2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. Androgen receptor antagonist-14

Androgen receptor antagonist-14 (Compound S-94) is a selective antagonist of the T878A mutant androgen receptor (AR) with an IC50 of 0.38 μM. Androgen receptor antagonist-14 selectively antagonizes the transcriptional activity of the ART878A, ARF877L/T878A and ARH875Y/T878A mutant androgen receptors. Androgen receptor antagonist-14 exhibits anticancer activity against prostate cancer. Androgen receptor antagonist-14 can be used in the research of prostate cancer.

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Androgen receptor antagonist-14

Androgen receptor antagonist-14 Chemical Structure

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Androgen receptor antagonist-14 Related Antibodies

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Description

Androgen receptor antagonist-14 (Compound S-94) is a selective antagonist of the T878A mutant androgen receptor (AR) with an IC50 of 0.38 μM. Androgen receptor antagonist-14 selectively antagonizes the transcriptional activity of the ART878A, ARF877L/T878A and ARH875Y/T878A mutant androgen receptors. Androgen receptor antagonist-14 exhibits anticancer activity against prostate cancer. Androgen receptor antagonist-14 can be used in the research of prostate cancer[1].

IC50 & Target[1]

ART878A

0.38 μM (IC50)

In Vitro

Androgen receptor antagonist-14 potently inhibits the transcriptional activity of T878A-mutated AR in LNCaP-ARR2PB-eGFP cells, with an IC50 of 0.38 μM[1].
Androgen receptor antagonist-14 (0.1-10 μM; 48 h) dose-dependently reduces the expression of DHT-induced AR target genes PSA, UBE2C and KLK2 in LNCaP cells without altering AR mRNA levels[1].
Androgen receptor antagonist-14 (0.1-10 μM; 48 h) dose-dependently reduces PSA protein levels in LNCaP cells without altering AR protein levels[1].
Androgen receptor antagonist-14 (3 days) selectively inhibits the proliferation of LNCaP cells with an IC50 of 10.32 μM, while it exhibits only extremely low cytotoxicity against other prostate cancer cell lines and non-cancerous cell lines[1].
Androgen receptor antagonist-14 (10 μM; 24 h) induces G1-phase cell cycle arrest in LNCaP cells and reduces the mRNA expression of key cell cycle regulators Cyclin A, CDC20 and CDK1[1].
Androgen receptor antagonist-14 (4 h) exhibits weak binding affinity for the ligand-binding pocket of wild-type AR, with an IC50 value of 85.60 μM[1].
Androgen receptor antagonist-14 potently and selectively inhibits the transcriptional activity of DHT-induced T878A mutant AR in HEK293T cells (IC50 = 0.49 μM), while its activity against wild-type AR is over 50-fold lower (IC50 = 27.18 μM)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Androgen receptor antagonist-14 Related Antibodies

Real Time qPCR[1]

Cell Line: LNCaP (harboring endogenous T878A-mutant AR)
Concentration: 0.1-10 μM
Incubation Time: 48 h
Result: Reduced DHT-induced transcriptional activation of the AR downstream target genes PSA, UBE2C, and KLK2 in a dose-dependent fashion.
Did not affect mRNA expression of AR itself.

Western Blot Analysis[1]

Cell Line: LNCaP (harboring endogenous T878A-mutant AR)
Concentration: 0.1-10 μM
Incubation Time: 48 h
Result: Decreased endogenous PSA protein levels in a dose-dependent manner.
Caused no significant alteration in AR protein levels.

Cell Proliferation Assay[1]

Cell Line: LNCaP, C4-2B, PC3, WPMY-1, NIH-3T3, DU145, GES-1, Chang, 22RV1
Concentration: Gradient concentrations
Incubation Time: 3 days
Result: Inhibited proliferation of LNCaP cells with an IC50 of 10.32 μM.
Exhibited minimal inhibitory effects on C4-2B, 22RV1, DU145, and PC3 prostate cancer cell lines.
Showed minimal cytotoxicity in non-cancerous WPMY-1, GES-1, Chang, and NIH-3T3 cell lines.

Cell Cycle Analysis[1]

Cell Line: LNCaP (harboring endogenous T878A-mutant AR)
Concentration: 10 μM (cell cycle assay); 0.1-10 μM (qPCR)
Incubation Time: 24 h (cell cycle assay); 48 h (qPCR)
Result: Decreased the S phase population and increased the G1 phase population in LNCaP cells compared to DMSO control.
Significantly reduced mRNA levels of the cell cycle regulators Cyclin A, CDC20, and CDK1.
In Vivo

Androgen receptor antagonist-14 (20-40 mg/kg; i.g., i.p.; daily; 26 days) administered at 20 mg/kg i.p. daily for 26 days significantly suppresses tumor growth in a BALB/c nude mouse LNCaP xenograft model, with reduced tumor cell proliferation and PSA expression, and no observed systemic toxicity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude (male, 3-4 weeks old, subcutaneous flank injection of LNCaP-FGC cells harboring T878A-mutant AR)[1]
Dosage: 40 mg/kg; 20 mg/kg
Administration: i.g.; daily; 26 days; i.p.; daily; 26 days
Result: Suppressed LNCaP tumor growth relative to vehicle control.
Significantly reduced tumor weight compared to vehicle at 20 mg/kg i.p. dose.
Decreased Ki67-positive staining (lower tumor cell proliferation) at 20 mg/kg i.p. dose.
Significantly decreased PSA protein levels in tumor tissues at 20 mg/kg i.p. dose.
Caused no significant weight loss or signs of toxicity throughout the study.
Molecular Weight

427.50

Formula

C26H25N3O3
SMILES

CC1=CC(NC([C@H](CC2=CNC3=C2C=CC=C3)NC(OC4=CC=CC=C4)=O)=O)=CC(C)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Androgen receptor antagonist-14 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Androgen receptor antagonist-14Androgen receptor antagonist14Androgen receptor antagonist 14Androgen ReceptorHEK293T cellsPSALNCaP-ARR2PB-eGFP cellsLNCaP cellsmineralocorticoid receptorsT878A-mutant androgen receptorglucocorticoid receptorsUBE2CKLK2progesterone receptorsInhibitorinhibitorinhibit

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