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1219807-87-0

1219807-87-0 Structure

1219807-87-0 Structure
IdentificationBack Directory
[Name]

4-Iodo Suberoylanilide HydroxaMic Acid
[CAS]

1219807-87-0
[Synonyms]

4-iodo-SAHA
4-Iodo Suberoylanilide HydroxaMic Acid
N1-Hydroxy-N8-(4-iodophenyl)octanediaMide
[Molecular Formula]

C14H19IN2O3
[MOL File]

1219807-87-0.mol
[Molecular Weight]

390.22
Chemical PropertiesBack Directory
[density ]

1.579±0.06 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

insoluble in H2O; insoluble in EtOH; ≥1.67 mg/mL in DMSO
[form ]

A crystalline solid
[pka]

9.48±0.20(Predicted)
Hazard InformationBack Directory
[Uses]

A SAHA derivative with antiproliferative activity in several human cancer cell lines.
[Uses]

A SAHA derivative with antiproliferative activity in several human cancer cell lines. Antitumor agent.
[Biological Activity]

4-iodo-saha is a hydrophobic derivative of saha, the class i and class ii histone deacetylase (hdac) inhibitor [1].the reversible acetylation of lysine residues in histone plays an important role in transcriptional activation and repression. the regulation of these post-translational modifications is balanced by histone acetyltransferase (hat) and histone deacetylase (hdac) activities. hdacs are also involved in reversible acetylation of non-histone proteins [1].4-iodo-saha is a histone deacetylase (hdac) inhibitor. in skbr3-breast-derived cell line, 4-iodo-saha inhibited cell proliferation with ec50 value of 1.1 μm. in ht29 colon-derived cell line, leukemia-derived u937 tumor cell line, ja16, hl60 and k562 cell lines, 4-iodo-saha inhibited cell proliferation with ec50 values of 0.95, 0.12, 0.24, 0.85 and 1.3 μm, respectively. 4-iodo-saha is 10-fold more potent as an inhibitor of u937 leukemia cell proliferation compared to saha (0.12 μm versus 1.2 μm). in skbr3 cells, 4-iodo-saha reduced acetylated h4 and p21 levels [1].
[in vivo]

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[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.
[storage]

Store at -20°C
[References]

[1]. salmi-smail c, fabre a, dequiedt f, et al. modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. j med chem. 2010 apr 22;53(8):3038-47.
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