GYS32661 | RAC1 inhibitor | Probechem Biochemicals

Chemical Structure : GYS32661

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GYS32661 (GYS 32661)

货号: PC-20183Not For Human Use, Lab Use Only.

GYS32661 (GYS 32661) is a potent Rac inhibitor capable of inhibiting both Rac1 and Rac1b, inhibited activated Rac1 with IC50 of 1.18 uM in in vitro pull-down assays.

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生物&药学活性

GYS32661 (GYS 32661) is a potent Rac inhibitor capable of inhibiting both Rac1 and Rac1b, inhibited activated Rac1 with IC50 of 1.18 uM in in vitro pull-down assays.
GYS32661 showed significant inhibition of Rac1 and Rac1b activity at 5 μmol/L in HCT116 colorectal cancer cells.
GYS32661 (10 uM) significantly blocked Rac1b-mediated NF-κB activity, attenuated TNFα-stimulated NF-κB activity.
GYS32661 attenuated phosphorylation of both IKBα and RelA/p65, inhibited downstream activation of NF-κB signaling in colorectal cancer. GYS32661sensitized colorectal cancer cells to chemotherapy (Oxaliplatin).
GYS32661 was shown to have higher activity against both recombinant Rac1 and recombinant Rac1b than EHT1864.
GYS32661 reduced the growth rates in xenograft models of human CRC in mice.

物理化学性质&存储条件

分子量	464.55
分子式	C23H27F3N4OS
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	4-((1-(5-((7-(trifluoromethyl)quinolin-4-yl)thio)pentyl)-1H-imidazol-4-yl)methyl)morpholine

参考文献

1. Erik T Goka, et al. Mol Cancer Ther. 2019 May;18(5):957-968.

GYS32661 (GYS 32661)

生物&药学活性

物理化学性质&存储条件

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GYS32661 (GYS 32661)

生物&药学活性

物理化学性质&存储条件

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