akr1c3-in-1

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

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].

AKR1C3-IN-15 (compound 30) is an effective and selective AKR1C3 inhibitor with an IC50 value of 5 nM. It enhances Sorafenib-induced ROS production, promotes apoptosis, and restores sensitivity to Sorafenib in hepatocellular carcinoma (HCC) models, as demonstrated in both in vitro and in vivo studies.

AKR1C3-IN-11 (Compound 6e) is an inhibitor of aldehyde ketone reductase 1C3 (AKR1C3) with an IC50 of 2.0 μM. When combined with abiraterone, AKR1C3-IN-11 can suppress cell proliferation and is applicable in prostate cancer research.

AKR1C3-IN-13 (Compound 4) is an inhibitor of AKR1C3. It can degrade AKR1C3 within prostate cancer cells.

AKR1C3-IN-14 (compound 4) is an inhibitor of AKR1C3 enzyme, exhibiting an IC50 value of 0.122 μM. It reduces excess androgen production by inhibiting the activity of the AKR1C3 enzyme, thereby regulating hormone-mediated signaling. Additionally, AKR1C3-IN-14 plays a role in the biosynthesis of prostaglandin PGF2α, influencing this pathway to regulate cell proliferation. This compound is utilized in the research of prostate cancer.

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

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.

PROTACAKR1C3 degrader-1 (compound 5) is an efficient AKR1C3 PROTAC degrader. It effectively reduces the protein expression of AKR1C3, AKR1C1/2, and ARv7. PROTACAKR1C3 degrader-1 shows potential for research in prostate cancer.

AKR1C2/3-IN-1 (compound 3a) is a potent inhibitor of AKR1C2 and AKR1C3, with IC50 values of 90 nM and 50 nM, respectively. It serves as a radiosensitizer and an enhancer of the cytotoxicity of chemotherapy.

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].