ACY-1215 is an orally bioavailable, specific inhibitor of histone deacetylase 6 (HDAC6) with potential antineoplastic activity. ACY-1215 selectively targets and binds to HDAC6, thereby disrupting the Hsp90 protein chaperone system through
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Histone deacetylase 6 inhibitor
Product Description
Rocilinostat (ACY-1215) is a selective HDAC6 inhibitor with IC50 of 5 nM. It is >10-fold more selective for HDAC6 than HDAC1/2/3 (class I HDACs) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2.
1.Santo L, Hideshima T, Kung AL, Tseng JC, Tamang D, Yang M, Jarpe M, van Duzer JH, Mazitschek R, Ogier WC et al.. (2012) Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma.. Blood, 119 (11):(2579-89). [PMID:22262760]
2.Kalin JH, Bergman JA. (2013) Development and therapeutic implications of selective histone deacetylase 6 inhibitors.. J Med Chem, 56 (16):(6297-313). [PMID:23627282]
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H2322089