4-iodo-SAHA (Synonyms: ISAHA) |
رقم الكتالوجGC17005 |
4-Iodo-SAHA (1k) عبارة عن مثبط نشط عن طريق الفم من الفئة الأولى والفئة الثانية من مثبطات هيستون ديستيلاز (HDAC) مع EC50s 1.1 و 0.95 و 0.12 و 0.24 و 0.85 و 1.3 ميكرومتر لخطوط الخلايا Skbr3 و HT29 و U937 و JA16 و HL60 ، على التوالى. يمكن استخدام 4-Iodo-SAHA (1 ك) لأبحاث السرطان
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1219807-87-0
Sample solution is provided at 25 µL, 10mM.
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].
Reference:
[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.
Average Rating: 5
(Based on Reviews and 11 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *