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] sup >.
For research use only. We do not sell to patients.
- CAS No.: 2927489-99-2
- Formula: C25H31ClN2O4
- Molecular Weight:458.98
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
MAO-A 4.58 μM (IC50) |
HSP90 0.016 μM (IC50) |
|
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] |
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.
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Cell Line:GL26, U251R cells
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Concentration:0.1, 0.3, 1, 3 μM
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Incubation Time:24 h
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Result:Decreased HER2 and phospho-Akt expression and increased the expression of HSP70 in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:GL26 orthotopic xenograft tumor models[1]
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Dosage:25mg/kg
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Administration:Intraperitoneal injection (i.p.)
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Result:Reduced tumor growth inhibition (TGI%) by 59.8% compared to the control group.
Chemical Information
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CAS No. 2927489-99-2
-
Molecular Weight 458.98
-
Formula C25H31ClN2O4
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[2]. Hui-Ju Tseng, et al. Design, synthesis, and biological activity of dual monoamine oxidase A and heat shock protein 90 inhibitors, N-Methylpropargylamine-conjugated 4-isopropylresorcinol for glioblastoma. European Journal of Medicinal Chemistry. Volume 256, 5 August 2023, 115459. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)