Androgen receptor allosteric antagonist 1
CAS No. : 927819-39-4
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| Cat. No. : | HY-121094 |
| M.Wt: | 336.43 |
| Formula: | C21H24N2O2 |
| Purity: | >98 % |
| Solubility: |
Androgen receptor allosteric antagonist 1(compound D36)is a a llosteric, competitive androgen receptor (AR) antagonist with the Ki of 9 μM. Androgen receptor allosteric antagonist 1 inhibits R1881-mediated transcription and proliferation and can be used for study of prostate cancer[1].
In Vitro:D36 (30 μM; 48 h) disrupts the AR/gelsolin interaction in a mammalian two-hybrid screening assay in HepG2 cells and inhibits R1881-induced AR transcriptional activation in an MMTV-luciferase reporter assay in LNCaP cells[1].
D36 (5-30 μM; 48 h) allosterically inhibits AR activity in an MMTV-luciferase reporter dose-response assay in LNCaP cells, decreasing Vmax and slightly increasing EC50 (<3-fold), with a calculated Ki of 9.0 μM[1].
D36 (1-40 μM; 24 h) dose-dependently inhibits R1881 (500 pM)-induced PSA mRNA expression in a qPCR assay in LAPC4 cells and suppresses the expression of multiple endogenous AR target genes in LNCaP cells[1].
D36 (1 nM-100 μM; 7 days) inhibits both basal and androgen-stimulated proliferation in cell proliferation assays in LAPC4, LNCaP (SR/SRAR), and VCaP cells; it retains full antagonist activity in AR-overexpressing hormone-refractory models (SRAR LNCaP, VCaP), with DNA content not reduced below baseline levels, indicating no cytotoxicity[1].
D36 (20-30 μM; 24 h) causes only a modest reduction in AR protein levels (normalized to GAPDH) in Western blot assays in LAPC4 and LNCaP cells[1].
D36 (30 μM; 4 h) does not induce AR nuclear translocation in a nuclear-cytoplasmic fractionation assay in SRAR LNCaP cells (unlike R1881, OHF, and Csx), and inhibits the recruitment of AR and cofactors (Pol II, p300, SRC1, TRAP220) to the PSA enhancer in a ChIP assay[1].
D36 (20-150 μM; SPR injection) directly binds to full-length AR saturated with R1881 in a surface plasmon resonance assay, with Kd=90 μM, kon=135 M-1s-11, and koff=0.012 s-1[1].
D36 (near IC50 concentration) effectively competes with R1881 for AR binding in a 3H-R1881 whole-cell competition binding assay in VCaP cells[1].
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