Chemical Structure : CCG258747
CAS No.: 2615910-00-2
货号: PC-23973Not For Human Use, Lab Use Only.
CCG258747 is a potent selective GRK2 inhibitor with IC50 of 18 nM, 83-fold selectivity over GRK5.
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CCG258747 is a potent selective GRK2 inhibitor with IC50 of 18 nM, 83-fold selectivity over GRK5.
CCG258747 is selective against GRK1 and PKA and shows little inhibition against ROCK1 at 10 µM.
CCG258747 demonstrated robust efficacy in blocking receptor internalization in HEK293 cells.
CCG258747 reduced MOR phosphorylation of Ser375 in pSer375-MOR for both HEK293 and U2OS stable cells.
分子量 | 502.55 | |
分子式 | C28H27FN4O4 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
Benzamide, 5-[(3S,4R)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-piperidinyl]-2-fluoro-N-(1H-indazol-3-ylmethyl)- |
1. Bouley RA, et al. Mol Pharmacol. 2020 Jun;97(6):392-401.
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