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Cat. No.: HY-148574

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MCT1-IN-3

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MCT1-IN-3 is a monocarboxylate transporter 1 (MCT1) inhibitor with an IC₅₀ value of 81.0 nM. MCT1-IN-3 has also significant inhibitivity against the multidrug transporter ABCB1. MCT1-IN-3 can be used for the research of cancer.

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Pureté: 98.65%
CAS No.: 2878360-80-4
Formule: C₂₂H₁₉N₃O₄
Masse moléculaire:389.40

Stockage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

MCT1-IN-3 Chemical Structure

CAS No.: 2878360-80-4

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

IC50: 81.0 nM (MCT1)^[1]
GI50: 20 μM (A-549); 15.1 μM (MCF-7)^[1]

Voir tous les produits spécifiques à Isoform Monocarboxylate Transporter :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780 ADR	EC₅₀	0.793 μM Compound: 24	Reversal of multi-drug resistance in human A2780 ADR cells expressing ABCB1 incubated for 72 hrs by MTT assay Reversal of multi-drug resistance in human A2780 ADR cells expressing ABCB1 incubated for 72 hrs by MTT assay	[PMID: 36584238]
A2780 ADR	GI₅₀	110 nM Compound: 24	Induction of doxorubicin sensitization in human A2780 ADR cells expressing ABCB1 assessed as doxorubicin at 3.5 uM incubated for 72 hrs by MTT assay Induction of doxorubicin sensitization in human A2780 ADR cells expressing ABCB1 assessed as doxorubicin at 3.5 uM incubated for 72 hrs by MTT assay	[PMID: 36584238]
A2780 ADR	GI₅₀	214 nM Compound: 24	Induction of doxorubicin sensitization in human A2780 ADR cells expressing ABCB1 assessed as doxorubicin at 2 uM incubated for 72 hrs by MTT assay Induction of doxorubicin sensitization in human A2780 ADR cells expressing ABCB1 assessed as doxorubicin at 2 uM incubated for 72 hrs by MTT assay	[PMID: 36584238]
A2780 ADR	GI₅₀	32.2 nM Compound: 24	Induction of doxorubicin sensitization in human A2780 ADR cells expressing ABCB1 assessed as doxorubicin at 5 uM incubated for 72 hrs by MTT assay Induction of doxorubicin sensitization in human A2780 ADR cells expressing ABCB1 assessed as doxorubicin at 5 uM incubated for 72 hrs by MTT assay	[PMID: 36584238]
A2780 ADR	GI₅₀	332 nM Compound: 24	Induction of doxorubicin sensitization in human A2780 ADR cells expressing ABCB1 assessed as doxorubicin at 1 uM incubated for 72 hrs by MTT assay Induction of doxorubicin sensitization in human A2780 ADR cells expressing ABCB1 assessed as doxorubicin at 1 uM incubated for 72 hrs by MTT assay	[PMID: 36584238]
A549	GI₅₀	19.4 nM Compound: 24	Induction of doxorubicin sensitization in human A549 cells expressing MCT1 assessed as doxorubicin IC50 at 500 nM incubated for 72 hrs by MTT assay Induction of doxorubicin sensitization in human A549 cells expressing MCT1 assessed as doxorubicin IC50 at 500 nM incubated for 72 hrs by MTT assay	[PMID: 36584238]
A549	GI₅₀	20 μM Compound: 24	Antiproliferative activity against human A549 cells expressing MCT1 assessed as growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells expressing MCT1 assessed as growth inhibition incubated for 72 hrs by MTT assay	[PMID: 36584238]
A549	GI₅₀	27.7 nM Compound: 24	Induction of doxorubicin sensitization in human A549 cells expressing MCT1 assessed as doxorubicin GI50 at 100 nM incubated for 72 hrs by MTT assay Induction of doxorubicin sensitization in human A549 cells expressing MCT1 assessed as doxorubicin GI50 at 100 nM incubated for 72 hrs by MTT assay	[PMID: 36584238]
A549	GI₅₀	40 nM Compound: 24	Induction of doxorubicin sensitization in human A549 cells expressing MCT1 assessed as doxorubicin GI50 at 50 nM incubated for 72 hrs by MTT assay Induction of doxorubicin sensitization in human A549 cells expressing MCT1 assessed as doxorubicin GI50 at 50 nM incubated for 72 hrs by MTT assay	[PMID: 36584238]
MCF7	GI₅₀	15.1 μM Compound: 24	Antiproliferative activity against human MCF7 cells expressing MCT1 assessed as growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells expressing MCT1 assessed as growth inhibition incubated for 72 hrs by MTT assay	[PMID: 36584238]

In Vitro

MCT1-IN-3 (compound 24) has inhibitory activity for MCT1 with an IC₅₀ value of 81.0 nM^[1].
MCT1-IN-3 has great antiproliferative activities against the MCT1-expressing cancer cell lines A-549 and MCF-7 with GI₅₀ values of 20 μM and 15.1 μM, respectively^[1].
MCT1-IN-3 (5 μM; 24 h) leads to cancer cell cycle arrest as well as apoptosis^[1].
MCT1-IN-3 (1.0, 2.0, 3.5, and 5.0 μM) shows to sensitize these cancer cells toward an antineoplastic agent^[1].
MCT1-IN-3 has also significant inhibitory power against the multidrug transporter ABCB1 and shows to reverse ABCB1-mediated multidrug resistance (MDR) ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[1]

Cell Line:

A-549 cells
Concentration:

5 μM
Incubation Time:

24 h
Result:

Caused a disruption of the cell cycle of A-549 cancer cells, indicated by a shift from the predominant Go/G, phase.

Apoptosis Analysis^[1]

Cell Line:

A-549 cells
Concentration:

5 μM
Incubation Time:

24 h
Result:

Increased the percentage of total apoptotic cells by a factor of 13 from 0.51 to 6.68%.

Chemical Information

CAS No. 2878360-80-4
Appearance Solid
Masse moléculaire 389.40
Formule C₂₂H₁₉N₃O₄
Color Off-white to light yellow
SMILES

COC(/C(C#N)=C/C1=CN(C2=CC=CC=C12)CC(NC3=CC=C(C=C3)OC)=O)=O
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Instruction de manipulation (2659 KB)

Références

[1]. Sachin Puri, et al. Indole Derivatives as New Structural Class of Potent and Antiproliferative Inhibitors of Monocarboxylate Transporter 1 (MCT1; SLC16A1). J Med Chem. 2023 Jan 12;66(1):657-676. [Content Brief]

Calculators

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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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100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Pureté et documentation
Références

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MCT1-IN-3

Anti-Cancer Metabolism Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cysteine Targeted Covalent Library

Anti-Drug-Resistant Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Membrane Transporter/Ion Channel Compound Library

Anti-Cancer Compound Library

Voir tous les produits spécifiques à Isoform Monocarboxylate Transporter

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

MCT1-IN-3

Anti-Cancer Metabolism Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cysteine Targeted Covalent Library

Anti-Drug-Resistant Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Membrane Transporter/Ion Channel Compound Library

Anti-Cancer Compound Library

Voir tous les produits spécifiques à Isoform Monocarboxylate Transporter

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

MCT1-IN-3 Related Classifications

HY-148574 Related Classifications