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).
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.