1. Neuronal Signaling Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  2. Monoamine Oxidase HSP
  3. MAO A/HSP90-IN-2

MAO A/HSP90-IN-2 (compound 4-C) 是 HSP90 和 MAO A 双抑制剂,其 IC50 值分别为 0.016 和 4.58 μM。MAO A/HSP90-IN-2 上调 HSP70 表达,下调 HER2 和磷酸化 AKT 表达,以及 GL26 细胞中 IFN-γ 诱导的 PD-L1 的上升。MAO A/HSP90-IN-2 可以抑制 Temozolomide (HY-17364) 敏感和耐药的 GBM 细胞胶质瘤、结肠癌、白血病和非小细胞肺癌等癌症的生长,具有抑制肿瘤免疫逃逸的潜力。

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MAO A/HSP90-IN-2 Chemical Structure

MAO A/HSP90-IN-2 Chemical Structure

CAS No. : 2927489-99-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MAO A/HSP90-IN-2 (compound 4-C) is a dual inhibitor of HSP90and MAO A with the IC50 values of 0.016 and 4.58 μM, respectively. MAO A/HSP90-IN-2 increases HSP70 expression and reduces HER2 and phospho-Akt expression, and decreases IFN-γ induced PD-L1 expression in GL26 cells. MAO A/HSP90-IN-2 inhibits the growth of Temozolomide (HY-17364) -sensitive and -resistant GBM cells, colon cancer, leukemia, non-small cell lung and other cancers, and has potential to inhibit tumor immune escape[1].

IC50 & Target

MAO-A

4.58 μM (IC50)

HSP90

0.016 μM (IC50)

体外研究
(In Vitro)

MAO A/HSP90-IN-2 抑制小鼠和人的胶质瘤细胞以及结肠癌、白血病和非小细胞肺癌细胞的生长 (GL26、U251S、U251R、U87MG、U373MG 和 LN229, IC50 值分别为 0.49、1.09、0.26、0.36、0.89 和 0.31 μM) [1]
MAO A/HSP90-IN-2(compound 4-C)(0.3~3 μM, 24 h) 上调 GL26 和 U251R 细胞中 HSP70 的表达,下调 HER2、磷酸化 AKT 表达[1]
MAO A/HSP90-IN-2 (0.5 - 1 μM, 24 h) 抑制 GL26 细胞中 IFN-γ 诱导的 PD-L1 的上升[1]

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

Western Blot Analysis [1]

Cell Line: GL26, U251R cells
Concentration: 0.1, 0.3, 1, 3 μM
Incubation Time: 24 h
Result: Decreased HER2 and phospho-Akt expression and increased the expression of HSP70 in a dose-dependent manner.
体内研究
(In Vivo)

MAO A/HSP90-IN-2 (compound 4-C) (25mg/kg,腹腔注射,8天) 在 GL26 异种移植肿瘤模型中抑制肿瘤的生长[1]

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

Animal Model: GL26 orthotopic xenograft tumor models[1]
Dosage: 25mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Reduced tumor growth inhibition (TGI%) by 59.8% compared to the control group.
分子量

458.98

Formula

C25H31ClN2O4

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
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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.

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产品名称:
MAO A/HSP90-IN-2
目录号:
HY-155580
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