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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
53 Results for "
VCaP
" in MedChemExpress (MCE) Product Catalog:
Products (53)
53 Results for "VCaP" in MCE Product Catalog:
Cat. No.: HY-175455
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LYA914 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 .
Cat. No.: HY-164807
CAS No.: 1489236-55-6
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SARD279 is a HyT degrader of androgen receptor (AR). SARD279 binds to AR, recruits HSP70, mediates ubiquitin-dependent proteasomal degradation, and competitively inhibits the transactivation of AR. SARD279 exhibits antiproliferative activity in AR-dependent prostate cancer cells and castration-resistant prostate cancer cells, including those harboring the AR F876L mutation. SARD279 can be used in studies related to prostate cancer and castration-resistant prostate cancer .
Cat. No.: HY-16985R
CAS No.: 1297538-32-9
Synonyms: ODM-201 (Standard); BAY-1841788 (Standard)
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Darolutamide (Standard) is the analytical standard of Darolutamide (HY-16985). This product is intended for research and analytical applications. Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a Ki of 11 nM for rat wild-type AR (wtAR) and an IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .
Cat. No.: HY-130845
CAS No.: 1818885-54-9
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AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
Cat. No.: HY-161483
CAS No.: 1936425-34-1
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CBP/p300 ligand 3 (conpound 3) is a CBP/p300 bromodomain ligand that binds to the CBP and p300 bromodomains with IC50 values of 1.1 nM and 1.3 nM, respectively. CBP/p300 ligand 3 can be used to synthesize CBPD-268 (HY-161369) .
Cat. No.: HY-148777
CAS No.: 2682255-44-1
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A031 is a PROTAC degrader targeting the androgen receptor. A031 induces time-dependent degradation of androgen receptor protein. A031 exerts tumor growth inhibitory effects in a zebrafish model xenografted with human prostate cancer cells. A031 can be used in studies related to prostate cancer .
Cat. No.: HY-146397
CAS No.: 2760703-21-5
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TD-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 .
Cat. No.: HY-156751
CAS No.: 2753650-84-7
Synonyms: (Rac)-RO7656594; PROTAC AR Degrader-6
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(Rac)-GDC-2992 ((Rac)-RO7656594; PROTAC AR Degrader-6) (Compound 1) is an androgen receptor (AR) PROTAC degrader with a DC50 of 10 nM in VCaP cells. (Rac)-GDC-2992 blocks androgen receptor-mediated signaling processes and also degrades the receptor itself. (Rac)-GDC-2992 can be used in prostate cancer research, including studies on castration-resistant prostate cancer and metastatic castration-resistant prostate cancer .
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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 .
Cat. No.: HY-133044
CAS No.: 2581824-70-4
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Boc-Pip-alkyne-Ph-COOH is a PROTAC linker, which refers to the alkyl/ether composition. Boc-Pip-alkyne-Ph-COOH can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 effectively induces degradation of androgen receptor (AR) protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM . Boc-Pip-alkyne-Ph-COOH is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cat. No.: HY-149434
CAS No.: 3032601-92-3
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PROTAC AR-NTD degrader 1 is a PROTAC degrader that recruits cereblon and targets the N-terminal domain of the androgen receptor (AR-NTD), thereby inducing the degradation of AR-FL and AR-V7 proteins. PROTAC AR-NTD degrader 1 can be used for studies related to androgen receptor degradation and prostate cancer .
Cat. No.: HY-173467
MTP3 is a MYC PROTAC Degrator. MTP3 facilitates ternary complex formation with CRBN, driving proteasome-dependent full-length MYC degradation and partially proteasome-independent N-terminal truncated MYC (tMYC) generation. MTP3 induces tMYC formation across multiple cancer cell lines with context-dependent response variability. MTP3 can be used for the research of prostate cancer, breast cancer .
Cat. No.: HY-168201
CAS No.: 3105406-14-9
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MJP6412 is a p300 and CBP PROTAC degrader that potently degrades p300 and CBP in 22Rv1 cells with DC50 values of 1.6 nM and 1.2 nM, respectively. MJP6412 downregulates the expression of AR-FL, AR-V7 and c-MYC, as well as androgen receptor target genes (KLK3, FKBP5, TMPRSS2). MJP6412 completely abolishes p300/CBP-dependent histone acetylation (H3K27Ac and H2BNTAC) and induces G1 cell cycle arrest. MJP6412 inhibits cancer cell proliferation and tumor growth. MJP6412 can be used in prostate cancer-related research .
Cat. No.: HY-169278
CAS No.: 2760247-27-4
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PROTAC SMARCA2 degrader-26 (compound 45) is a potent SMARCA2 PROTAC degrader. PROTAC SMARCA2 degrader-26 induces SMARCA2 and SMARCA4 degradation in VCaP cells with the percent degradation of 94% and 57% for SMARCA2 and SMARCA4, respectively. PROTAC SMARCA2 degrader-26 shows antiproliferative activity .
Cat. No.: HY-169273
CAS No.: 2760246-90-8
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PROTAC SMARCA2 degrader-22 (Compound 5) is a PROTAC degrader for SMARCA2 with a degradation efficacy of 94% at 100 nM. PROTAC SMARCA2 degrader-22 inhibits the proliferation of cell A549 with an EC50 < 250 nM .
Cat. No.: HY-160263S
CAS No.: 2408740-75-8
Cat. No.: HY-152512
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RLA-4842 is an iron activator containing anti-androgen. RLA-4842 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line .
Cat. No.: HY-173640
CAS No.: 2785317-21-5
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ID11916 is an orally active androgen receptor (AR) antagonist and a phosphodiesterase 5 (PDE5) inhibitor. ID11916 blocks androgen binding to AR, nuclear translocation, and androgen-dependent transcriptional activity of AR, while increasing intracellular cGMP levels and activating PKG via inhibition. ID11916 shows potent anti-cancer effect in prostate cancer cell lines VCaP and 22Rv1 and in AR-positive breast cancer cell lines SK-BR-3 .
Cat. No.: HY-152520
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RLA-5331 is an iron activator containing anti-androgen. RLA-5331 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line .
Cat. No.: HY-155666
CAS No.: 2952994-34-0
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YXG‑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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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
