anti-androgen

Bicalutamide (ICI-176334), a synthetic, nonsteroidal antiandrogen, competitively binds to cytosolic androgen receptors in target tissues, thereby inhibiting the receptor binding of androgens.

4-Diethylaminobenzaldehyde, a reversible aldehyde dehydrogenase (ALDH) inhibitor (Ki: 4 nM for ALDH1), exhibits a potent anti-androgenic effect (IC50: 1.71 μM).

p,p'-DDE (p,p'-dichlorodiphenyldichloroethylene) is a metabolite and degradation product of the organochlorine pesticide DDT

CLP-3094 (2-([2-(4-CHLOROPHENOXY)ETHYL]THIO)-1H-BE) is a potent androgen receptor BF3 (binding function 3) inhibitor. BF3-IN-1 inhibits AR transcriptional activity with IC50 of 4 μM. CLP-3094 is a selective and potent GPR142 antagonist.

Nilutamide (RU23908), an antineoplastic hormonal agent, is mainly used in the treatment of prostate Y. Nilutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors, but not for estrogen, progestogen, or glucocorticoid receptors. Therefore, Nilutamide can block the action of androgens of testicular and adrenal origin that stimulate the growth of malignant and normal prostatic tissue. Prostate Y is mainly androgen-dependent and can be treat with chemical castration or surgical. So far, antiandrogen monotherapy has not consistently been certified to be equivalent to castration.

2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the antioxidant component of vitamin E (α-tocopherol) and exhibits significant androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines.

RU 58841 (PSK-3841) is a specific androgen receptor antagonist with significant effects on hair regrowth.

Enzalutamide-D3 is a deuterium-labeled form of the androgen receptor antagonist Enzalutamide (T6002), retaining potent anti-androgen and antineoplastic activity with an IC50 of 36 nM in LNCaP prostate cancer cells, and is primarily used in pharmacokinetic, metabolic tracing, and drug interaction studies.

SK33 is a potent and tissue selective anti-androgen agent. SK33 reduces androgen receptor (AR) transcriptional activity.

UT-34 is a selective and orally active antagonist of second-generation pan-androgen receptor (AR) and degrader(IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively), and has anti-prostate cancer efficacy.

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.

Gridegalutamide exhibits anti-androgen and anti-tumor activities.

Pentomone (LY-113935) is an anti-androgen compound that acts as a prostate growth inhibitor.

Cyproterone, an anti-androgen, is used in combination with estrogen for the therapy of hirsutism and severe acne in females and as a palliative in prostatic carcinoma.

PeS-9 is an androgen receptor (AR) degrader that induces the degradation of androgen receptors. It enhances the production of cytotoxic reactive oxygen species (ROS), leading to mitochondrial and endoplasmic reticulum stress, which results in the release of mitochondrial cytochrome C and AIF. PeS-9 activates caspase-9 and caspase-3, causing DNA fragmentation and apoptosis. It exhibits anti-prostate cancer activity and demonstrates antitumor and antimetastatic effects in vivo with minimal side effects. PeS-9 is applicable for targeted therapy research in GLUT-1 overexpressing tumors.

RU 56279 is an androgen receptor (AR) antagonist with potent systemic anti-androgen activity. It serves as a common, effective, and long-lasting anti-androgen metabolite of RU 56187 and RU 58841 in vivo. RU 56279 can be used as an AR ligand to develop AR-targeted prodrug systems for research on AR-positive tumor cells.

Lupeol (Monogynol B) is a novel androgen receptor inhibitor with anti-inflammatory and antioxidant activity.

Vicenin 2 is an angiotensin-converting enzyme (ACE) inhibitor (IC50=43.83 μM) from the aerial parts of Desmodium styracifolium. Vicenin 2 is an inhibitor of α-glucosidase, PTP1B, and RLAR. Vicenin 2 has hepatoprotective, anti-cancer, antioxidant and anti-inflammatory activities, and DTL co-administration is more effective than either of the single agents in androgen-independent prostate cancer. Vicenin 2 might be a useful lead for the development of multiple target-oriented therapeutic modalities for the treatment of diabetes and diabetes-associated complications. Vicenin 2 could act as a UV light barrier to protect the plants.

AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.Phase 1.

EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ～6 μM and a selective PPAR-gamma modulator.

A-849519 is a reversible inhibitor of MetAP2 that has demonstrated anti-angiogenesis and anticancer activity in a number of in vitro and in vivo models. In this study, we evaluated the anticancer activity of A-849519 in a modified Dunning model of androgen-independent prostate cancer and compared its efficacy with TNP-470, an established MetAP2 inhibitor.

RLA-4842, an iron activator with anti-androgen properties, exhibits anti-proliferative effects on the metastatic castration-resistant prostate cancer (mCRPC) cell line [1].

RLA-5331 is an anti-androgen compound with iron-activating properties, demonstrating anti-proliferative effects on the metastatic castration-resistant prostate cancer (mCRPC) cell line [1].

Galloylalbiflorin (6′-O-Galloylalbiflorin) is an androgen receptor (AR) antagonist isolated from the roots of Paeonia lactiflora and exhibits an IC50 value of 53.3 μM. Galloylalbiflorin (6′-O-Galloylalbiflorin) has been reported to possess anti-androgen activity. The androgen receptor antagonistic activity of Galloylalbiflorin (6′-O-Galloylalbiflorin) supports the application of Galloylalbiflorin (6′-O-Galloylalbiflorin) in research investigating androgen receptor signaling, hormone-responsive cellular pathways, and androgen-dependent disease mechanisms.