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CAS No.: 568544-03-6

GSTO1-IN-1 Catalog No. CSN21143

Synonyms: GSTO1-1 inhibitor C1-27

GSTO1-IN-1 is a potent glutathione S-transferase omega 1 (GSTO1) inhibitor with an IC50 of 31 nM

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技术信息

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].
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.2135 mL
- 16.0674 mL
- 32.1347 mL
- 5 mM
- 0.6427 mL
- 3.2135 mL
- 6.4269 mL
- 10 mM
- 0.3213 mL
- 1.6067 mL
- 3.2135 mL

技术信息

CAS号

568544-03-6

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C10H12Cl2N2O3S

运输

蓝冰

分子量

311.18

别名

GSTO1-1 inhibitor C1-27

溶解度

DMSO	300.0 mg/mL (964.1 mM)

动物实验配方

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