Keap1-IN-1
Keap1-IN-1 (Compound 27) is the inhibitor for Keap1, that covalently modifys the Cys151 site in the BTB domain of KEAP1, and interfers with the interaction between Keap-Nrf. Keap1-IN-1 upregulates the mRNA expression of the antioxidant stress element (ARE) -dependent gene NQO1 with an EC50 of 160 nM. Keap1-IN-1 exhibits cytotoxicity in cell U2OS with an EC50 of 527 nM[1].
Product Specifications
UNSPSC
12352005
Target
Keap1-Nrf2; Quinone Reductase
Related Pathways
Metabolic Enzyme/Protease; NF-κB
Applications
Metabolism-protein/nucleotide metabolism
Field of Research
Others
Smiles
CCP1(CCN(C2=C(S(=O)(C3=C(Cl)C(Cl)=CC=C3)=O)N=C(S(=O)(CC)=O)S2)CC1)=O
Molecular Formula
C17H21Cl2N2O5PS3
Molecular Weight
531.43
References & Citations
[1]Fejes I, et al., Covalent Inhibitors of KEAP1 with Exquisite Selectivity. J Med Chem. 2024 Dec 12;67 (23) :21208-21222.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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