2. Metabolic Enzyme/Protease
  3. Glutathione S-transferase
  4. GSTO1-IN-4

GSTO1-IN-4 是一种选择性、强效的 GSTO1-1 抑制剂 (IC50 = 0.04 μM) (KI = 0.16 μM)。GSTO1-IN-4 对 GSTO2-2、GSTA1-1 和 GSTP1-1 的抑制作用较弱。GSTO1-IN-4 能够减轻小鼠炎症，并显著增强 Cisplatin (HY-17394) 的细胞毒性。GSTO1-IN-4 可用于炎症和乳腺癌的研究。

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GSTO1-IN-4

GSTO1-IN-4 Chemical Structure

CAS No. : 158890-33-6

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GSTO1-IN-4 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

生物活性

GSTO1-IN-4 is a selective, potent GSTO1-1 inhibitor (IC50 = 0.04 μM; KI = 0.16 μM). GSTO1-IN-4 shows low inhibition to GSTO2-2, GSTA1-1 and GSTP1-1. GSTO1-IN-4 shows a capacity to attenuate inflammation in mice and to significantly enhance the cytotoxicity of Cisplatin (HY-17394). GSTO1-IN-4 can be used for the study of inflammation and breast cancer[1].

体外研究
(In Vitro)

GSTO1-IN-4 (5 μM，2 小时) (Compound 10u) 能有效抑制 BMDM 细胞内 GSTO1-1 的活性，从而抑制 NLRP3 炎症小体的激活和 IL-1β 的释放[1]。
GSTO1-IN-4 (10 μM) 对 GSTO1-1 具有高度选择性，但对 GSTA1-1 和 GSTP1-1 的抑制水平较低[1]。
GSTO1-IN-4 (5-50 μM，24 小时) 在 5 μM (6.3 %) 和 10 μM (13.9 %) 浓度下对 MDA-MB 231 细胞的细胞毒性较低，但在 50 μM (74.3 %) 浓度下细胞毒性显著升高[1]。

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

GSTO1-IN-4 相关抗体:

ELISA Assay[1]

Cell Line: BMDMs stimulated with 200 ng/mL LPS for 3 h, then incubated in serum-free DMEM containing the test compound and incubated in DMEM containing 5 mM ATP for another 1 h.
Concentration: 5 μM
Incubation Time: 2 h
Result: Significantly reduced IL-1β release, decreasing the release level to 2.6 ± 0.5% (relative to untreated cells), with an inhibition rate of 97.4%.

Cell Cytotoxicity Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 5 μM, 10 μM, 50 μM
Incubation Time: 24 h
Result: Showed low cytotoxicity at 5 μM (6.3 %) and 10 μM (13.9 %), and a significantly higher cytotoxicity at 50 μM (74.3 %).
Significantly raise the cytotoxicity of 20 μM Cisplatin (42.2 %) to 68.8 %, 68.0 %, and 88.7 % at 5 μM, 10 μM, and 50 μM, respectively.
The cytotoxicity of 20 μM Cisplatin in combination with 50 μM test compound was also not significantly different from that of 50 μM test compound alone.
体内研究
(In Vivo)

GSTO1-IN-4 (50 mg/kg，腹腔注射，一次) 可以抵抗小鼠中 Lipopolysaccharides (LPS) (HY-D1056) 诱导的炎症作用[1]。

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

Animal Model: C57BL/6 female mice, 8 weeks of age[1].
Dosage: 50 mg/kg
Administration: I.p., injection 0.5 h before LPS administration
Result: Did not show a decrease in body temperature at 6 h and were not significantly different from normal control mice that were not treated with LPS.
Significantly suppressed the release of IL-1β up to 4 h, but after 6 h, the level of IL-1β had risen to levels that were not significantly different from the control wild-type mice treated with LPS.
分子量

279.80

Formula

C16H22ClNO
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

GSTO1-IN-4 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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-4158890-33-6Glutathione S-transferaseGlutathione transferasesGSTsGlutathione transferase Omega-1NLRP3 inflammasomeGSTO1-1 inhibitorCovalent inhibitorAnti-inflammationAnti-CancerInhibitorinhibitorinhibit

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