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SB-505124

CAS No. : 694433-59-5

MCE 国际站：SB-505124

产品活性：SB-505124 是一种选择性的 TGF-βI 型受体 (ALK4，ALK5，ALK7) 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。

研究领域：TGF-beta/Smad

作用靶点：TGF-β Receptor

In Vitro: SB-505124 demonstrates no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. 505124 inhibits the closely related ALK4 with an IC₅₀ 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. SB-505124 (10 µM) impairs Smad2 phosphorylation and CTGF and α-SMA expression in vitro. 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.

In Vivo: SB-505124 (5 mg/kg; i.p.) alone has no effect in C57Bl6 mice with A549 xenografts, but administration of SB-505124 with a single dose of Carboplatin (60 mg/kg) results in durable responses without the need for maintenance therapy in five animals.

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