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CCG-63802
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CCG-63802图片
CAS NO:620112-78-9
规格:98%
分子量:450.52
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
RGS protein inhibitor
CAS:620112-78-9
分子式:C26H18N4O2S
分子量:450.52
纯度:98%
存储:Store at -20°C

Background:

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].
参考文献:
[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.