akr1c1 in 1

AKR1C1-IN-1 is a human 20α-hydroxysteroid dehydrogenase (AKR1C1) inhibitor (Ki: 4 nM for AKR1C1).

1-Tetralol, (S)- ((S)-1-Hydroxytetralin) can be used as a substrate of AKR1C1 in cell assays.

AKR1Cs-IN-1 (Compound 29) is an effective and broad-spectrum inhibitor of the Aldo-Keto Reductase 1C family (AKR1C1-1C4). It achieves subtype inhibition by simultaneously binding to the SP2 and SP3 pockets, thereby blocking metabolic pathways related to drug resistance. In enzyme assays, AKR1Cs-IN-1 exhibits significant inhibitory activity with IC50 values of 0.09, 0.28, 0.05, and 0.51 µM for AKR1C1, AKR1C2, AKR1C3, and AKR1C4, respectively. The compound shows excellent resensitizing effects in doxorubicin (DOX)-resistant breast cancer cell line MCF-7/ADR, effectively enhancing the cytotoxicity of DOX. AKR1Cs-IN-1 holds promise for research on breast cancer resistance.

Keap1-Nrf2-IN-28 (SG16) is an orally active inhibitor of Keap1-Nrf2. It demonstrates antioxidant properties and upregulates the expression of Nrf2, HO-1, GCLM, and Akr1c1. Additionally, Keap1-Nrf2-IN-28 can mitigate acute liver injury induced by APAP.