ITD 1|cas 1099644-42-4|DC Chemicals

Cas No.:	1099644-42-4
Chemical Name:	Ethyl 2,7,7-trimethyl-5-oxo-4-(4-phenylphenyl)-1,4,6,8-tetrahydroquinoline-3-carboxylate
Synonyms:	ITD 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
SMILES:	O=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]
Formula:	C₂₇H₂₉NO₃
M.Wt:	415.5241
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

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.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC7739	SD-208	SD-208 is a potent, orally active ATP-competitive transforming growth factor-β receptor 1 (TGF-βRI) inhibitor (IC50= 49 nM)
DC6312	SB525334	SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM, is 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6.
DC5189	SB-431542	SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM, 100-fold more selective for ALK5 than p38 MAPK and other kinases.
DC7259	Repsox（ALK5 Inhibitor II）	RepSox(E-616452; SJN 2511) is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation, respectively.
DC7587	ML347	ML347 is a selective BMP receptor inhibitor with IC50 of 32 nM for ALK2, >300-fold selectivity over ALK3. Also inhibits ALK1 activity with IC50 of 46 nM
DC10675	LY3200882	LY3200882 is a novel, highly selective TGFβRI small molecule inhibitor.
DC6306	LY2157299(Galunisertib)	LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM. Phase 2.
DC7914	LDN-214117	LDN-214117 is a potent and selective ALK2 inhibitor with IC50 of 22 nM; > 100 fold selectivity for ALK5; also inhibits BMP6(IC50=100 nM).
DC7742	K02288	K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA.
DC8028	ITD-1	ITD-1 is a novel and highly selective TGFβ pathway inhibitor. ITD-1 molecule turns stem cells into heart cells.