ITD-1 --- TGFβ inhibitor


Catalog No. size PriceQuantity
M60060-2D 10 mM in DMSO (0.482 mL) $139
M60060-2S 2mg solid $139
M60060-10S 10mg solid $549

Description

ITD-1 is a novel and highly selective TGFβ pathway inhibitor identified by a high throughput, embryonic stem cell (ESC) cardiac differentiation screening. ITD-1 promoted cardiomyocyte differentiation specifically via degradation of the TGFβ type II receptor (TGFBR2), effectively clearing the receptor from the cell surface and selectively inhibiting intracellular signaling (IC50 0.4–0.8 µM), revealing a role for TGFβ signaling mechanism as a repressor of cardiomyocyte fate. ITD-1 selectively enhanced the differentiation of uncommitted mesoderm to cardiomyocytes, but not to vascular smooth muscle and endothelial cells. In contrast to other commonly used TGFβ receptor (ALK) inhibitors, ITD-1 importantly only inhibits TGFβ signaling, but does not block the closely related Activin A signaling pathway, and represents a unique reagent for exploring TGFβ function in various biological contexts such as embryonic development and models of disease.

Product information

CAS Number: 1099644-42-4

Molecular Weight: 415.52

Formula: C27H29NO3

Chemical Name: ethyl 4-([1,1'-biphenyl]-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate

Smiles: CC1NC2CC(C)(C)CC(=O)C=2C(C=1C(=O)OCC)C1C=CC(=CC=1)C1C=CC=CC=1

InChiKey: ULFUJLFTRWWLPO-UHFFFAOYSA-N

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

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 50 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

ITD-1 was used at 5 µM final concentration in vitro and in cellular assays.

References:

  1. Willems E, et al. Small Molecule-Mediated TGF-β Type II Receptor Degradation Promotes Cardiomyogenesis in Embryonic Stem Cells. (2012) Cell Stem Cell.11(2):242-52.

Products are for research use only. Not for human use.


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