SKLB-23bb
规格
Cas Number | 1815580-06-3 |
规格或纯度 | ≥97% |
纯度 | ≥97% |
包装 | 10mg 或 1mg 或 5mg 或 25mg 或 2mg |
产品信息
品牌 | 阿拉丁 |
溶解性 | Solubility (25°C) In vitro DMSO: 79 mg/mL (199.27 mM); Ethanol: 79 mg/mL (199.27 mM); Water: Insoluble; |
简短描述 | HDAC6 选择性抑制剂 |
英文简短描述 | HDAC6 Selective Inhibitors |
过滤标签 | 表观遗传学,HDAC,Cell Cycle/DNA Damage |
储存温度 | -20°C储存 |
运输条件 | 超低温冰袋运输 |
生化和生理学机理 | SKLB-23bb 是一种可口服的 HDAC6 选择性抑制剂,对大多数细胞株的 IC50 值低于 100 nmol/L。它还具有破坏微管的能力。 |
描述 |
SKLB-23bb 是一种有效的选择性 HDAC6 抑制剂,IC50 为 17 nM,比抑制 HDAC1 (IC50= 422 nM) 和 HDAC8 (IC50=3398 nM) 选择性分别高 25 倍和 200 倍。 |
英文描述 |
Product description: SKLB-23bb is a potent and selective inhibitor for HDAC6 with an IC50 of 17 nM and shows 25-fold and 200-fold selectivity relative to HDAC1 (IC50=422 nM) and HDAC8 (IC50=3398 nM), respectively. Information SKLB-23bb is an orally bioavailableHDAC6-selectiveinhibitor with IC50 values under 100 nmol/L, against most of the cell lines checked. It also has microtubule-disrupting ability. Targets HDAC6 (Cell-based assay) <100 nM In vitro SKLB-23bb shows cytotoxic effects against a panel of solid and hematologic tumor cell lines at the low submicromolar level. In contrast to the reported HDAC6-selective inhibitors, SKLB-23bb is more efficient against solid tumor cells. SKLB-23bb selectively inhibits cellular HDAC6, but the antitumor activity of SKLB-23bb is independent of HDAC6. SKLB-23bb could bind to the colchicine site in β-tubulin and act as a microtubule polymerization inhibitor. It blocks tumor cell cycle at G2-M phase and triggers cellular apoptosis. In vivo In solid tumor xenografts, oral administration of SKLB-23bb efficiently inhibits tumor growth. SKLB-23bb has good pharmacokinetic profiles and is orally bioavailable. Cell Research(from reference) Cell lines:HCT116 and A2780S cells Concentrations:200 nM Incubation Time:3, 6, 12 and 24 h |