MCT1-IN-3

Name: MCT1-IN-3
Brand: MedChemExpress
SKU: HY-148574
Rating: 4.5 (1 reviews)

Cat. No.: HY-148574 Purity: 98.65%: Data Sheet
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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.

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

MCT1-IN-3 Chemical Structure

CAS No. : 2878360-80-4

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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MCT1 MCT2 MCT4

Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

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

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%.

Molecular Weight

389.40

Formula

C₂₂H₁₉N₃O₄

CAS No.

2878360-80-4

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Purity: 98.65%

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Data Sheet (275 KB) SDS (251 KB)

COA (256 KB) HNMR (106 KB) LCMS (98 KB)

Handling Instructions (2659 KB)

References

[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]

MCT1-IN-3 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:

MCT1-IN-32878360-80-4Monocarboxylate TransporterP-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243monocarboxylate transporter 1 (MCT1)multidrug transportercancerInhibitorinhibitorinhibit

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MCT1-IN-3

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MCT1-IN-3 Related Classifications

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