Keap1-Nrf2-IN-4

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Keap1-Nrf2-IN-4 is a potent neddylation inhibitor. Keap1-Nrf2-IN-4 exhibits potent anti-proliferation activity against MGC-803 cells (IC₅₀=2.55 µM). Keap1-Nrf2-IN-4 blocks the migration ability and induces apoptosis of gastric cancer cells. Keap1-Nrf2-IN-4 inhibits tumor growth without obvious toxicity.

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

Keap1-Nrf2-IN-4 Chemical Structure

CAS No. : 2851480-01-6

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Description

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	3.88 μM Compound: 4g	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34624825]
GES1	IC₅₀	8.7 μM Compound: 4g	Cytotoxicity against human GES1 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human GES1 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34624825]
HepG2	IC₅₀	2.89 μM Compound: 4g	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34624825]
HGC-27	IC₅₀	3.17 μM Compound: 4g	Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34624825]
MCF7	IC₅₀	3.74 μM Compound: 4g	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34624825]
MGC-803	IC₅₀	2.55 μM Compound: 4g	Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34624825]

In Vitro

Keap1-Nrf2-IN-4 (compound 4g) (72 h) shows anti-proliferation activity (IC₅₀ s of 2.55, 3.88, 3.74, 2.89 µM in MGC-803, MCF-7, A549, HepG-2 cells, respectively)^[1].
Keap1-Nrf2-IN-4 inhibits neddylation of cullin1, cullin3, cullin5^[1].
Keap1-Nrf2-IN-4 blocks the migration ability of MGC-803 without cell cycle arrest^[1].
Keap1-Nrf2-IN-4 (24, 48 h) induces apoptosis of MGC-803 and HGC-27 cells in concentration- and time-dependent manners^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	MGC-803, MCF-7, A549, HepG-2 cells
Concentration:
Incubation Time:	72 h
Result:	Showed anti-proliferation activity (IC₅₀ of 2.55, 3.88, 3.74, 2.89 µM in MGC-803, MCF-7, A549, HepG-2 cells, respectively).

Apoptosis Analysis^[1]

Cell Line:	MGC-803, HGC-27 cells
Concentration:	2.5, 5, 7.5 µM for MGC-803 cells; 3, 6, 9 µM for HGC-27 cells
Incubation Time:	24 h, 48 h
Result:	Induced apoptosis of MGC-803 and HGC-27 cells in concentration- and time-dependent manners.

In Vivo

Keap1-Nrf2-IN-4 (50, 100 mg/kg; i.g.; per day for 21 days) exhibits antitumor activity on xenograft model without obvious side effect^[1].

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

Animal Model:	5-6 weeks, 18-20 g, NOD SCID mice (xenograft tumor model)^[1]
Dosage:	50, 100 mg/kg
Administration:	i.g.; per day, 21 days
Result:	Exihibited good antitumor activity on xenograft model without obvious side effect.

Molecular Weight

390.56

Formula

C₂₆H₃₄N₂O

CAS No.

2851480-01-6

SMILES

CCCCCC1=CC=C(C=C1)NC(C2CCN(CC2)C/C=C/C3=CC=CC=C3)=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

Handling Instructions (2659 KB)

References

[1]. Wang B, et al. Discovery of a cinnamyl piperidine derivative as new neddylation inhibitor for gastric cancer treatment. Eur J Med Chem. 2021; 226:113896. [Content Brief]

Keap1-Nrf2-IN-4 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.

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