ITD-1 - TGF-β Receptor 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEITD-1Cat. No.: HY-12704CAS No.: 1099644-42-4分式: CHNO分量: 415.52作靶點(diǎn): TGF- Receptor作通路: TGF-beta/Smad儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 28 mg/mL (67.39 mM; Need ultrasonic and war

2、ming)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.02 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.02 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 ITD-1第個選擇性的 TGF 受體抑制劑，IC50 為 460 nM。IC50 & Target IC50:

3、 460 nM (TGF receptor)體外研究 ITD-1 potently blocks phosphorylation of the effector SMAD2/3 proteins induced by TGF2, and onlyminimally in response to Activin A. HEK293T cells are transfected with a Smad4 response element drivingluciferase (SBE4-Luc) to test whether ITD-1 blocks Activin A/Nodal and/or

4、TGF signaling, which utilize thesame intracellular signaling cascade through Smad4. ITD-1 strongly inhibits TGF2 signaling with similarefficacy (92% vs. 99% respectively), but with lower potency compared to SB-431542, an ACVR1B/TGFBR1kinase inhibitor (IC50= 850nM vs. 70nM respectively), and is a wea

5、k and partial inhibitor of Activin A signals.ITD-1 selectively enhances the differentiation of uncommitted mesoderm to cardiomyocytes, but not tovascular smooth muscle and endothelial cells. ITD-1 reveals an unexpected role for TGF signaling incontrolling cardiomyocyte differentiation from multipote

6、nt cardiovascular precursors.PROTOCOLCell Assay For the Smad4-Response element (SBE4) assay, 293T cells are grown in Phenol Free DMEM-high glucosesupplemented with 1% FBS. About 30000 cells/cm2 are reverse transfected onto white 384-well cell-cultureplates with 10ng of SBE4-Lux and CMV-Renilla-Lux u

7、sing Lipofectamine 2000. Cells are allowed to adherefor at least 12 hours and induced with either TGF2 (15 ng/mL), Activin A (15 ng/mL). Simultaneously, ITD-1(0.001, 0.01, 0.1, 1, and 10 M) is added to cells. SB-431542 is used as a positive control for Activin A/TGF-signaling inhibition. To determin

8、e luminescence levels, Dual-Glo kit is used and measured on an Envisionplate reader. Firefly luminescence is normalized against renilla luciferase.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Oncotarget. 2017 Dec 14;9(3):3188-3197.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Willems E, et al. Small molecule-mediated TGF- type II receptor degradation promotes cardiomyogenesis in embryonic stem cells. CellStem Cell. 2012 Aug 3;11(2):242-52.McePdfHeightCaution: Product has not been fully validated for medical