SB-505124

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Chemical Structure| 694433-59-5 同义名 : -
CAS号 : 694433-59-5
货号 : A114347
分子式 : C20H21N3O2
纯度 : 99%+
分子量 : 335.4
MDL号 : MFCD11045901
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 110 mg/mL(327.97 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 5%DMSO+40%PEG400+5% tween80+H2O 5 mg/mL clear

生物活性
靶点

  • TGFβRI/ALK5

    ALK5, IC50:47 nM

  • ALK4

    ALK4, IC50:129 nM
描述 Transforming growth factor (TGF) -β is a multifunctional cytokine that can inhibit endothelial and epithelial cellular proliferation, stimulate matrix accumulation, and suppress inflammation. Signaling by the TGF-β superfamily is mediated by two types of transmembrane receptor serine/threonine kinases, types I and II, ligand interaction with a homodimer of type II receptors recruits and activates homodimers of type I receptors or activin receptor-like kinases (ALKs)[3]. SB505124 is an inhibitor of TGFβ receptor ALK4 and ALK5 with IC50 of 47 nM and 129 nM, respectively[3]. FaO cells or NRP 154 cells were protected from TGF-β–induced apoptosis by SB-505124 (0.01-1µM) in a concentration-dependent manner[3]. Specific inhibition of the TGF-β type I receptor/ALK5 serine-threonine kinase with SB-505124 (500 nM) abolished the effects of TGF-β1 on F-actin assembly in HUVEC cells[4]. Treatment with 0.25 μM-SB505124 in Sh3bp2KI/KI bone marrow stromal cultures reduced RANKL (a critical regulator of osteoclast formation) expression almost back down to wild type levels[5].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
human HaCaT cells Function assay Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay, IC50=43.8 nM 24786585
mouse 4T1 cells Function assay Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay, IC50=76.6 nM 24786585
mouse NMuMG cells 0.1-0.5 μM Function assay 1 h Inhibition of ALK5 activity in mouse NMuMG cells assessed as TGFbeta-induced phosphorylation of Smad2 at 0.1 to 0.5 uM after 1 hr by Western blot analysis 23047226
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.98mL

0.60mL

0.30mL

14.91mL

2.98mL

1.49mL

29.82mL

5.96mL

2.98mL
参考文献

[1]Hu T, Ramachandrarao SP, et al. Reactive oxygen species production via NADPH oxidase mediates TGF-beta-induced cytoskeletal alterations in endothelial cells. Am J Physiol Renal Physiol. 2005 Oct;289(4):F816-25.

[2]DaCosta Byfield S, Major C, et al. SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7. Mol Pharmacol. 2004 Mar;65(3):744-52.

[3]DaCosta Byfield S, Major C, Laping NJ, Roberts AB. SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7. Mol Pharmacol. 2004 Mar;65(3):744-52. doi: 10.1124/mol.65.3.744. PMID: 14978253.

[4]Hu T, Ramachandrarao SP, Siva S, Valancius C, Zhu Y, Mahadev K, Toh I, Goldstein BJ, Woolkalis M, Sharma K. Reactive oxygen species production via NADPH oxidase mediates TGF-beta-induced cytoskeletal alterations in endothelial cells. Am J Physiol Renal Physiol. 2005 Oct;289(4):F816-25. doi: 10.1152/ajprenal.00024.2005. PMID: 16159901; PMCID: PMC1460011.

[5]Liu Y, Sharma T, Chen IP, Reichenberger E, Ueki Y, Arif Y, Parisi D, Maye P. Rescue of a cherubism bone marrow stromal culture phenotype by reducing TGFβ signaling. Bone. 2018 Jun;111:28-35. doi: 10.1016/j.bone.2018.03.009. Epub 2018 Mar 9. PMID: 29530719; PMCID: PMC5924722.