AR-V7 Degrader
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MTX-23
0 ImagesSynonyms: PROTAC AR-V7 degrader-2MTX-23 is a PROTAC degrader targeting androgen receptor splice variant 7 (AR-V7) and full-length androgen receptor (AR-FL), with DC50 values of 0.37 μM and 2 μM, respectively. MTX-23 binds to the DNA-binding domains of AR-V7 and AR-FL, recruits the VHL E3 ubiquitin ligase (E3 ubiquitin ligase) and induces their degradation. MTX-23 reduces the proliferation of prostate cancer cells, promotes their apoptosis (apoptosis), and also inhibits tumor growth in mouse models. MTX-23 can be used for the research of prostate cancer.
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PROTAC AR Degrader-11
0 ImagesCat. No.: HY-177694CAS No.: 2798907-41-0PROTAC AR Degrader-11 is a PROTAC degrader that targets the androgen receptor (AR) and its splice variant AR-V7. PROTAC AR Degrader-11 simultaneously degrades full-length AR and AR-V7 via the ubiquitin-proteasome system by recruiting the CRL4-CRBN E3 ligase (FIG.2A). PROTAC AR Degrader-11 reduces the viability of cancer cells. PROTAC AR Degrader-11 can be used in studies related to castration-resistant prostate cancer.
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YXG-158
0 ImagesCat. No.: HY-155666CAS No.: 2952994-34-0YXG‑158 is an orally active, anticancer bifunctional steroid analog with both androgen receptor (AR) degradation activity (DC50 = 1.28 μM) and CYP17A1 inhibitory activity (IC50 = 100 nM). YXG-158 reduces AR protein and mRNA expression via proteasome-dependent degradation, degrades AR-V7, and inhibits CYP17A1 enzymatic activity to block androgen biosynthesis. YXG-158 inhibits the activities of ERα and ERβ, as well as cancer cell proliferation. YXG-158 decreases the weight of androgen-sensitive organs in castrated rats treated with testosterone propionate, downregulates AR protein, reduces PSA levels, and suppresses tumor growth in Enzalutamide (HY-70002)-sensitive and -resistant xenograft models. YXG-158 can be used in prostate cancer-related research.
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TD-802
0 ImagesCat. No.: HY-146397CAS No.: 2760703-21-5TD-802 is a CRBN-recruiting PROTAC androgen receptor (AR) degrader with liver microsomal stability and in vivo pharmacokinetic properties. TD-802 exhibits weak degrading activity against the AR-V7 splice variant, and its degradation process depends on the ubiquitin-proteasome system and Cullin-Ring ubiquitin ligase. TD-802 inhibits the proliferation of AR-dependent prostate cancer cells and the growth of AR-positive prostate cancer tumors in in vivo xenograft models.
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LYA914
0 ImagesCat. No.: HY-175455LYA914 is an orally effective AR/AR-V7 PROTAC degrader. LYA914 recruits CRBN to target and bind the conserved DBD domain of AR and AR-V7, inducing their ubiquitination and subsequent degradation, thereby completely blocking AR signaling and transcriptional activity. LYA914 can be used for the research of castration-resistant prostate cancer.
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EST1140
0 ImagesCat. No.: HY-187458CAS No.: 3105892-11-0EST1140 is a covalent molecular glue degrader targeting RNF126 for AR/AR-V7, with DC50 values of 33 μM and 30 μM, respectively, in 22Rv1 cells. EST1140 covalently binds to the E3 ligase RNF126 to achieve targeted protein degradation. EST1140 can be used in the research of androgen-independent prostate cancer.
