vcap

AR antagonist 1 is a potent antagonist of the androgen receptor. It binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266.

RD162 is a non-steroidal antiandrogen (NSAA) specifically binding to the androgen receptor (AR).

Cetylpyridinium Chloride (Hexadecylpyridinium Chloride) is a cationic quaternary ammonium compound used as oropharyngeal antiseptic.

YJ1206 is a highly potent and selective CDK12/13 PROTAC degrader (IC50 =12.55 nM) with the advantages of oral administration and low toxicity, which triggers gene-length-dependent transcription elongation defects, leading to DNA damage and cell-cycle arrest, and inhibits the proliferation of a subpopulation of prostate cancer cells. YJ1206 can synergize with AKT pathway inhibitors to effectively inhibit prostate cancer.

ARD-2128 is a highly potent, orally bioavailable PROTAC (proteolysis-targeting chimera) that degrades the androgen receptor (AR), effectively reducing AR protein levels, suppressing AR-regulated gene expression in tumor tissues, and inhibiting tumor growth without evident toxicity. This compound holds promise for prostate cancer research.

EZM 2302 (GSK3359088) is a selective, and orally available arginine methyltransferase CARM1 inhibitor (IC50: 6 nM).[1]

ARD-2585 is an orally active and selective androgen receptor PROTAC degrader with anticancer activity for the study of prostate cancer.

HIVCapsid-IN-2 (Compound IC-2b4) is a potent inhibitor of the HIV-1 capsid protein (CA). It effectively inhibits both HIV-1, with an EC50 of 0.08 μM, and HIV-2. HIVCapsid-IN-2 operates by directly stabilizing the binding to HIV-1 CA, exerting its inhibitory effects in both early and late stages of infection.

HIVcapsid modulator 1 is a potent modulator of the HIV capsid and a phenylalanine derivative with a quinazolin-4-one structure. It exhibits antiviral activity against both HIV-1 and HIV-2.

HIVcapsid modulator 2 (Compound 7t) is a modulator of the HIV capsid protein (CA). It exhibits antiviral activity by inhibiting the HIV-1IIIB strain and HIV-2ROD strain, with EC50 values of 0.04 and 0.13 μM, respectively. Additionally, HIVcapsid modulator 2 demonstrates metabolic stability in human liver microsomes.

GDC-2992 is a selective and orally active androgen receptor (AR) degradator that degrades AR (DC50 = 2.7 nM) and inhibits proliferation (IC50 = 9.7 nM) in VCaP cells, making it suitable for studying castration-resistant prostate cancer (CRPC).

VHL Ligand 8, a VHL ligand essential for synthesizing ARD-266, acts as a highly potent VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. It efficiently facilitates the degradation of AR protein in AR-positive prostate cancer cell lines LNCaP, VCaP, and 22Rv1, exhibiting DC50 values ranging from 0.2-1 nM [1].

Boc-Pip-alkyne-Ph-COOH, a PROTAC linker characterized by its alkyl/ether composition, plays a crucial role in synthesizing PROTACs including ARD-266. This compound demonstrates significant efficacy in promoting the degradation of androgen receptor (AR) protein across AR-positive prostate cancer cell lines such as LNCaP, VCaP, and 22Rv1, showcasing DC50 values ranging from 0.2-1 nM[1].

PROTAC SMARCA2 degrader-26 (compound 45) is an effective degrader of SMARCA2 using the PROTAC technology. It induces degradation of SMARCA2 and SMARCA4 in VCaP cells, with degradation percentages of 94% and 57%, respectively. Additionally, PROTAC SMARCA2 degrader-26 demonstrates antiproliferative activity.

YJ9069 is a selective CDK12/CDK13P ROTAC degrader with an IC50 of 22.22 nM in VCaP cells. Rapid degradation of CDK12/13 by this compound triggers transcription elongation defects dependent on gene length, leading to DNA damage and cell cycle arrest. YJ9069 effectively inhibits the proliferation of prostate cancer cell subpopulations and significantly suppresses prostate tumor growth in vivo.

ID11916 is an orally active compound functioning as both an androgen receptor (AR) antagonist and a phosphodiesterase 5 (PDE5) inhibitor. It disrupts androgen binding to AR, impedes nuclear translocation, and blocks androgen-dependent transcriptional activity of AR, while simultaneously elevating intracellular cGMP levels by inhibiting PKG activation. Moreover, ID11916 exhibits potent anticancer effects in prostate cancer cell lines VCaP and 22Rv1, as well as in AR-positive breast cancer cell line SK-BR-3.

CBPD-409 is an orally active CBP/p300 degrader with a DC50 of 0.2–0.4 nM. It exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP, and 22Rv1, with an IC50 of 1.2–2.0 nM. Additionally, CBPD-409 shows antitumor activity.

LYA914 is an orally active AR/AR-V7 PROTAC degrader. It targets the proteolysis of the androgen receptor's (AR) conserved DNA-binding domain (DBD). LYA914 demonstrates effective antiproliferative activity in Enzalutamide-insensitive or resistant cells and inhibits tumor growth in VCaP/LNCaP tumor mouse models. It is suitable for studying castration-resistant prostate cancer (CRPC).

PROTACAR Degrader-11 is an effective PROTAC degrader of the androgen receptor (androgen receptor) and its splice variant 7. It exhibits potent cytotoxicity in both CWR22RV1 and VCaP cells and is utilized in prostate cancer research.

ARD-69 is a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer. ARD-69 induces degradation of AR protein in AR-positive prostate cancer cell lines in a dose- and time-dependent mann

BWA-522 is a small molecule, orally available protein-targeting chimera (PROTAC) that potentates the degradation of both full-length androgen receptor (AR-FL) and the AR-V7 splice variant. It specifically antagonizes the N-terminal domain (AR-NTD) of the androgen receptor (Androgen Receptor), prompting apoptosis in prostate cancer (PC) cells. In LNCaP xenograft models, BWA-522 demonstrated tumor growth inhibition (60 mg/kg, po; TGI=76%). The compound effectively reduced levels of AR-V7 and AR-FL by 77.3% at 1 μM and 72.0% at 5 μM, respectively, in VCaP and LNCaP cell lines [1].

PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule from the protein-targeting chimeras (PROTACs) that selectively targets the N-terminal domain (AR-NTD) of the Androgen Receptor variant AR-V7. By antagonizing AR-NTD, it effectively degrades AR-V7 protein and induces apoptosis in prostate cancer (PC) cells, with degradation efficiencies of 62.2% (1 μM) and 71.1% (5 μM) in VCaP cells [1].

ARD-2051 is a potent, orally active proteolysis-targeting chimera degrader of the androgen receptor (AR), exhibiting DC50 values of 0.6 nM in degrading AR protein within LNCaP and VCaP prostate cancer cell lines. It holds potential for prostate cancer research applications [1].

ARD-1676 is an orally administered androgen receptor (AR) PROTAC degrader that combines an AR ligand with a cereblon ligand. It demonstrates AR-degrading activity both in vitro and in vivo, and effectively inhibits VCaP tumor growth in mouse xenograft models [1].