4-iodo-SAHA (Synonyms:4-碘辛二酰苯胺氧肟酸;ISAHA)
目录号 : KCM10719 CAS No. : 1219807-87-0 纯度 : ≥98%
4-iodo-SAHA is a hydrophobic derivative of the class I and class II histone deacetylase (HDAC) inhibitor SAHA. At 1 μM it demonstrates >60% inhibition of HDAC1 and HDAC6 activity in a deacetylase activity assay, similar to that of SAHA. 4-iodo-SAHA inhibits proliferation of SK-BR-3 breast-derived and HT29 colon-derived cell lines with EC values comparable to that of SAHA (1.1 and 0.95 μM versus 2.1 and 2 μM, respectively). It is 10-fold more potent as an inhibitor of U937 leukemia cell proliferation compared to SAHA (0.12 μM versus 1.2 μM, respectively).
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生物活性

4-Iodo-SAHA (1k) is an orally active class I and class II histone deacetylase (HDAC) inhibitor with EC50s 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) can be used for the research of cancer.

体外研究

4-Iodo-SAHA (0.1-100 μM; 48 h) inhibits Skbr3, HT29, U937, JA16 and HL60 cell lines. . 4-Iodo-SAHA (2 μM; 6-24 h) affects acetylated H4 and p21 levels in SKBR3 cells.

 

Cell Proliferation Assay

Cell Line: SKBR3, HT29, U937, JA16 and HL60 cell lines
Concentration: 0.1-100 μM
Incubation Time: 48 hours
Result: Inhibited SKBR3, HT29, U937, JA16 and HL60 cell lines with EC50s 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

Cell Line: SKBR3-breast-derived cell line
Concentration: 2 μM
Incubation Time: 6, 12 and 24 hours
Result: Time-dependently up regulated histone H4 acetylation and p21/WAF1 cell cycle inhibitor accumulation in SKBR3 cells.
体内研究

4-Iodo-SAHA (1k) (50 mg/kg; p.o. five times a week for two weeks) compares to SAHA-treated and control mice with similar toxicity.

 

Animal Model: 8-week-old fvb mice
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.
 
分子式
C14H19In2O3
分子量
390.2
CAS号
1219807-87-0
中文名称
4-碘辛二酰苯胺氧肟酸
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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工作液浓度 mg/ml;

DMSO母液配制方法 mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,

体内配方配制方法μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。

配置后的溶液总体积

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