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

MAO A/HSP90-IN-1 (4-b) 是一种 MAO A/HSP90 双抑制剂,在恶性胶质瘤 GL26 细胞中的 IC50 值为1.77 μM,对 HSP90α 的IC50 值为0.019 μM。MAO A/HSP90-IN-1 (4-b) 通过抑制 MAO A 的活性,HSP90 的结合以及 HER2 和 phospho-Akt 的表达来抑制恶性胶质瘤 (GMB),它们还能减少抑制 T 细胞活化的 PD-L1 表达,具有抑制肿瘤免疫逃逸的潜力。可用于脑肿瘤相关疾病的研究。

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MAO A/HSP90-IN-1 Chemical Structure

MAO A/HSP90-IN-1 Chemical Structure

CAS No. : 2927489-95-8

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  • 生物活性

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  • 参考文献

生物活性

MAO A/HSP90-IN-1 (4-b) is a MAO A/HSP90 dual inhibitor with IC50 value of 1.77 μM and 0.019 μM in Glioblastoma (GBM) GL26 cells and HSP90α, respectively. MAO A/HSP90-IN-1 (4-b) can inhibit MAO A activity, HSP90 binding and the expression of HER2 and phospho-Akt to inhibit the growth of GBM, they also reduce PD-L1 expression, which inhibits T cell activation. MAO A/HSP90-IN-1 (4-b) have potential to inhibit tumor immune escape. MAO A/HSP90-IN-1 (4-b) can be used for brain tumor-related diseases research[1].

IC50 & Target[1]

HSP90

0.019 μM (IC50)

MAO-A

1.77 μM (IC50)

体外研究
(In Vitro)

MAO A/HSP90-IN-1 (4-b) (0.1 μM-3 μM, 24小时) 通过抑制 MAO A 和 HSP90,从而减少 GBM 细胞的增殖[1]
MAO A/HSP90-IN-1 (0.1 μM-3 μM, 24小时) 在 GL26 中的 IC50 为0.73 μM,在GL26中的 IC50 为1.68 μM,在 U251R 中的 IC50 为0.84 μM[1]
MAO A/HSP90-IN-1 (0μM, 0.35μM, 0.7μM, 1.4μM, 24小时) 在小鼠胶质瘤 GL26 细胞中抑制IFN-γ 诱导的PD-L1表达[1]

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

Cell Viability Assay[1]

Cell Line: U87MG, U373MG, LN229, A172, T98G, P1S, P3, and P3R human GBM cells
Concentration: 50 μM
Incubation Time: 72 h
Result: Inhibited cell growth in GBM cell lines with an IC50 ratio was around 1 except A172 cell.

Western Blot Analysis[1]

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

MAO A/HSP90-IN-1 (4-b) (25 mg/kg,腹腔注射,每天) 抑制 GBM 小鼠模型肿瘤生长[1]

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

Animal Model: GL26 GBM mouse model[1]
Dosage: 25 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Decreased tumor growth inhibition (TGI%) was 63.2% compared to vehicle group.
分子量

444.95

Formula

C24H29ClN2O4

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-1
目录号:
HY-155577
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