DC Chemicals · Product datasheet

ITD-1 — Datasheet

CAT. NO. DC8028

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ParameterValue
Chemical NameEthyl 2,7,7-trimethyl-5-oxo-4-(4-phenylphenyl)-1,4,6,8-tetrahydroquinoline-3-carboxylate
CAS No.1099644-42-4
SynonymsITD 1;ITD-1;ITD1;AOB6123;BCP15865;BC600702;AK546995;J3.518.866E;ethyl 4-(biphenyl-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate;ethyl 2,7,7-trimethyl-5-oxo-4-(4-phenylphenyl)-1,4,5,6,7,8-hexahydro-3-quinolinecarboxylate;4-[1,1'-Biphenyl]-4-yl-1,4,5,6,7,8-hexahydro-2,7,7-trimethyl-5-oxo-3-quinoline;Ethyl 2,7,7-trimethyl-5-oxo-4-(4-phenylphenyl)-1,4,6,8-tetrahydroquinoline-3-carboxylate;(+)-ITD-1;BCP29917;s6713;ITD-1, (+)-;ethyl 2,7,7-trimethyl-5-oxo-4-(4-phenylphenyl)-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate;2,7,7-Trimethyl-4-(biphenyl-4-yl)-5-oxo-1,4,5,6,7,8-hexahydroquinoli
FormulaC27H29NO3
M.Wt415.5241
SMILESO=C1C2C([H])(C3C([H])=C([H])C(C4C([H])=C([H])C([H])=C([H])C=4[H])=C([H])C=3[H])C(C(=O)OC([H])([H])C([H])([H])[H])=C(C([H])([H])[H])N([H])C=2C([H])([H])C(C([H])([H])[H])(C([H])([H])[H])C1([H])[H]
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

ITD-1 is the first selective TGFβ inhibitor with an IC50 of 460 nM.

In Vitro

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.

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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