1. Metabolic Enzyme/Protease
    Apoptosis
  2. E1/E2/E3 Enzyme
    Apoptosis
  3. Keap1-Nrf2-IN-4

Keap1-Nrf2-IN-4 

Cat. No.: HY-144099
Handling Instructions

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

Keap1-Nrf2-IN-4 Chemical Structure

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Description

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[1].

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].

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].

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Keap1-Nrf2-IN-4
Cat. No.:
HY-144099
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