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

Keap1-Nrf2-IN-4 是一种有效的 neddylation 抑制剂。Keap1-Nrf2-IN-4 对 MGC-803 细胞表现出较强的抗增殖活性 (IC50=2.55 µM)。Keap1-Nrf2-IN-4 阻断胃癌细胞的迁移能力并诱导细胞凋亡 apoptosis。Keap1-Nrf2-IN-4 抑制肿瘤生长且无明显毒性。

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Keap1-Nrf2-IN-4 Chemical Structure

Keap1-Nrf2-IN-4 Chemical Structure

CAS No. : 2851480-01-6

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Keap1-Nrf2-IN-4 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

细胞效力
(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]
体外研究
(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.

Keap1-Nrf2-IN-4 相关抗体:

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.
体内研究
(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.
分子量

390.56

Formula

C26H34N2O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Keap1-Nrf2-IN-4 相关分类

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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:

Keap1-Nrf2-IN-42851480-01-6E1/E2/E3 EnzymeApoptosisE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseAntitumorgastric cancerxenograft tumor modelMGC-803 cellsHGC-27 cellsapoptosismigration abilityInhibitorinhibitorinhibit

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