Vorinostat (SAHA) 是一种有效的，可口服的 HDAC1，HDAC2，HDAC3 (Class I)，HDAC7 (Class II) 和 Class IV (HDAC11) 的抑制剂，对 HDAC1/3 的 ID50 值分别为 10 nM 和 20 nM。Vorinostat 可以诱导细胞凋亡 (apoptosis)。Vorinostat 还是一种人类乳头瘤病毒 (HPV)-18 DNA 扩增的有效抑制剂。
| CAS No. | 149647-78-9 |
| 生物活性 | Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis. Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification. |
| 分子式 | C14H20N2O3 |
| 分子量 | 264.32 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | Powder -20°C 3 years |
| 溶解性数据 | DMSO : ≥ 100 mg/mL (378.33 mM) |
| 体内研究 | Vorinostat (50 mg/kg/day) reduces tumor growth by more than 50% in nude mice injected with 5×10 MES-SA cells. |
| 体外研究 | Vorinostat efficiently suppresses MES-SA cell growth at a low dosage (3 μM) already after 24 hours treatment. HDACs class I (HDAC2 and 3) as well as class II (HDAC7) are preferentially affected by this treatment. Vorinostat significantly increases p21 expression and apoptosis in MES-SA cells. Vorinostat inhibits SK-N-SH and SK-N-Be(2)C with the IC25 values of 1 µM and 0.5 µM, respectively. Vorinostat is an effective inhibitor of HPV-18 DNA amplification, reduces oncoproteins E6 and E7 activities and triggers apoptosis in HPV-infected, differentiated cells. |
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