Belinostat (PXD101)
Catalog #
27608-1
$145
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Description
Belinostat, also known as PXD101, is a novel and potent hydroxamate-type HDAC inhibitor.
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Synonyms
PXD-101, PXD 101, PX105684, PX-105684, (E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide
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Product Data Gallery
Product Info
Storage and Usage
Citations
Purity
≥98% by HPLC
Target(s)
HDAC
Formula
C15H14N2O4S
MW
318.4 Da
Solubility
Soluble in DMSO
Biological Activity
Belinostat (also known as PXD101) is a novel and potent hydroxamate-type inhibitor of histone deacetylase (HDAC) that inhibits the activity of HDAC in Hela cell extracts with IC50 value of 27 nM. In the treatment of urothelial carcinoma cell lines, belinostat dose-dependently inhibits proliferation in 5637, T24, J82 and RT4 cells with IC50 values of 1.0 µM, 3.5 µM, 6.0 µM and 10 µM respectively; while, in prostate cancer cell lines, it inhibits cancer cell growth with IC50 values ranging from 0.5 to 2.5 µM.
CAS Registry #
414864-00-9
Background
Belinostat has been found to significantly increase the acetylation of histones H3 and H4 and exerts cytotoxicity in a wide range of tumor cell lines.
References
1. Buckley,MT, et al. J. Transl. Med. 2007; 5:49.
2. Gravina, GL et al. Int. J. Oncol. 40: 711-720, 2012.
3. Plumb JA, et al. Mol Cancer Ther. 2003 Aug;2(8):721-8.
2. Gravina, GL et al. Int. J. Oncol. 40: 711-720, 2012.
3. Plumb JA, et al. Mol Cancer Ther. 2003 Aug;2(8):721-8.