BIM-46174 | Heterotrimeric Gα/Gβγ inhibitor | Probechem Biochemicals

Chemical Structure : BIM-46174

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BIM-46174 (BIM46174)

货号: PC-23379Not For Human Use, Lab Use Only.

BIM-46174 is a selective inhibitor of heterotrimeric G-protein complex Gα/Gβγ subunits, abrogates cancer cell invasion controlled by several GPCR agonists.

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生物&药学活性

BIM-46174 is a selective inhibitor of heterotrimeric G-protein complex Gα/Gβγ subunits, abrogates cancer cell invasion controlled by several GPCR agonists.
BIM-46174 competitively inhibitscholera toxin–induced cAMP accumulation with a pA2 value of 5.3.
BIM-46174 only affects cAMP generation induced by cholera toxin via Gαs and not by forskolin directly acting on adenylyl cyclase. BIM46174 has no effect on cancer cell invasion induced by individual subunits of heterotrimeric G-protein complex: Gα12, Gα13, or Gβ1γ2 dimer.
BIM46174 inhibits the growth of a large panel of human cancer cell lines, including anticancer drug-resistant cells.
BIM-46174 combined with either cisplatin, farnesyltransferase inhibitor, or topoisomerase inhibitors, significantly reduced the growth rate of human tumor xenografts in athymic mice.

物理化学性质&存储条件

分子量	398.57
分子式	C22H30N4OS
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(R)-2-amino-1-((S)-8-(cyclohexylmethyl)-2-phenyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl)-3-mercaptopropan-1-one

参考文献

1. Prévost GP, et al. Cancer Res. 2006 Sep 15;66(18):9227-34.

BIM-46174 (BIM46174)

生物&药学活性

物理化学性质&存储条件

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BIM-46174 (BIM46174)

生物&药学活性

物理化学性质&存储条件

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