ITD-1 MedChemExpress (MCE)

Product 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 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
EINECS
Chemical Formula	C27H29NO3
Molecular Weight	415.52
inchi
Package	10 mM * 1 mL;1 mg;5 mg;10 mg;50 mg;100 mg
Price	Email to quote
Descriptions	ITD-1 ITD-1 MedChemExpress (MCE) HY-12704 1099644-42-4 99.41% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions ITD-1 ITD-1 MedChemExpress (MCE) HY-12704 1099644-42-4 99.41% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. ITD-1 is the first selective TGFβ receptor inhibitor with an IC50 of 460 nM. 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[1]. For the Smad4-Response element (SBE4) assay, 293T cells are grown in Phenol Free DMEM-high glucose supplemented with 1% FBS. About 30000 cells/cm2 are reverse transfected onto white 384-well cell-culture plates with 10ng of SBE4-Lux and CMV-Renilla-Lux using Lipofectamine 2000. Cells are allowed to adhere for at least 12 hours and induced with either TGFβ2 (15 ng/mL), Activin A (15 ng/mL). Simultaneously, ITD-1 (0.001, 0.01, 0.1, 1, and 10 μM) is added to cells. SB-431542 is used as a positive control for Activin A/TGFβ-signaling inhibition. To determine luminescence levels, Dual-Glo kit is used and measured on an Envision plate reader. Firefly luminescence is normalized against renilla luciferase. IC50: 460 nM (TGFβ receptor) Cellular Effect Cell Line Type Value Description References \| \| \| \| \| \| \| \| \| \| [1]. Willems E, 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. [Content Brief]
Last Update	2025-04-01 14:45:47

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