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Chemical Structure : SBI-46
Catalog No.: PC-20402Not For Human Use, Lab Use Only.
SBI-46 (SBI 46) is an antiandrogen-equipped histone deacetylase (HDAC) inhibitor, strongly binds to androgen receptor (AR, IC50=8.4 nM) and potently inhibited HDACs and the proliferation of AR+ CRPC.
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SBI-46 (SBI 46) is an antiandrogen-equipped histone deacetylase (HDAC) inhibitor, strongly binds to androgen receptor (AR, IC50=8.4 nM) and potently inhibited HDACs and the proliferation of AR+ CRPC.
SBI-46 showed much tighter affinity than enzalutamide (MDV-3100, Cat# PC-45932).
SBI-46 possessed potent anti-HDAC activity against HDAC1 and HDAC6 with IC50 of 66 and 15 nM, respectively, much less potent against HDAC8 (IC50=3,500 nM).
SBI-46 potently inhibited cell growth of AR+ (LNCaP IC50=500 nM), and AR+ splice variants (AR-SV) and CRPC cells (C4-2B-IC50=480 nM and 22Rv1 IC50=560 nM), without effects against AR-null PC-3 cells.
SBI-46 caused a dose-dependent upregulation of acetylated H4 and tubulin in LNCaP cells.
SBI-46 inhibited cytoplasmic and nuclear expressions of AR and AR-V, downregulated DHT-induced AR expression in CRPC cells.
SBI-46 (20 mg/kg, orally, five days/week for four weeks) potently suppressed PCa xenografts tumor growth in nude mice.
| M.Wt | 629.62 | |
| Formula | C30H31F4N7O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Chandrasekaran B, et al. Cancers (Basel). 2023 Mar 15;15(6):1769.
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