4-Iodo-SAHA (1k) 是一种具有口服活性的I类和II类histone deacetylase (HDAC)抑制剂,对 Skbr3、 HT29、 U937、 JA16 和 HL60细胞的EC50值分别为1.1、0.95、0.12、0.24、0.85和1.3 μM。4-Iodo-SAHA (1k) 可用于癌症的研究。
产品描述
4-Iodo-SAHA (1k) is an orally active class I and class II histone deacetylase (HDAC) inhibitor with EC 50 s of 1.1, 0.95, 0.12, 0.24, 0.85 and 1.3 μM for Skbr3, HT29, U937, JA16 and HL60 cell lines, respectively. 4-Iodo-SAHA (1k) is able to be used for the research of cancer [1].
体外活性
4-Iodo-SAHA (1k) (0.1-100 μM; 48 h ) inhibits Skbr3, HT29, U937, JA16 and HL60 cell lines [1]. In SKBR3 cells, 4-Iodo-SAHA (1k) (2 μM; 6-24 h ) also affects acetylated H4 and p21 levels [1]. Cell Proliferation Assay [1] Cell Line: SKBR3, HT29, U937, JA16 and HL60 cell lines Concentration: 0.1-100 μM Incubation Time: 48 h Result: Inhibited SKBR3, HT29, U937, JA16 and HL60 cell lines with EC 50 s of 1.1, 0.95, 0.12, 0.24, 0.85 and 1.3 μM, respectively. Showed 10-fold potent as an inhibitor of U937 cell line compared to SAHA. Western Blot Analysis [1] Cell Line: SKBR3-breast-derived cell line Concentration: 2 μM Incubation Time: 6, 12 and 24 h Result: Time-dependently up regulated histone H4 acetylation and p21/WAF1 cell cycle inhibitor accumulation in SKBR3 cells.
体内活性
4-Iodo-SAHA (1k) (50 mg/kg; p.o. five times a week for two weeks) has similar toxicity compared to SAHA-treated and control mice [1]. Animal Model: 8-week-old fvb mice [1] Dosage: 50 mg/kg Administration: Oral gavage; 50 mg/kg five times per week; for 2 weeks Result: Compared to both SAHA-treated and control mice with similar body weights and hematological counts.
Cas No.
1219807-87-0
分子式
C14H19IN2O3
分子量
390.22
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years