2. Metabolic Enzyme/Protease
  3. Aminopeptidase
  4. GSK235

GSK235 是一种口服有效的选择性变构内质网氨肽酶1 (ERAP1) 抑制剂，对人源和鼠源 ERAP1 的 pIC50 值分别为 8.45 和 7.59。GSK235 对两种同源性最高的酶 ERAP2 和 IRAP 的选择性超过 1000 倍。GSK235 可以调节癌细胞的免疫肽组，并增强癌细胞的抗原性。GSK235 可用于结直肠癌和关节炎的研究。

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GSK235

GSK235 Chemical Structure

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GSK235 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSK235 is an orally active, selective and allosteric endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor with pIC50 values of 8.45 and 7.59 for human and mouse ERAP1, respectively. GSK235 exhibits over 1000-fold selectivity for the two most homologous enzymes, ERAP2 and IRAP. GSK235 can regulate the immunopeptidome of cancer cells and enhance cancer cell antigenicity. GSK235 can be used for the study of colorectal cancer and arthritis[1].

体外研究
(In Vitro)

GSK235 (compound 21) (1 μM，0.61 μM；1 小时，24 小时) 在人和小鼠酶中对 ERAP1 和 ERAAP 具有强效抑制作用，并具有高选择性[1]。
GSK235 在 HeLa 抗原呈递试验中显示 pIC50 值为 7.25[1]。
GSK235 (1 µM；30 天) 对 CT26 肿瘤细胞中多种免疫肽产生影响。观察到肽链长度显著增加；例如，10 肽和 11 肽的显著增加伴随着 9 肽和 8 肽的减少[1]。
GSK235 对 hERG 通道无活性[1]。

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

GSK235 相关抗体:
体内研究
(In Vivo)

GSK235 (compound 21) (30, 90, 270 mg/kg，口服，每日两次，共 17 天) 在 CT26 同源小鼠模型中，以剂量依赖性方式降低肿瘤生长并调节免疫肽组[1]。
GSK235 (30, 90, 270 mg/kg，口服，每日两次； 从第 18 天到第 36 天) 以剂量依赖性方式降低胶原诱导性关节炎 (CIA) 小鼠模型中的关节炎评分和免疫激活，且无自身免疫加重的证据[1]。

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

Animal Model: Female BALB/c (6-8 weeks old) were inoculated subcutaneously in the right hind flank with 5x104 CT26 cells[1]
Dosage: 30 mg/kg, 90 mg/kg, 270 mg/kg
Administration: Oral; twice daily (BID); for 17 days
Result: Observed with significant reduction in tumor volume by termination of the study, day 17, at the highest dose (270 mg/kg) and no significant dose-dependent body-weightchanges were observed.
Animal Model: Male DBA/1OlaHsd (6-7 weeks old) (Collagen-induced arthritis (CIA) model)[1]
Dosage: 30 mg/kg, 90 mg/kg, 270 mg/kg
Administration: Oral; twice daily (BID); from day 18 to day 36
Result: Showed a dose-dependent reduction in arthritis scores, with the highest dose (270 mg/kg) achieving a reduction comparable to the TNF inhibitor Enbrel.
Also reduced anti-collagen type II IgG levels, IL-12p40, and IL-6 levels, and decreased MHC-I expression on B cells and cDCs.
No exacerbation of autoimmune responses was observed.
分子量

386.49

Formula

C21H30N4O3
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

GSK235 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:

GSK235GSK 235GSK-235AminopeptidaseERAP1orally activecolorectal cancerarthritisimmunopeptidomeInhibitorinhibitorinhibit

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