1c3

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-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-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-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-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-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.

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

Cyclosporin A is a natural product and an active fungal metabolite, classified as a cyclic polypeptide immunosuppressant. It binds to cyclophilin and inhibits the activity of calcineurin (IC₅₀ = 7 nM) as well as CD11a/CD18 adhesion molecules. It is commonly used to induce uremia models.

5-Fluorouracil (5-FU) is a uracil analog and inhibitor of DNA synthesis, exhibiting antitumor activity by affecting pyrimidine synthesis through thymidylate synthase inhibition; it induces apoptosis and autophagy.

IBMX (Methylisobutylxanthine) is a broad-spectrum phosphodiesterase (PDE) inhibitor with inhibitory activity against PDE3, PDE4, and PDE5 (IC50=6.5/26.3/31.7 μM). IBMX enhances the intracellular cAMP level.

(-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.

Q-VD-OPh is an irreversible caspase inhibitor with an IC50 value of 48 nM against caspase-7 and between 25 and 400 nM against caspase-1, 3, 8, 9, 10, 12. Q-VD-OPh inhibits HIV infection and can cross the blood-brain barrier.

Rutin (Quercetin 3-O-rutinoside), a flavonoid, has a variety of biological activities including antiallergic, anti-inflammatory, antiproliferative, and anticarcinogenic properties.

Corticosterone (Kendall's compound B) is an adrenocortical steroid with salocorticoid and glucocorticoid activity that is orally active. Corticosterone is involved in the regulation of energy, immune responses, and stress responses in the body.

diABZI STING agonist-1 (Tautomerism) (diABZI STING agonist (Compound 3)) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.

Deoxynivalenol (Vomitoxin) is a mycotoxin produced by Fusarium spp. of the single trichothecene family and is commonly found in contaminated food and feed.Deoxynivalenol crosses the intestinal mucosa via a cellular bypass at the tight junctions.Deoxynivalenol transporters are unaffected by inhibitors of P-glycoprotein (PgP) or multidrug resistance-associated protein (MRP). Deoxynivalenol commonly causes diarrhea, vomiting, and gastrointestinal inflammation in humans and animals.

Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.

Adezmapimod (SB 203580) is a selective, ATP-competitive p38 MAPK inhibitor (IC50=0.3-0.5 μM) that activates autophagy and mitochondrial autophagy, with more than 100-fold higher selectivity over PKB, LCK, and GSK-3β.

Dinaciclib (SCH 727965) is a selective CDK inhibitor targeting CDK1, CDK2, CDK5, and CDK9 (IC50 = 3/1/1/4 nM). It exhibits potential antitumor activity by inhibiting the incorporation of thoracic glycan (dThd) DNA.