MEK-IN-5

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MEK-IN-5 is a potent MEK inhibitor and NO donor. MEK-IN-5 significantly reduces the levels of pMEK and pERK in a dose-dependent and time-dependent manner. MEK-IN-5 induces apoptosis in MDA-MB-231 cells.

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

MEK-IN-5 Chemical Structure

CAS No. : 2417022-06-9

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	1.35 μM Compound: 18h	Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay	[PMID: 32305784]
HCT-116	IC₅₀	0.64 μM Compound: 18h	Antiproliferative activity against human HCT116 cells harboring KRAS G13D mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay Antiproliferative activity against human HCT116 cells harboring KRAS G13D mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay	[PMID: 32305784]
L02	IC₅₀	5.62 μM Compound: 18h	Cytotoxicity against human HL7702 cells assessed as reduction in cell viability after 96 hrs by Celltiter-Glo assay Cytotoxicity against human HL7702 cells assessed as reduction in cell viability after 96 hrs by Celltiter-Glo assay	[PMID: 32305784]
MDA-MB-231	IC₅₀	0.034 μM Compound: 18h	Antiproliferative activity against human MDA-MB-231 cells harboring KRAS G13D/BRAF G464V mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay Antiproliferative activity against human MDA-MB-231 cells harboring KRAS G13D/BRAF G464V mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay	[PMID: 32305784]
Vero	IC₅₀	21.07 μM Compound: 18h	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 96 hrs by Celltiter-Glo assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 96 hrs by Celltiter-Glo assay	[PMID: 32305784]

In Vitro

MEK-IN-5 (compound 18h) shows anti-proliferation activities for different tumor cells and low toxicity for normal cells^[1].
MEK-IN-5 (0.1, 1, 10 µM; 1, 2, 4, 6 h) decreases the expression level of pMEK and pERK in a dose-dependent and time-dependent manner^[1].
MEK-IN-5 (1, 10 µM; 24 h) induces apoptosis in MDA-MB-231 cells^[1].
MEK-IN-5 (100 µM; 2h) significantly induce NO release in HCT116 cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	MDA-MB-231, HCT116, A549, Vero, HL7702 cells
Concentration:
Incubation Time:
Result:	Showed anti-proliferation activities in MDA-MB-231, HCT116, A549, Vero, HL7702 cells with IC₅₀s of 0.034, 0.64, 1.35, 21.07, 5.62 µM, respectively.

Western Blot Analysis^[1]

Cell Line:	MDA-MB-231 cells
Concentration:	0.1, 1, 10 µM
Incubation Time:	1, 2, 4, 6 h
Result:	Decreased the expression level of pMEK and pERK in a dose-dependent and time-dependent manner.

Apoptosis Analysis^[1]

Cell Line:	MDA-MB-231 cells
Concentration:	1, 10 µM
Incubation Time:	24 h
Result:	Induced apoptosis in MDA-MB-231 cells.

Molecular Weight

674.67

Formula

C₂₉H₂₇FN₄O₁₀S₂

CAS No.

2417022-06-9

SMILES

O=C1OC2=C(C(C)=C1CC3=C(F)C(NS(=O)(NC)=O)=CC=C3)C=CC(OCCCOC4=NO[N+]([O-])=C4S(=O)(C5=CC=CC=C5)=O)=C2

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

Handling Instructions (2659 KB)

References

[1]. Wang C, et al. Hybrids of MEK inhibitor and NO donor as multitarget antitumor drugs. Eur J Med Chem. 2020; 196:112271. [Content Brief]

MEK-IN-5 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:

MEK-IN-52417022-06-9ApoptosisMEKMitogen-activated protein kinase kinaseMAPKKMAP2KAntitumorMDA-MB-231 cellspMEKpERKapoptosisNO releaseanti-proliferationHCT116 cellsInhibitorinhibitorinhibit

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