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Chemical Structure : GSK1120360A
Catalog No.: PC-49790Not For Human Use, Lab Use Only.
GSK1120360A (GSK360A) is a potent, specific and orally active inhibitor of HIF PHD enzyme with pIC50 of 8.0/7.0/6.9 for PHD1/2/3, respectively.
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GSK1120360A (GSK360A) is a potent, specific and orally active inhibitor of HIF PHD enzyme with pIC50 of 8.0/7.0/6.9 for PHD1/2/3, respectively.
GSK360A acts by competing with the a-ketoglurtarate site and has little or no activity on inhibiting HIF-1 asparaginyl hydroxylase (FIH-1) or collagen 4-prolyl hydroxylase (pIC50 =5.0 and 5.7, respectively).
GSK360A increased secreted EPO protein level by 50% at 3 uM and vascular endothelial growth factor protein level by 50% at 1 uM, respectively, in Hep3B cells.
GSK360A exerts systemic and local effects by stabilizing HIF-1 alpha signaling and improves long-term ventricular function, remodeling, and vascularity in a model of established ventricular dysfunction.
GSK360A enhances rotator cuff regeneration following a chronic tear.
| M.Wt | 348.33 | |
| Formula | C17H17FN2O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Weike Bao, et al. J Cardiovasc Pharmacol. 2010 Aug;56(2):147-55.
2. J P Gumucio, et al. Bone Joint Res. 2017 Jan;6(1):57-65.
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