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) 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.

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MAO A/HSP90-IN-1

MAO A/HSP90-IN-1 Chemical Structure

CAS No. : 2927489-95-8

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Description

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)

Cellular Effect
Cell Line Type Value Description References
A 172 IC50
3.31 μM
Compound: 4-b
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
0.19 μM
Compound: 4-b
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-b
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
0.04 μM
Compound: 4-b
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-b
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
0.05 μM
Compound: 4-b
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
0.4 μM
Compound: 4-b
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
0.04 μM
Compound: 4-b
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
0.08 μM
Compound: 4-b
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
0.38 μM
Compound: 4-b
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
0.52 μM
Compound: 4-b
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
0.29 μM
Compound: 4-b
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
0.32 μM
Compound: 4-b
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-b
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
0.42 μM
Compound: 4-b
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
0.05 μM
Compound: 4-b
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-b
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
0.32 μM
Compound: 4-b
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
0.84 μM
Compound: 4-b
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
1.68 μM
Compound: 4-b
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
1.46 μM
Compound: 4-b
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
0.35 μM
Compound: 4-b
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-1 (4-b) (0.1 μM-3 μM, 24h) reduces the proliferation of GBM cells via inhibiting MAO A and HSP90[1].
MAO A/HSP90-IN-1 (0.1 μM-3 μM, 24h) shows IC50 0.73 μM in GL26, 1.68 μM in U251S, and 0.84 μM in U251R[1].
MAO A/HSP90-IN-1 (0μM, 0.35μM, 0.7μM, 1.4μM, 24h) inhibits IFN-γ induced PD-L1 expression concentration-dependently in GL26 mouse GBM cells [1].

MedChemExpress (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.
In Vivo

MAO A/HSP90-IN-1 (4-b) (25 mg/kg for intraperitoneal injection, once a day) shows significantly decreased tumor growth in GL26 GBM mouse model[1].

MedChemExpress (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.
Molecular Weight

444.95

Formula

C24H29ClN2O4

CAS No.
SMILES

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

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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MAO A/HSP90-IN-1
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