JNJ-26481585
Catalog #
27632-1
$235
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Description
JNJ-26481585, also known as Quisinostat, is a potent pan-HDAC inhibitor. JNJ-26481585 induces histone acetylationand inhibits cancer cell proliferation.
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Synonyms
Quisinostat; N-hydroxy-2-[4-[[(1-methylindol-3-yl)methylamino]methyl]piperidin-1-yl]pyrimidine-5-carboxamide
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Product Data Gallery
Product Info
Storage and Usage
Citations
Purity
≥98% by HPLC
Target(s)
HDAC
Formula
C21H26N6O2
MW
394.5 Da
Solubility
Soluble in DMSO
Biological Activity
JNJ-26481585 inhibits HDAC1, HDAC2, HDAC4, HDAC10, and HDAC11 with IC50 values of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM, and 0.37 nM, respectively.
CAS Registry #
875320-29-9
Background
Quisinostat, also known asJNJ-26481585, is an orally bioavailable, second-generation, hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor JNJ-26481585 inhibits HDAC leading to an accumulation of highly acetylated histones, which may result in an induction of chromatin remodeling; inhibition of the transcription of tumor suppressor genes; inhibition of tumor cell division; and the induction of tumor cell apoptosis. HDAC, an enzyme upregulated in many tumor types, deacetylates chromatin histone proteins. Compared to some first generation HDAC inhibitors, JNJ-26481585 may induce superior HSP70 upregulation and bcl-2 downregulation.
References
Rajak, H., et al. Curr Med Chem. 2014;21(23):2642-64.
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