HG122 promotes androgen receptor (AR) degradation through the proteasome pathway inhibiting the castration-resistant prostate cancer.
Triptophenolide is a colorless crystalline plate isolated from ethyl acetate extracts of Tripterygium wilfordii. IC50 value:Target:In vitro: Triptophenolide can remarkably inhibit the delayed type hypersensitivity (DTH) reaction induced by DNCB and BSA; and diminished the peripheral blood ANAE+lymphocytes in rats and micc. Moreover, triptophenolide can dramatically increase the amount of total serum complement and significautly decrcase the serum antibody products (1gG ) of rats and mice. The phagocytosis of perioneal exudate macrophages in mice present double effects in vitro [1].In vivo:
LY2452473 is an orally bioavailable, selective androgen receptor modulator (SARM).
UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively. UT-34 binds to ligand-binding domain (LBD) and function-1 (AF-1) domains and requires ubiquitin proteasome pathway to degrade the AR. UT-34 has anti-prostate cancer efficacy[1][2].
Ostarine(MK-2866; GTX-024) is a modulator of human androgen receptor.IC50 value:Target: androgen receptorOstarine (MK-2866) is an androgen receptor modulator (SARM) with an ED50 of 0.44 mg/day. Ostarine (MK-2866) has anabolic activity. Lack of PSA increases in men and hair growth in women further corroborated selective anabolic effects of Ostarine (MK-2866). Ostarine (MK-2866) also resulted in a dose-dependent decrease in LDL and HDL cholesterol levels, with the average LDL/HDL ratio for all doses remaining in the low cardiovascular risk catergory.
RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer[1].
Androgen receptor antagonist 3 (Compound C18) is an androgen receptor (AR) antagonist with an IC50 of 2.4 μM. Androgen receptor antagonist 3 shows anticancer activities[1].
Trimegestone (RU 27987) is an orally active 19-norpregnane progestin. Trimegestone binds to progesterone receptor (PR) with an IC50 value of 3.3 nM (rat PR). Trimegestone increases alkaline phosphatase activity (EC50=0.1 nM) but not luciferase activity. Trimegestone also shows a weak antiandrogenic activity (weak androgen receptor affinity). Trimegestone can be used in studies of contraception or menopausal syndromes[1][2].
Boldenone Cypionate is an androgenic anabolic steroid.
Isosilybin B, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation[1][2].
Brassicasterol, a metabolite of Ergosterol, plays a role in the inhibitory effect on bladder carcinogenesis promotion via androgen signaling[1]. Brassicasterol shows dual anti-infective properties against HSV-1 (IC50=1.2 µM) and Mycobacterium tuberculosis, and cardiovascular protective effect[2]. Brassicasterol exerts an anti-cancer effect by dual-targeting AKT and androgen receptor signaling in prostate cancer[3].
TD-802 (Compound 33c) is an androgen receptor (AR) PROTAC degrader with good microsomal stability. TD-802 has good antitumor efficacy in vivo and can be used for metastatic castration-resistant prostate cancer research[1].
AR antagonist 2 (compound 58) is a potent androgen receptor (AR) inhibitor with an IC50 of 0.95 μM. AR antagonist 2 has the potential for cancer research[1].
SNIPER(AR)-51 (AR-51), consists of a cIAP1 ligand and an androgen ligand, connected by a linker[1]. SNIPER(AR)-51 induces androgen receptor (AR) protein degradation[1].
Rezvilutamide (SHR3680) is an androgen receptor antagonist. Rezvilutamide (SHR3680) is used for the study of prostate cancer[1][2].
Galloylalbiflorin (6′-O-Galloylalbiflorin) is an androgen receptor (AR) antagonist (IC50=53.3 μM) and can be found in the roots of Paeonia lactiflora. Galloylalbiflorin shows anti-androgens activity[1].
ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations[1].
N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.
LGD-4033 is a novel nonsteroidal, oral SARM that binds to androgen receptor with high affinity (Ki of 1 nM) and selectivity.IC50 value: 1 nM (Ki, for androgen receptor) Target: androgen receptorin vitro: LGD-4033, a novel nonsteroidal oral, selective androgen receptor modulator, binds androgen receptor with high affinity and selectivity.in vivo: LGD-4033 has demonstrated anabolic activity in the muscle, anti-resorptive and anabolic activity in bone, and robust selectivity for muscle versus prostate In animal models. LGD-4033 is well tolerated, has a long elimination half-life and dose-proportional accumulation upon multiple dosing. LGD-4033 is safe, has favorable pharmacokinetic profile, and increases lean body mass even during this short period without change in prostate-specific antigen.
Androgen receptor antagonist 4 (Compound AT2) is an androgen receptor (AR) antagonist with an IC50 of 0.15 μM. Androgen receptor antagonist 4 efficiently antagonizes AR transcriptional activity, suppresses downstream target gene of AR, and blocks the DHT-induced AR nuclear translocation. Androgen receptor antagonist 4 shows anticancer activities[1].
JJH260 is AIG1inhibitor, and inhibit the fluorophosphonate reactivity and fatty acid esters of hydroxy fatty acid (FAHFA) hydrolysis activity of AIG1in HEK293T cells, with IC50 values of 0.50 μM and 0.57 μM, respectively[1].
BX341 is an anti-androgen.
Spironolactone is a potent antagonist of the androgen receptor. Target: Androgen ReceptorSpironolactone is a potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. 5% topical spironolactone cream acts as an antiandrogen in human sebaceous glands, competing with DHT receptors and producing a decrease of labelled DHT. At the concentrations used the effect has been only local. No side-effects were recorded during both studies [1]. Patients who received spironolactone had a significant improvement in the symptoms of heart failure, as assessed on the basis of the New York Heart Association functional class (P<0.001). Gynecomastia or breast pain was reported in 10 percent of men who were treated with spironolactone, as compared with 1 percent of men in the placebo group (P<0.001). The incidence of serious hyperkalemia was minimal in both groups of patients [2].
YXG-158 (Compound 23-h) is an orally active AR degrader and CYP17A1 inhibitor. YXG-158 has AR degradation activity with DC50 value of 1.28 μM. YXG-158 can inhibit CYP17A1 with IC50 value of 100 nM. XG-158 can be used for the research of enzalutamide-resistant prostate cancer[1].
Stanolone benzoate (Androstanolone benzoate) is a synthetic androgen and anabolic steroid[1].
MK-0773 is a selective androgen receptor modulators (SARMs) that binds to AR with an IC50 of 6.6 nM.
Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.Target: androgen receptor in vitro: Flutamide (Eulexin) is an antiandrogen drug. Flutamide-OH, the active metabolite of flutamide, directly binds at rat anterior pituitary androgen receptor with Ki values of 55 nM [1]. lutamide does not affect the proliferation of an androgen-sensitive clone of the mouse mammary carcinoma Shionogi SC-l 15 cells in culture, shows only antiandrogenic effect, but not androgenic effect [2]. Flutamide provides treatment for prostate cancer when used along with leuprolide [3].in vivo: Flutamide causes a markedly reduction in rat ventral prostate weight from 319 mg to 245 mg. A combination of flutamide and LHRH agonist induces an additive effect with a decrease in prostate weight to 101 mg, and an marked drop in prostatic ODC activity [4].
ARD-69 (compound 34) is a potent PROTAC androgen receptor degrader. ARD-69 induces degradation of androgen receptor (AR) protein in AR-positive prostate cancer cell lines. ARD-69 suppresses AR-regulated gene expression[1].
Testosterone decanoate-d3 is the deuterium labeled Testosterone decanoate. Testosterone decanoate is a naturally occurring androgen testosterone ester. Testosterone decanoate shows long-acting male antifertility effects.
ASC-J9 is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.