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  3. MAO A/HSP90-IN-2

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].

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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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Description

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)

In Vitro

MAO A/HSP90-IN-2 (compound 4-C) inhibits the growth of mouse and human GBM, colon cancer, leukemia, non-small cell lung and other cancers (GL26, U251S, U251R, U87MG, U373MG and LN229 cells with the IC50 values of 0.49, 1.09 0.26, 0.36, 0.89 and 0.31 μM) [1].
MAO A/HSP90-IN-2 (0.3 - 3 μM, 24h) increases the expression of HSP70,and decreases HER2 and phospho-Akt expression in GL26 and U251R cell lines [1].
MAO A/HSP90-IN-2(0.5 - 1 μM, 24 h) inhibits IFN-γ induced PD-L1 expression concentration-dependently in GL26 cells [1].

MedChemExpress (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.
In Vivo

MAO A/HSP90-IN-2(compound 4-C) (25 mg/kg for i.p., eight days) reduces tumor growth in GL26 orthotopic xenograft tumor models[1].

MedChemExpress (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.
Molecular Weight

458.98

Formula

C25H31ClN2O4

CAS No.
SMILES

O=C(C1=C(C=C(C(C(C)C)=C1)O)O)N(C2=CC(Cl)=C(C=C2)OCCCN(CC#C)C)CC

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    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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MAO A/HSP90-IN-2
Cat. No.:
HY-155580
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