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GSTO1-IN-1

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Chemical Structure| 568544-03-6 同义名 : -
CAS号 : 568544-03-6
货号 : A420085
分子式 : C10H12Cl2N2O3S
纯度 : 97%
分子量 : 311.185
MDL号 : MFCD03965279
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 300 mg/mL(964.06 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Glutathione S-transferases are a family of enzymes primarily involved in phase II metabolism. Glutathione S-transferase omega 1 (GSTO1) is an atypical GST isoform that catalyzes S-phenacyl glutathione reduction and monomethylarsonate (V) reduction. GSTO1-IN-1 is a potent GSTO1 inhibitor that inhibits the enzyme activity of GSTO1 with an IC50 value of 31nM. GSTO1-IN-1 potently competed with CMFDA for binding to endogenous and recombinant GSTO1 in HCT116 soluble proteome. Treatment with GSTO1-IN-1 at 0.12-10µM inhibited the colony formation of HCT116 cells. The incubation of HCT116 cells with 5µM GSTO1-IN-1 for 24 h led to a decrease in the G0/G1 population and a concomitant increase in the S-phase population. Administration of GSTO1-IN-1 at 20-45mg/kg/day for 5 weeks significantly inhibited tumor growth in nude mice bearing HCT116 xenografts as compared to the vehicle-treated group. In the KRAS-mutant CRM-13-180 PDX model, GSTO1-IN-1 treatment (50mg/kg) resulted in a modest inhibition of tumor growth with a percent treated/control (%T/C) of 67[1].
作用机制 GSTO1-IN-1 is a potent, covalent GSTO1 inhibitor that binds to GSTO1-IN-1 through both hydrophobic and hydrophilic interactions[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.21mL

0.64mL

0.32mL

16.07mL

3.21mL

1.61mL

32.13mL

6.43mL

3.21mL
参考文献

[1]Ramkumar K, Samanta S, Kyani A, et al. Mechanistic evaluation and transcriptional signature of a glutathione S-transferase omega 1 inhibitor. Nat Commun. 2016;7:13084.