2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. Glutathione S-transferase Interleukin Related
  4. GSTO1-IN-3

GSTO1-IN-3 是一种强效的 GSTO1-1 抑制剂，IC50 值为 0.11 μM，且对 GSTO2-2、GSTA1-1 和 GSTP1-1 具有选择性 (IC50 > 100 μM)。GSTO1-IN-3 可增强 Cisplatin (HY-17394) 对人乳腺癌细胞的细胞毒性。GSTO1-IN-3 可抑制小鼠骨髓来源巨噬细胞 (BMDM) 中 IL-1β 的释放。GSTO1-IN-3 可减轻小鼠体内的炎症反应。GSTO1-IN-3 可用于乳腺癌和炎症的相关研究。

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GSTO1-IN-3

GSTO1-IN-3 Chemical Structure

CAS No. : 158890-32-5

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GSTO1-IN-3 相关抗体

Top Publications Citing Use of Products

查看 Interleukin Related 亚型特异性产品:

查看所有亚型
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSTO1-IN-3 is a potent GSTO1-1 inhibitor with an IC50 of 0.11 μM, and shows selectivity over GSTO2-2, GSTA1-1 and GSTP1-1 (IC50 > 100 μM). GSTO1-IN-3 enhances the cytotoxicity of Cisplatin (HY-17394) against human breast cancer cells. GSTO1-IN-3 inhibits IL-1β release in mouse bone marrow-derived macrophage (BMDM) cells. GSTO1-IN-3 attenuates inflammation in mice. GSTO1-IN-3 can be used for breast cancer and inflammation research[1].

IC50 & Target[1]

GSTO1-1

0.11 μM (IC50)

体外研究
(In Vitro)

GSTO1-IN-3 (compound 5C-1) 表现出良好的体外安全性，在 ALARM NMR 实验中未检测到硫醇反应性，在 Ames 试验中对在浓度高达 2 mg/mL 时对鼠伤寒沙门氏菌 TA98 和 TA100 菌株无致突变性，并且在人肝微粒体中的稳定性比在小鼠体系中更高[1]。
GSTO1-IN-3 与 GSTO1-1 的 Cys32 形成共价键，其抑制效率常数 kᵢₙₐcₜ/Kᵢ 为 3.4 × 104 M-1s-1[1]。
GSTO1-IN-3 (5 μM) 可抑制小鼠骨髓来源巨噬细胞 (BMDM) 中 IL-1β 的释放，抑制率为 59.2%[1]。
GSTO1-IN-3 (5-50 μM，24 小时) 与 Cisplatin 具有协同作用，能以浓度依赖的方式显著增强对人乳腺癌 MDA-MB-231 细胞的细胞毒性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

GSTO1-IN-3 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 5, 10, and 50 μM
Incubation Time: 24 h
Result: Showed no particularly cytotoxicity at 5 μM (5.8%) in MDA-MB-231 cells.
Showed a low level of cytotoxicity at 10 μM (13.0%) and a significantly higher level of cytotoxicity (83.2%) at a concentration of 50 μM.
Acted synergistically to significantly raise the cytotoxicity of 20 μM Cisplatin to 55.1%.
Increased the cytotoxicity of Cisplatin to 73.6% at 10 μM.
Achieved a cytotoxicity level of 83.3% at 50 μM when combined with Cisplatin, which was not significantly different from its effect when administered alone.
体内研究
(In Vivo)

GSTO1-IN-3 (30 mg/kg，腹腔注射，LPS 注射前 30 分钟单次给药) 可减轻脂多糖 (LPS) (HY-D1056) 在小鼠中引起的炎症[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female C57BL/6 mice (8 weeks old) intraperitoneally injected with LPS[1]
Dosage: 30 mg/kg
Administration: i.p., single dose 30 min pre-LPS
Result: Significantly attenuated the LPS-induced reduction in body temperature at 6 h compared to the LPS-only control.
Showed significant protection against the inflammatory effects of LPS on mice at 4 h.
Significantly suppressed the release of IL-1β up to 4 h, but this suppression was not sustained at 6 h, likely due to the short in vivo half-life of the inhibitors.
分子量

251.75

Formula

C14H18ClNO
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

GSTO1-IN-3 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSTO1-IN-3158890-32-5Glutathione S-transferaseInterleukin RelatedGlutathione transferasesGSTsILGSTO1-1MDA-MB-231IL-1βBMDMbreast cancerinflammationInhibitorinhibitorinhibit

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