CCG-63808 是 G 蛋白信号 (RGS) 蛋白调节剂的可逆抑制剂。
| Cas No. | 620113-73-7 |
| 别名 | ALPHA-[[2-(4-氟苯氧基)-9-甲基-4-氧代-4H-吡啶并[1,2-A]嘧啶-3-基]亚甲基]-2-苯并噻唑乙腈,CCG63808;CCG 63808 |
| 化学名 | (E)-2-(1,3-benzothiazol-2-yl)-3-[2-(4-fluorophenoxy)-9-methyl-4-oxopyrido[1,2-a]pyrimidin-3-yl]prop-2-enenitrile |
| Canonical SMILES | CC1=CC=CN2C1=NC(=C(C2=O)C=C(C#N)C3=NC4=CC=CC=C4S3)OC5=CC=C(C=C5)F |
| 分子式 | C25H15FN4O2S |
| 分子量 | 454.49 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | CCG-63808 is a selective inhibitor of RGS4 with IC50 value of 1.4 μM [1].
RGS (regulators of G protein signaling) are multi-functional, GTPase-accelerating proteins and plays an important role in promoting GTP hydrolysis via heterotrimeric G proteins α subunit. RGS 4 is also known as RGP4 and plays a pivotal role in negatively regulating signaling upstream or at the level of the heterotrimeric G protein [2].
CCG-63808 is a potent RGS4 inhibitor and is different from the reported RGS4 irreversibly inhibitor CCG-4986. Using the [32P] GTP single-turnover GAP assay, it was shown that CCG-63808 treatment inhibited GAP activity of RGS4 and the inhibition could be reversed by washing [1].
References:
[1].Blazer, L.L., et al., Reversible, allosteric small-molecule inhibitors of regulator of G protein signaling proteins. Mol Pharmacol, 2010. 78(3): p. 524-33.
[2].Dobrivojevic, M., et al., Interaction between bradykinin and natriuretic peptides via RGS protein activation in HEK-293 cells. Am J Physiol Cell Physiol, 2012. 303(12): p. C1260-8. |
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