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SB-505124 hydrochloride

Catalog No. T21637 CAS 356559-13-2

SB-505124 hydrochloride functions as a selective, concentration-dependent inhibitor targeting TGF-β Receptor type I (ALK4, ALK5, ALK7), exhibiting IC50 values of 129 nM for ALK4 and 47 nM for ALK5. Notably, it does not affect ALK1, 2, 3, or 6.

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SB-505124 hydrochloride Chemical Structure

SB-505124 hydrochloride, CAS 356559-13-2

Pack Size	Availability	Price/USD	Quantity
2 mg	5 days	$ 46.00
5 mg	5 days	$ 93.00

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Description	SB-505124 hydrochloride functions as a selective, concentration-dependent inhibitor targeting TGF-β Receptor type I (ALK4, ALK5, ALK7), exhibiting IC50 values of 129 nM for ALK4 and 47 nM for ALK5. Notably, it does not affect ALK1, 2, 3, or 6.
In vitro	SB-505124 is non-toxic to renal epithelial A498 cells at levels up to 100 μM over 48 hours. It also inhibits ALK4 (IC 50 = 129±11 nM), approximately 2.5 times less sensitive than ALK5, without affecting ALK2 at concentrations up to 10 μM. At a concentration of 1 μM, SB-505124 effectively prevents TGF-β-induced Smad2 phosphorylation in a concentration-dependent manner across three cell lines. Moreover, at 1 or 5 μM, it significantly blocks TGF-β-triggered activation of JNK/SAP, extracellular signal-regulated kinase 1/2, and p38, despite varying activation patterns observed in the cells. At 10 μM, SB-505124 disrupts Smad2 phosphorylation and reduces CTGF and α-SMA expression in vitro. Additionally, it suppresses CTGF and α-SMA expression as observed through immunofluorescence. Application of SB-505124 during glaucoma filtration surgery (GFS) enhances cell outgrowth from eye explants, contrasting with the poor outgrowth in explants treated with MMC.
In vivo	SB-505124 (5 mg/kg; i.p.) does not elicit any response when administered alone to C57Bl6 mice bearing A549 xenografts. However, when combined with a single dose of Carboplatin (60 mg/kg), SB-505124 induces sustained therapeutic effects in five subjects, eliminating the necessity for ongoing maintenance therapy. This synergy between SB-505124 and Carboplatin presents a potent treatment strategy without the requirement for continuous intervention in the specified animal model, highlighting its potential efficacy in a therapeutic context.

Molecular Weight	371.87
Formula	C20H22ClN3O2
CAS No.	356559-13-2

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

SB-505124 hydrochloride 356559-13-2 SB 505124 hydrochloride SB-505124 Hydrochloride SB 505124 Hydrochloride SB505124 Hydrochloride SB505124 hydrochloride inhibitor inhibit

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