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1099644-42-4 (ITD-1)

1

Identification

ITD-1 ITD-1
Name ITD-1
Formula C27H29NO3
MW 415.52
CAS No. 1099644-42-4
EINECS
Smiles O=C(C1=C(C)NC2=C(C(CC(C)(C)C2)=O)C1C3=CC=C(C4=CC=CC=C4)C=C3)OCC
Synonyms ethyl 4-([1,1'-biphenyl]-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
InChI InChI=1S/C27H29NO3/c1-5-31-26(30)23-17(2)28-21-15-27(3,4)16-22(29)25(21)24(23)20-13-11-19(12-14-20)18-9-7-6-8-10-18/h6-14,24,28H,5,15-16H2,1-4H3
2

Introduction

ITD-1 is an inducer of TGFβ type II receptor degradation-1, is a potent and highly selective TGFβ pathway inhibitor (IC50 = 0.85 μM). IC50 value: 0.85 μM Target: TGFβ in vitro: ITD-1 selectively enhances the differentiation of uncommitted mesoderm to cardiomyocytes, but not to vascular smooth muscle and endothelial cells.

Background Information

Selective inhibitor of TGF-β signaling ......by AOBIOUS INC
ITD-1 is an inducer of TGFβ type II receptor degradation-1, is a potent and highly selective TGFβ pathway inhibitor (IC50 = 0.85 μM). IC50 value: 0.85 μM Target: TGFβ in vitro: ITD-1 selectively enhances the differentiation of uncommitted mesoderm to cardiomyocytes, but not to vascular smooth muscle and endothelial cells. ITD-1 is the first selective TGFβ inhibitor and reveals an unexpected role for TGFβ signaling in controlling cardiomyocyte differentiation from multipotent cardiovascular precursors. ITD-1 downregulates HA-TGFBR2 and TGFBR2-mCherry with nearly the same potency (IC50 = 1.05 and 1.31 μM, respectively). ITD-1 acts by enhancing degradation rather than by blocking synthesis, which would affect cell surface and intracellular receptor pools equally. ......by MedChemexpress Co., Ltd.
Selective inhibitor of TGF-<span class='symbol'>&#946;</span> signaling (IC<sub>50</sub> = 0.85 <span class='symbol'>&#956;</span>M); displays little or no inhibition of activin, Wnt or BMP signaling pathways. Induces proteasomal degradation of the TGF-<span class='symbol'>&#946;</span> type II receptor. Inhibits TGF-<span class='symbol'>&#946;</span>-induced mesoderm formation from mouse embryonic stem cells (ESCs) during early differentiation; selectively promotes the differentiation of ESCs to cardiomyocytes <em>in vitro</em> between days 3-5. Does not induce differentiation of vascular smooth muscle cells or endothelial cells. ......by Tocris Bioscience Inc.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:Light yellow to yellow Solid EBNumber:EB000071681

Storage condition

4°C by MedChemexpress Co., Ltd.
Store at +4&deg;C by Tocris Bioscience Inc.

Solubility

10 mM in DMSO by CHEMSCENE, LLC
10 mM in DMSO by MedChemexpress Co., Ltd.
Soluble to 20 mM in DMSO and to 10 mM in ethanol with gentle warming by Tocris Bioscience Inc.
5

Mechanism and Indication

Signaling Pathways TGF-beta/Smad
Target TGF-β Receptor
Research Area Cardiovascular Disease
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
ITD-1 - Not Found
ITD-1 - No Development Reported
7

Safety Data of ITD-1

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Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC 1mg/USD21() USA
CHEMSCENE, LLC USA
MedChemexpress Co., Ltd. 5mg/USD90(In stock);10mg/USD120(In stock);50mg/USD440(In stock);100mg/USD650(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. China
Tocris Bioscience Inc. USA
10

Related Products

Other Forms of 1099644-42-4

Name CAS No Formula MW

Recommended Compounds in TGF-β Receptor

Name CAS No Formula MW
K 02288 1431985-92-0 C20H20N2O4 352.38
ML347 1062368-49-3 C22H16N4O 352.39
DMH-1 1206711-16-1 C24H20N4O 380.44
LDN-212854 1432597-26-6 C25H22N6 406.48
SB-505124 (hydrochloride) 356559-13-2 C20H22ClN3O2 371.86
A 77-01 607737-87-1 C18H14N4 286.33
SB-505124 694433-59-5 C20H21N3O2 335.4
LY-364947 396129-53-6 C17H12N4 272.3
LDN193189 (Hydrochloride) 1062368-62-0 C25H26Cl4N6 552.33
SD-208 627536-09-8 C17H10ClFN6 352.75
RepSox 446859-33-2 C17H13N5 287.32
LDN193189 1062368-24-4 C25H22N6 406.48
A 83-01 909910-43-6 C25H19N5S 421.52
LY2109761 700874-71-1 C26H27N5O2 441.52
LY2157299 700874-72-2 C22H19N5O 369.42
GW788388 452342-67-5 C25H23N5O2 425.48
SB 525334 356559-20-1 C21H21N5 343.42
SB-431542 301836-41-9 C22H16N4O3 384.39
EW-7197 1352608-82-2 C22H18FN7 399.42
R-268712 879487-87-3 C20H18FN5O 363.39

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

12

References

13

More Information

ITD-1

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