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Cat. No.: HY-155577

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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.

For research use only. We do not sell to patients.

CAS No.: 2927489-95-8
Formula: C₂₄H₂₉ClN₂O₄
Molecular Weight:444.95

Storage:

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

Data Sheet (270 KB)

MAO A/HSP90-IN-1 Chemical Structure

CAS No.: 2927489-95-8

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

HSP90

0.019 μM (IC₅₀)

MAO-A

1.77 μM (IC₅₀)

All Monoamine Oxidase Isoforms :

MAO-A
MAO-B

All HSP Isoforms :

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.

Chemical Information

CAS No. 2927489-95-8
Molecular Weight 444.95
Formula C₂₄H₂₉ClN₂O₄
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
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Tseng HJ, 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. Eur J Med Chem. 2023 Aug 5;256:115459. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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MAO A/HSP90-IN-1

All Monoamine Oxidase Isoforms

All HSP Isoforms