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Nrf2-IN-3

CAT: 0804-HY-149508-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-149508-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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 , Gefitinib (HY-50895), and KEAP1 G333C-mutated xenograft to Cisplatin.
CAS Number
6325-13-9
UNSPSC
12352005
Target
Keap1-Nrf2; Reactive Oxygen Species (ROS)
Type
Reference compound
Related Pathways
Immunology/Inflammation; Metabolic Enzyme/Protease; NF-κB
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/nrf2-in-3.html
Purity
99.19
Solubility
DMSO : 116.67 mg/mL (ultrasonic)
Smiles
O=C(CCCSCCCC(N/N=C/C1=C(O)C=CC=C1)=O)N/N=C/C2=C(O)C=CC=C2
Molecular Formula
C22H26N4O4S
Molecular Weight
442.53
References & Citations
[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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported