SB-505124 hydrochloride 是TGF-βI型受体(ALK4，ALK5，ALK7) 的选择性抑制剂，对 ALK4，ALK5 的IC50值分别为 129 nM 和 47 nM，对 ALK1，2，3 或 6 无作用。

SB-505124 hydrochloride is a selective and concentration-dependent inhibitor of TGF-β Receptor type I receptor ( ALK4, ALK5, ALK7 ), with IC 50 s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.

SB-505124 shows no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. 505124 inhibits the closely related ALK4 with an IC 50 value of 129±11 nM (about 2.5-fold less sensitive than ALK5) but does not inhibit ALK2 at concentrations up to 10 μM. SB-505124 (1 μM) inhibits the TGF-β-induced phosphorylation of Smad2 in all three of these cell lines in a concentration-dependent fashion. SB-505124 (1 or 5 μM) potently inhibits TGF-β-induced activation of JNK/SAP, extracellular signal-regulated kinase 1/2, and p38 despite the different patterns of activation in these cells [1]. SB-505124 (10 μM) impairs Smad2 phosphorylation and CTGF and α-SMA expression in vitro [2]. SB-505124 susspresses CTGF and α-SMA observed by immunofluorescence. Cell outgrowth from explants dissected from eyes to which SB-505124 is applied during GFS is robust while outgrowth is poor from those treated with MMC [3].

SB-505124 (5 mg/kg; i.p.) alone has no effect in C57Bl6 mice with A549 xenografts, but SB-505124 administered with a single dose of Carboplatin (60 mg/kg) causes durable responses without the need for maintenance therapy in five animals [4]. Animal Model: C57Bl6 mice with A549 xenografts [4] Dosage: 5 mg/kg Administration: I.p.; daily Result: Had no effect alone, but administration with a single dose of carboplatin (60 mg/kg) resulted in durable responses without the need for maintenance therapy in five animals.

356559-13-2

C20H22ClN3O2

371.86

SB-505124 hydrochloride

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years