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.
CCG-63808
目录号: GC14412纯度: >98%同义词: 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
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
| 规格 | 价格 | 库存 | 数量 | 操作 |
|---|---|---|---|---|
| 5mg | ¥720.00 | 现货 | 1 | |
| 10mg | ¥1,080.00 | 现货 | 1 | |
| 25mg | ¥1,620.00 | 现货 | 1 | |
| 50mg | ¥2,302.00 | 现货 | 1 | |
| 100mg | ¥3,240.00 | 现货 | 1 |
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产品描述 Description
产品文档 Product Documents
Purity:>98%
化学性质Chemical Properties
CAS 号
620113-73-7
同义词
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
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 g/mol
溶解性
Soluble in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。
计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度
g/mol