Androgen Receptor

Enzalutamide D3 is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells.

Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases.

AH3960 (compound 16c) is a androgen receptor antagonist. AH3960 can bind to both wild-type and T877 mutant androgen receptors, selectively inhibiting T877 (IC50=0.82 μM). AH3960 is also an agonist of the parathyroid hormone receptor PTHR1.

Enzalutamide-d6 is a deuterium-labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cancer cells.

Gumelutamide is a tetrahydropyridine and pyrimidine compound that acts as an anti-androgen and anti-tumor agent. Gumelutamide is an androgen receptor antagonist.

VPC-14228 is an effective androgen receptor DNA binding domain (AR-DBD) inhibitor that can interfere with the interaction between AR and androgen response elements, effectively blocking AR transcriptional activity. VPC-14228 can be used for research on prostate cancer.

ARD-69 (compound 34) is a potent PROTAC androgen receptor degrader.

VPC-13566, a BF3-specific small molecule, is an androgen receptor (AR) inhibitor.

BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7.

ARD-2051 is a potent and orally active androgen receptor (AR) proteolysis-targeting chimera degrader.

EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs).

(R)-SKBG-1 is an RNA-binding protein NONO inhibitor.

Androgen receptor-IN-6 (compound 16) is an orally available androgen receptor (Androgen Receptor) potent inhibitor (IC50=0.12 μM in vitro), targeting the disordered N-terminal domain (NTD).

ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand.

VNPP433-3β is a molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2.

SC912 is an AR-V7 inhibitor (IC50 = 0.36 μM).

GA32 (compound 58r) is potent androgen receptor (AR)/glucocorticoid receptor (GR) dual inhibitor with IC50 values of 0.13 μM and 0.83 μM for AR and GR, respectively.

SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain.

Spironolactone -d 6 -1 is the deuterium labeled Spironolactone.

Ketodarolutamide -d 6 (BAY 1896953-d 6 ) is the deuterium labeled Ketodarolutamide.

PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS).