AKR1C3

AKR1C3-IN-9, a selective Aldo-keto Reductase 1C3 (AKR1C3) inhibitor (IC50 = 8.92 nM), can significantly reverse Doxorubicin (DOX) resistance in a resistant breast cancer cell line.

AKR1C3-IN-4, a potent and selective inhibitor of aldo-keto reductase 1C3 (AKR1C3) with an IC50 of 0.56 μM, shows potential for castrate-resistant prostate cancer (CRPC) research.

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

S19-1035 is a potent and specific inhibitor of aldo-keto reductase 1C3 (AKR1C3), displaying an inhibitory concentration (IC50) of 3.04 nM. It is primarily utilized in tumor research.

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

Obafistat is a potent inhibitor of aldo-keto reductase AKR1C3 with an IC50 of 1.2 nM for human AKR1C3.

ASP-9521 is a selective, potent and orally active indole-based AKR1C3 inhibitor with an IC50 of 11 nM for human AKR1C3.

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.

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.

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

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].

AKR1C3-IN-7 (Compound 13) is a potent and selective AKR1C3 inhibitor with an IC50 of 0.19 μM, exhibiting antitumor activity.

AKR1C3-IN-8 (Compound 5) is a potent and selective AKR1C3 inhibitor (IC50 = 0.069 μM) with demonstrated antitumor activity.

AKR1C3-IN-5 (Compound 6e) is a potent inhibitor of AKR1C3, derived from drupanin, with significant activity against MCF-7 cells (IC50: 9.6 ± 3 μM; SI: 5.5). AKR1C3 enzymes are overexpressed in hormone-dependent prostate and breast tumors.

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-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.

Liquiritin (Liquiritigenin-4'-O-glucoside) (LIQ) is a main component among the licorice flavonoids, and possesses anti-inflammatory and anti-cancer abilities.

WEHL-04 is an intermediate used to prepare (isoquinolinylsulfonyl)benzoic acids as inhibitors of type 5 71-β-hydroxysteroid dehydrogenase AKR1C3. It is also used in the synthesis of 2-aminooctahydrocyclopentalene-3a-carboxamides as potent CCR2 antagonists

LX1, an anti-prostate cancer compound, specifically targets the androgen receptor (AR), AR variants, and the steroidogenic enzyme AKR1C3. It inhibits AKR1C3's enzymatic function, decreases the conversion of androstenedione to testosterone, and reduces the expression of both AR and AR-V7, subsequently downregulating their target genes. Additionally, LX1 is effective in overcoming tumor cell resistance to Enzalutamide, and when combined with Enzalutamide, it further suppresses tumor growth.

Pyrone-211 acts as a potent GPR84 agonist and an AKR1C3 inhibitor. It is involved in the extended polyamine pathway.

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.

RJG-2051 is a selective covalent inhibitor of aldo-keto reductase family 1 member C3 (AKR1C3), with an IC50 value of 13 nM. It interferes with the metabolism of substrates such as androgens, estrogens, and prostaglandins through AKR1C3. RJG-2051 holds potential for cancer research.