Androgen Receptor Inhibitor

CDK9-IN-50 is a selective and orally active CDK9 inhibitor with an IC₅₀ of 2.2 nM. CDK9-IN-50 targets a distinct CDK9-specific subpocket to disrupt RNA polymerase II Ser2 phosphorylation and downregulate short-lived oncoproteins, including AR-V7 and Myc. CDK9-IN-50 exhibits antiproliferative activity against cancer cells, induces apoptosis and induces tumor growth inhibition in CRPC orthotopic mice models. CDK9-IN-50 can be used for the research of cancer, such as prostate cancer.

Procyanidin B3 (Standard) is the analytical standard of Procyanidin B3. This product is intended for research and analytical applications. Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis.

AR antagonist 8 (compound 16), an unnatural entestrane, is a potent Lupeol-inspired androgen receptor (AR) antagonist with an IC₅₀ of 0.76 μM.

β-catenin inhibitory peptoid (compound 13) inhibits the β-catenin:TCF interaction with an IC₅₀ of 5.44 µM. β-catenin inhibitory peptoid inhibits both Wnt (IC₅₀ of 0.105 µM) and androgen receptor (AR)-signaling (IC₅₀ of 1.02 µM) in prostate cancer cell lines. β-catenin inhibitory peptoid markedly diminishes cell proliferation of prostate cancer cell lines.

Bicalutamide sulfide (compound 39) is a nonsteroidal antiandrogen. Bicalutamide sulfide can be used for the study of androgen-responsive benign and malignant disease.

AR/AR-V7-IN-1 (Compound 20i) is an AR/ARV7 inhibitor (IC₅₀ = 172.85 nM). AR/AR-V7-IN-1 potently inhibits cell growth with IC₅₀ values of 4.87 and 2.07 μM in the LNCaP and 22RV1 cell lines, respectively. AR/AR-V7-IN-1 exhibits effective tumor growth inhibition in the 22RV1 xenograft study. AR/AR-V7-IN-1 can be used for the research of prostate cancer.

Topilutamide (Standard) is the analytical standard of Topilutamide. This product is intended for research and analytical applications. Topilutamide is a topical nonsteroidal antiandrogen (NSAA).

Ac-PPPHPHARIK-NH2 (compound S1) is a compound that inhibits the interaction between androgen receptor and Src. It can inhibit the binding of androgen or estrogen-induced receptor and Src in cancer cells, as well as the activation of related signaling pathways, and can also inhibit cell cycle progression and tumor growth.

Androgen receptor-IN-7 is a potent androgen receptor (AR) inhibitor. Androgen receptor-IN-7 exhibits potent anticancer activity against PC-3 cells (IC₅₀ =370.37 nM) and LNCaP cells via both AR-dependent and AR-independent pathways. Androgen receptor-IN-7 induces ROS production in PC-3 cells. Androgen receptor-IN-7 can be used for prostate cancer research.

WNY0824 (PLK1/BRD4-IN-1) is an orally active dual inhibitor of PLK1 and BET protein families, with IC₅₀ values ​​of 22, 402.5, 150.7, 103.9, and 311.9 nmol/L for PLK1, BRD2, BRD3, BRD4, and BRDT, respectively. WNY0824 induces cell cycle arrest and apoptosis by inhibiting AR- and MYC-mediated transcriptional processes. In addition, WNY0824 also inhibits tumor growth in Enzalutamide (HY-70002) resistant CRPC xenograft tumor models.

VPC13163 is a potent androgen receptor (AR) BF3 inhibitor with an IC₅₀ of 0.31 µM. VPC13163 has anticancer effects.

AR antagonist 6 (compound 6i) is a diphenyl ether androgen receptor (AR) antagonist that binds AR at a concentration of 120 nM. AR antagonist 6 exhibits low toxicity and in vitro activity against the golden Syrian hamster ear model.

Androgen receptor-IN-4 (Compound 206) is an androgen receptor inhibitor, and can be used for research of Kennedy's disease.

Ch-319 is a Triphenyltin (IV) carboxylate derivative. Ch-319 reduces androgen receptor expression, AKT and PRAS40 phosphorylation levels, and increases FOXO3a expression. Ch-319 increases Apoptosis. Ch-319 can be used in the research of prostate cancer.

WH23 is a dehydrogenase/reductase SDR family member 11 (DHRS11) inhibitor with IC₅₀ values of 0.037 μM. WH23 binds to DHRS11, forming a hydrogen bond with the enzyme’s His210 residue. WH23 suppresses androgen receptor mRNA and protein expression, reduces c-Myc expression, and inhibits cancer cell proliferation. WH23 inhibits PI3K/AKT signaling by reducing phosphorylation of PDK1, AKT, mTOR, and ERK. WH23 enhances Capivasertib (HY-15431)-induced cytotoxicity and apoptosis. WH23 can be used for the research of luminal androgen receptor-positive triple-negative breast cancer.

L-Ornithine (hydrochloride) (Standard) is the analytical standard of L-Ornithine (hydrochloride). This product is intended for research and analytical applications. L-Ornithine hydrochloride is a non-proteinogenic amino acid, is mainly used in urea cycle removing excess nitrogen in vivo. L-Ornithine hydrochloride shows nephroprotective.

RU 58642 is an orally active non-steroidal antiandrogen, which displays a strong and selective affinity for androgen receptor.

KF-19418 is a hair follicle stimulator with hair growth promoting activity. KF-19418 stimulates proliferation of cultured hair bulb cells from newborn mice. KF-19418 accelerates hair regrowth in hair-clipped mouse alopecia model following topical application. KF-19418 can be used for the research of alopecia.

GSK-3β/G9a-IN-1 (Compound T2) is an orally active, selective, blood-brain-barrier permeable, competitive G9a (substrate-competitive, IC₅₀: 1.1 μM) and GSK-3β (ATP competitive, IC₅₀: 0.8 μM) inhibitor. GSK-3β/G9a-IN-1 is a potent H3K9me2 inhibitor that reshapes chromatin landscape. GSK-3β/G9a-IN-1 lowers tau phosphorylation, reduces Aβ aggregation. GSK-3β/G9a-IN-1 displays inhibition toward glucocorticoid receptor, androgen receptor, and alpha-2A adrenergic receptor. GSK-3β/G9a-IN-1 also upregulates SAGA complex members such as Eny2 and Sgf29. GSK-3β/G9a-IN-1 markedly improves memory, restores social behaviors, and increases synaptic complexity in late-onset Alzheimer’s disease.

XY25028 is an orally active LRH-1 inhibitor with an IC₅₀ of 0.30 μM. XY25028 inhibits the proliferation of androgen receptor (AR)-positive prostate cancer cells and suppresses the expression of AR target genes KLK2 and KLK3. XY25028 can be used in the research of castration-resistant prostate cancer.