AKR1C3 IN 1

AKR1C3-IN-1 is a potent and selective inhibitor of AKR1C3(IC50 of 13 nM).

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

S07-2005 racemic is a chemically potent and selective inhibitor of aldo-keto reductase 1C3 (AKR1C3), with an IC50 value of 0.13 μM and 0.75 μM for AKR1C3 and AKR1C4, respectively. Due to its inhibitory properties, it exhibits potential as a chemotherapeutic potentiator, specifically in the context of overcoming drug resistance in cancer [1].

AKR1C3-IN-6 (Compound 1) is a potent and specific AKR1C3 inhibitor, exhibiting IC50 values of 0.31 μM against AKR1C3 and 73.23 μM against AKR1C2. It demonstrates significant antitumor activity [1].

S07-1066, an aldo-keto reductase 1C3 (AKR1C3) inhibitor, enhances doxorubicin (DOX) cytotoxicity by selectively inhibiting AKR1C3-mediated reduction of DOX and reversing DOX resistance in cells with elevated AKR1C3 expression [1].

AKR1C3-IN-10 (compound 5r), a selective inhibitor of AKR1C3 with an IC50 of 51 nM, demonstrates efficacy in a prostate cancer xenograft model [1].

AKR1C3-IN-12 (compound 2j), an inhibitor of aldo-keto reductase 1C3 (AKR1C3), exhibits potent activity with an IC50 of 27 nM. It has been shown to enhance the effectiveness of Gemcitabine and Cisplatin in treating bladder cancer [1].