Bioactivity | 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]. |
Formula | C17H21Cl2N2O5PS3 |
Molar Mass | 531.43 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Fejes I, et al., Covalent Inhibitors of KEAP1 with Exquisite Selectivity. J Med Chem. 2024 Dec 12;67(23):21208-21222. |