2. Neuronal Signaling Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. Monoamine Oxidase HSP
  4. 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

MAO A/HSP90-IN-2 Chemical Structure

CAS No. : 2927489-99-2

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MAO A/HSP90-IN-2 Related Antibodies

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

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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)

Cellular Effect
Cell Line Type Value Description References
A 172 IC50
0.89 μM
Compound: 4-c
Antiproliferative activity against human A-172 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 method
Antiproliferative activity against human A-172 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 method
[PMID: 37172473]
A549 GI50
0.14 μM
Compound: 4-c
Growth inhibition of human A549 cells incubated for 48 hrs by SRB assay
Growth inhibition of human A549 cells incubated for 48 hrs by SRB assay
[PMID: 37172473]
HCT-116 GI50
0.08 μM
Compound: 4-c
Growth inhibition of human HCT-116 cells incubated for 48 hrs by SRB assay
Growth inhibition of human HCT-116 cells incubated for 48 hrs by SRB assay
[PMID: 37172473]
HL-60 GI50
0.06 μM
Compound: 4-c
Growth inhibition of human HL-60 cells incubated for 48 hrs by SRB assay
Growth inhibition of human HL-60 cells incubated for 48 hrs by SRB assay
[PMID: 37172473]
K562 GI50
0.07 μM
Compound: 4-c
Growth inhibition of human K562 cells incubated for 48 hrs by SRB assay
Growth inhibition of human K562 cells incubated for 48 hrs by SRB assay
[PMID: 37172473]
KM12 GI50
0.06 μM
Compound: 4-c
Growth inhibition of human KM12 cells incubated for 48 hrs by SRB assay
Growth inhibition of human KM12 cells incubated for 48 hrs by SRB assay
[PMID: 37172473]
LN-229 IC50
0.31 μM
Compound: 4-c
Antiproliferative activity against human LN-229 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 method
Antiproliferative activity against human LN-229 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 method
[PMID: 37172473]
NCI-H460 GI50
0.05 μM
Compound: 4-c
Growth inhibition of human NCI-H460 cells incubated for 48 hrs by SRB assay
Growth inhibition of human NCI-H460 cells incubated for 48 hrs by SRB assay
[PMID: 37172473]
NCI-H522 GI50
0.07 μM
Compound: 4-c
Growth inhibition of human NCI-H522 cells incubated for 48 hrs by SRB assay
Growth inhibition of human NCI-H522 cells incubated for 48 hrs by SRB assay
[PMID: 37172473]
RPMI-8226 GI50
0.33 μM
Compound: 4-c
Growth inhibition of human RPMI-8226 cells incubated for 48 hrs by SRB assay
Growth inhibition of human RPMI-8226 cells incubated for 48 hrs by SRB assay
[PMID: 37172473]
SF-268 GI50
1.43 μM
Compound: 4-c
Growth inhibition of human SF-268 cells incubated for 48 hrs by SRB assay
Growth inhibition of human SF-268 cells incubated for 48 hrs by SRB assay
[PMID: 37172473]
SF-295 GI50
0.32 μM
Compound: 4-c
Growth inhibition of human SF-295 cells incubated for 48 hrs by SRB assay
Growth inhibition of human SF-295 cells incubated for 48 hrs by SRB assay
[PMID: 37172473]
SF-539 GI50
0.31 μM
Compound: 4-c
Growth inhibition of human SF-539 cells incubated for 48 hrs by SRB assay
Growth inhibition of human SF-539 cells incubated for 48 hrs by SRB assay
[PMID: 37172473]
SNB-19 GI50
0.44 μM
Compound: 4-c
Growth inhibition of human SNB-19 cells incubated for 48 hrs by SRB assay
Growth inhibition of human SNB-19 cells incubated for 48 hrs by SRB assay
[PMID: 37172473]
SNB-75 GI50
0.86 μM
Compound: 4-c
Growth inhibition of human SNB-75 cells incubated for 48 hrs by SRB assay
Growth inhibition of human SNB-75 cells incubated for 48 hrs by SRB assay
[PMID: 37172473]
SW-620 GI50
0.24 μM
Compound: 4-c
Growth inhibition of human SW-620 cells incubated for 48 hrs by SRB assay
Growth inhibition of human SW-620 cells incubated for 48 hrs by SRB assay
[PMID: 37172473]
T98G IC50
0.46 μM
Compound: 4-c
Antiproliferative activity against human T98G cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 method
Antiproliferative activity against human T98G cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 method
[PMID: 37172473]
U-251 GI50
0.37 μM
Compound: 4-c
Growth inhibition of human U-251 cells incubated for 48 hrs by SRB assay
Growth inhibition of human U-251 cells incubated for 48 hrs by SRB assay
[PMID: 37172473]
U-251 IC50
0.26 μM
Compound: 4-c
Antiproliferative activity against human Temozolomide-resistant U-251 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
Antiproliferative activity against human Temozolomide-resistant U-251 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
[PMID: 37172473]
U-251 IC50
1.09 μM
Compound: 4-c
Antiproliferative activity against human Temozolomide-sensitive U-251 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
Antiproliferative activity against human Temozolomide-sensitive U-251 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
[PMID: 37172473]
U-373MG ATCC IC50
0.89 μM
Compound: 4-c
Antiproliferative activity against human U373 MG cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 method
Antiproliferative activity against human U373 MG cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 method
[PMID: 37172473]
U-87MG ATCC IC50
0.36 μM
Compound: 4-c
Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 method
Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 method
[PMID: 37172473]
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.

MAO A/HSP90-IN-2 Related Antibodies

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MAO A/HSP90-IN-2 Related Classifications

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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:

MAO A/HSP90-IN-22927489-99-2Monoamine OxidaseHSPMAOHeat shock proteinsHSP70GL26U251RU87MGGlioblastomaPD-L1colon cancerleukemianon-small cell lung cancerInhibitorinhibitorinhibit

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