ITD-1 - Physico-chemical Properties
| Molecular Formula | C27H29NO3 |
| Molar Mass | 415.52 |
| Density | 1.18±0.1 g/cm3(Predicted) |
| Boling Point | 569.9±50.0 °C(Predicted) |
| Solubility | DMSO: < 9 mg/mL |
| pKa | 1.33±0.70(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | 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 (IC 50 = 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 . |
ITD-1 - Preparation solution concentration reference
| 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 |
| 5 mM | 0.048 ml | 0.241 ml | 0.481 ml |
Last Update：2024-01-02 23:10:35
ITD-1 - Reference Information
| biological activity | ITD-1 are effective TGF-β inhibitors. It does not inhibit the kinase activity of TGFBR1 or TGFBR, but can effectively inhibit the phosphorylation of the effector SMAD2/3 induced by TGFβ2, and has little effect on Activin A. |
| target | TargetValue TGF-β () |
| Target | Value |
| in vitro study | 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 (IC 50 = 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 . |
Last Update：2024-04-09 21:11:58
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