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SB-505124 hydrochloride
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SB-505124 hydrochloride
CAS No. : 356559-13-2
MCE 站:SB-505124 hydrochloride
产品活性:SB-505124 hydrochloride 是一种选择性的?TGF-β Receptor type I receptor (ALK4,ALK5,ALK7) 抑制剂,对 LK4,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 ?M) 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.
相关产品:SB-431542 | Dorsomorphin | A 83-01 | LDN193189 | RepSox | SB 525334 | DMH-1 | SB-505124 | BMP signaling agonist sb4 | GW788388 | ITD-1 | LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA) | SD-208 | LDN-212854 | K02288 | LDN-214117 | R-268712 | SM 16 | A 77-01 | ALK2-IN-2 | PD-161570 | pm26TGF-β1 peptide TFA | Isosaponarin | BIO-013077-01
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