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Cat. No.: HY-144099

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Keap1-Nrf2-IN-4

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.

CAS No.: 2851480-01-6
Formula: C₂₆H₃₄N₂O
Molecular Weight:390.56

Storage:

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

Data Sheet (266 KB)

Keap1-Nrf2-IN-4 Chemical Structure

CAS No.: 2851480-01-6

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Use of MCE Products

Fluorescent Dye

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

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

Biological Activity

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.

Chemical Information

CAS No. 2851480-01-6
Molecular Weight 390.56
Formula C₂₆H₃₄N₂O
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (266 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]. 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]

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.

Keywords

100 mg

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