CCG-63802 是一种选择性、可逆和变构的 RGS4 抑制剂。
| Cas No. |
620112-78-9 |
| 别名 |
ALPHA-[[9-甲基-2-(3-甲基苯氧基)-4-氧代-4H-吡啶并[1,2-A]嘧啶-3-基]亚甲基]-2-苯并噻唑乙腈,CCG 63802;CCG63802 |
| 化学名 |
(E)-2-(1,3-benzothiazol-2-yl)-3-[9-methyl-2-(3-methylphenoxy)-4-oxopyrido[1,2-a]pyrimidin-3-yl]prop-2-enenitrile |
| Canonical SMILES |
CC1=CC(=CC=C1)OC2=C(C(=O)N3C=CC=C(C3=N2)C)C=C(C#N)C4=NC5=CC=CC=C5S4 |
| 分子式 |
C26H18N4O2S |
| 分子量 |
450.52 |
| 溶解度 |
Limited solubility, 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 |
| 半岛bd体育手机客户端 描述 |
CCG-63802 is a selective inhibitor of RGS4 with IC50 value of 1.9 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 [1, 2].
CCG-63802 is a potent RGS 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-63802 treatment inhibited GAP activity of RGS4 [1]. When tested with HEK-293 cells, administration of CCG-63802 successfully reversed 8-Br-cGMP inhibition on BK via inhibiting RGS4 [2].
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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