Butanoic acid, 4,4'-thiobis-, bis[[(2-hydroxyphenyl)methylene]hydrazide] (9CI)
![Butanoic acid, 4,4'-thiobis-, bis[[(2-hydroxyphenyl)methylene]hydrazide] (9CI) Structure](CAS/20240320/GIF/6325-13-9.gif)
- CAS No.
- 6325-13-9
- Chemical Name:
- Butanoic acid, 4,4'-thiobis-, bis[[(2-hydroxyphenyl)methylene]hydrazide] (9CI)
- Synonyms
- Nrf2-IN-3;Butanoic acid, 4,4′-thiobis-, bis[[(2-hydroxyphenyl)methylene]hydrazide];Butanoic acid, 4,4'-thiobis-, bis[[(2-hydroxyphenyl)methylene]hydrazide] (9CI)
- CBNumber:
- CB511803392
- Molecular Formula:
- C22H26N4O4S
- Molecular Weight:
- 442.53
- MDL Number:
- MOL File:
- 6325-13-9.mol
Butanoic acid, 4,4'-thiobis-, bis[[(2-hydroxyphenyl)methylene]hydrazide] (9CI) Chemical Properties,Uses,Production
Uses
Nrf2-IN-3 (Compound R16) is a small-molecule NRF2 inhibitor and increases reactive oxygen species (ROS) production. Nrf2-IN-3 selectively binds KEAP1 mutants and restores their NRF2-inhibitory function by repairing the disrupted KEAP1/NRF2 interactions, leading to proteasome-dependent NRF2 degradation in cells. Nrf2-IN-3 sensitizes KEAP1-mutated tumor cells to Cisplatin (HY-17394), Gefitinib (HY-50895), and KEAP1 G333C-mutated xenograft to Cisplatin [1].
in vivo
Nrf2-IN-3 (110 mg/kg i.p. daily for 5 days per week for six weeks) inhibits tumor growth and selectively sensitizes mKEAP1 A549ctl xenograft to Cisplatin (HY-17394)[1].
| Animal Model: | Palpable tumors were generated by subcutaneous injection of a million A549ctl or A549(WT-KEAP1) cells in the flank of NOD-SCID mice[1]. |
| Dosage: | 110 mg/kg for Nrf2-IN-3 and 2 mg/kg for Cisplatin. |
| Administration: | Combination of Cisplatin (2 mg/kg) and Nrf2-IN-3 (110 mg/kg). The treatment started on day 18 after subcutaneous injection of A549ctl cells. Mice were treated i.p. with R16 at 110 mg/kg daily for 5 consecutive days per week, Cisplatin at 2 mg/kg twice per week, or the combination of both, or the vehicle |
| Result: | Combination of Cisplatin and Nrf2-IN-3 strongly inhibited the growth of A549ctl xenograft, while Cisplatin or Nrf2-IN-3 alone has no effect[1]. Cisplatin alone or in combination with Nrf2-IN-3 significantly inhibited the growth of A549(WT-KEAP1) xenograft, but Nrf2-IN-3 did not significantly enhance the efficacy of cisplatin against this WT-KEAP1 tumor[1]. Cisplatin alone caused slight, but significant, weight loss, Nrf2-IN-3 did not enhance Cisplatin toxicity. Nrf2-IN-3 alone or in combination with Cisplatin significantly decreased the levels of the NRF2 protein in the A549ctl tumors but not in the A549 (WT-KEAP1) tumors. |
References
[1] Aboulkassim T, et al. A NRF2 inhibitor selectively sensitizes KEAP1 mutant tumor cells to cisplatin and gefitinib by restoring NRF2-inhibitory function of KEAP1 mutants. Cell Rep. 2023 Sep 12;42(9):113104. DOI:10.1016/j.celrep.2023.113104
Butanoic acid, 4,4'-thiobis-, bis[[(2-hydroxyphenyl)methylene]hydrazide] (9CI) Preparation Products And Raw materials
Raw materials
Preparation Products
Butanoic acid, 4,4'-thiobis-, bis[[(2-hydroxyphenyl)methylene]hydrazide] (9CI) Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Shanghai Chaolan Chemical Technology Center | 021-QQ：65489617 15618227136 | Sales@ATKchemical.com | China | 9343 | 58 |
| ShangHai ChuanQian Chemcial Technique Centre | 15869524721 | 3525679403@qq.com | China | 4665 | 58 |
| Bide Pharmatech Ltd. | 400-1647117 13681763483 | product02@bidepharm.com | China | 62321 | 58 |
| Wuhan Jingkangen Biomedical Technology Co., Ltd | 13720134139 086-15871494362 13720134139 | orders@jknbiochem.com | China | 6203 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 24803 | 58 |
| Jiangsu Aikon Biopharmaceutical R&D Co.,Ltd | 025-58851090 17714375163 | 2881759498@qq.com | China | 13011 | 58 |
| Selleck Chemicals | 400-668-6834 | info@selleck.cn | China | 6071 | 58 |