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 |
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 . |
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 |
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 . |