2. Signaling Pathways
  3. Vitamin D Related/Nuclear Receptor
  4. Androgen Receptor
  5. Androgen Receptor Degrader

Androgen Receptor Degrader

Androgen Receptor Degraders (20):

Cat. No. Product Name Effect Purity
  • HY-153342
    Luxdegalutamide
    		Degrader 98.94%
    Luxdegalutamide (ARV-766) is an orally active protein hydrolysis targeted chimeric (PROTAC) targeting androgen receptor (AR), which can degrade AR resistance related mutants, including T878/H875/L702 mutants. Luxdegalutamide has anti-tumor activity and can be used in the study of castration resistant prostate cancer.
  • HY-158101
    BMS-986365
    		Degrader 99.92%
    BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader, capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. (Blue: HY-W247437; Black: linker (HY-W126831); Pink: HY-168697).
  • HY-156111
    ARD-1676
    		Degrader 99.36%
    ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models.
  • HY-160777
    VNPP433-3β
    		Degrader 98.01%
    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. VNPP433-3β inhibits proliferation of cancer cell LNCaP, C4-2B and CWR22Rv1 with GI50 of 0.2, 0.3 and 0.31 μM. VNPP433-3β exhibits good pharmacokinetic characters in CD-1 mouse and inhibits tumor growth in the CWR22Rv1 xenograft mouse model.
  • HY-161741
    VinclozolinM2-2204
    		Degrader 98.00%
    VinclozolinM2-2204 is a androgen receptor (AR) AUTOTAC degrader, with an DC50 of 200 nM in LNCaP prostate cancer cells. VinclozolinM2-2204 induces the formation of AR+LC3+ autophagic membranes. VinclozolinM2-2204 can be used for the research of cancer.(Pink: AR inhibitor (HY-168296); Black: linker (HY-128833); Blue: CRBN Ligand (HY-168293))
  • HY-164807
    SARD279
    		Degrader
    SARD279 is a potent and selective Androgen Receptor degrader with DC50 value of 1099 nM. SARD279 can be used in prostate cancer research.(Structure Note: Pink: target protein ligand (HY-117486); Blue,: Hyt (HY-W001578); Black: linker (HY-W004896))
  • HY-149914
    WCA-814
    		Degrader
    WCA-814 is an androgen receptor (AR) antagonist-Hsp90 inhibitor conjugate. WCA-814 induces the degradation of full-length and AR-V7. WCA-814 has cytotoxic effect in prostatic cancer cells (IC50: 171.2 nM, 26.5 nM for LNCaP, 22Rv1 cell).
  • HY-156751
    PROTAC AR Degrader-6
    		Degrader
    PROTAC AR Degrader-6 (Compound 1) is a PROTAC androgen receptor degrader (DC50: 10 nM in VCaP cell). PROTAC AR Degrader-6 blocks the process of androgen receptor transduction and also degrades the receptor itself. PROTAC AR Degrader-6 can be used for prostate cancer research. Pink: AR ligand (HY-130845); Blue: E3 ligase ligand (HY-W1003189); Black: linker (HY-169975).
  • HY-163813
    AR Degrader-2
    		Degrader
    AR Degrader-2 (Compound 2) is a molecular glue that degrades androgen receptor (AR) with a DC50 of 0.3-0.5 μM in cell VCaP.
  • HY-157491
    K2-B4-5e
    		Degrader
    K2-B4-5e is a E3 ligase KLHDC2-based BRD4 and androgen receptor (AR) degradation PROTAC. K2-B4-5e is capable of inducing rapid and robust degradation of BET-family and AR proteins in cells.
  • HY-170448
    PROTAC AR Degrader-9
    		Degrader
    PROTAC AR Degrader-9 (Compound c6) is a PROTAC degrader for androgen receptor, that degrades AR in human hair follicle papilla cells (HDPCs) with a DC50 of 262.38 nM. PROTAC AR Degrader-9 promotes the expressions of paracrine factors, such as TGF-β1 and β-catenin, exhibits hair regenerating efficacy in mouse models. (Pink: ligand for target protein AR ligand-38 (HY-170450); Black: linker; Blue: ligand for E3 ligase Cereblon (HY-170449))
  • HY-163641
    AR Degrader-1
    		Degrader
    AR Degrader-1 (Compound ML 2-9) is a molecular glue androgen receptor (AR) monovalent degrader. AR Degrader-1 degrades AR through DCAF16 (E3 ligase) without obvious cytotoxicity in LNCaP prostate cancer cells.
  • HY-160262
    AR/BET protein degrader-1
    		Degrader
    AR/BET protein degrader-1 (Compound 149) is an Androgen Receptor and BET (bromodomain and extra-terminal domain) protein degrader that can be used in cancer research.
  • HY-155666
    YXG-158
    		Degrader
    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.
  • HY-149127
    Rosolutamide
    		Degrader
    Rosolutamide (ASC-JM17), a curcumin analog, is an orally active, potent Nrf1 and Nrf2 activator. Rosolutamide activates Nrf1, Nrf2 and heat shock factor 1 (Hsf1), thereby activating the expression of proteasome subunits, antioxidant enzymes and molecular chaperones. Rosolutamide degrades the polyglutamine (polyQ) androgen receptor (AR) via the ubiquitin-proteasome pathway and improves motor function in mouse models of spinal and bulbar muscular atrophy (SBMA). Rosolutamide improves mitochondrial function and promotes autophagy, decreases mutant protein aggregates, and attenuates intracellular/mitochondrial reactive oxygen species (ROS) levels.
  • HY-162702
    AZ'3137
    		Degrader
    AZ‘3137 (Compound 22) is an orally active PROTAC-type androgen receptor (AR) degrader, with a DC50 value of 22 nM. AZ'3137 can inhibit cell proliferation of LNCaP, with a GI50 value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice (Red: AR antagonists; Blue: CRBN ligand (HY-A0003); Black: linker).
  • HY-170329
    PROTAC AR Degrader-8
    		Degrader
    PROTAC AR Degrader-8 (Compound NP18) is the PROTAC degrader for androgen receptor (AR), that degrades AR-FL with DC50 of 0.018 μM and 0.14 μM in 22Rv1 cell and LNCaP cell, degrades AR-V7 with DC50 of 0.026 μM in 22Rv1 cell. PROTAC AR Degrader-8 inhibits the proliferation of cancer cell 22Rv1 and LNCaP with IC50 of 0.038 μM and 1.11 μM. PROTAC AR Degrader-8 arrests cell cycle at G2/M phase, induces apoptosis in 22Rv1 cell. PROTAC AR Degrader-8 exhibits anticancer efficacy in mouse and zebrafish model. (Pink: ligand for target protein AR ligand-33 (HY-170330); Black: linker (HY-W007731); Blue: ligand for E3 ligase Cereblon (HY-14658))
  • HY-148777
    A031
    		Degrader
    A031 is a highly effective PROTAC androgen receptor (AR) degrader with an IC50 value less than 0.25 μM for AR protein degradation. A031 has an inhibitory effect on tumor growth in zebrafish with human prostate cancer (VCaP).
  • HY-169385
    ATC-324
    		Degrader
    ATC-324 is an bivalent AR (Androgen Receptor) degrader based on the protein degradation technology platform AUTOphagy-TArgeting Chimera (AUTOTAC). ATC-324 induces the formation of AR/p62 complex, leading to autophagy-lysosomal degradation of AR. ATC-324 can reduce nuclear AR levels and downregulate target gene expression of AR and AR-v7, and also has a degradation effect on common AR mutants in PCa. ATC-324 is composed of target-binding ligand (TBL) Enzalutamide (HY-70002) and p62/SQSTM1 autophagy-targeting ligand (ATL) YT 6-2 analog-1 (HY-169386), connected by Boc-NH-PEG4-CH2CH2NH2 (HY-W008352). Among them, the active control of the target protein ligand is Enzalutamide carboxylic acid (HY-70002B), and the conjugate composed of the autophagy-targeting ligand and the linker is YT 6-2-PEG3-C2-NH2 (HY-169387).
  • HY-162764
    Androgen receptor degrader-5
    		Degrader
    Androgen receptor degrader-5 (compound 14k) exhibits promising properties, including superior androgen receptor degradation activity and antiproliferative activity.