A selective inhibitor of HDAC6 (IC50 = 5 nM); suppresses tumor growth and increases survival in mice with multiple myeloma and mantle cell lymphoma xenografts when combined with proteasome inhibitors

ACY-1215 – 100 mg

Brand:
Cayman
CAS:
1316214-52-4
Storage:
-20
UN-No:
De Minimis - 3077 / 9

ACY-1215 is an inhibitor of histone deacetylase 6 (HDAC6; IC50 = 5 nM).{33843} It is at least 10-fold less active against other HDACs in enzymatic assays. ACY-1215 shows synergistic activity with the proteasome inhibitor bortezomib (Item No. 10008822) against multiple myeloma (MM) cells, inducing protracted endoplasmic reticulum stress and apoptosis.{33843,33840} ACY-1215 combined with proteasome inhibitors suppresses tumor growth and increases survival in mice with MM and mantle cell lymphoma xenografts.{33840,33843,33842} A multicenter phase I trial examining ACY-1215 combined with the E3 ligase inhibitor lenalidomide (Item No. 14643) and dexamethasone (Item No. 11015) in multiple myeloma found inhibition of HDAC6 in vivo.{33845} ACY-1215 also diminishes liver cyst development and fibrosis in a rat model of polycystic liver disease.{33841}  

 

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Description

A selective inhibitor of HDAC6 (IC50 = 5 nM); suppresses tumor growth and increases survival in mice with multiple myeloma and mantle cell lymphoma xenografts when combined with proteasome inhibitors

Formal name: 2-(diphenylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]-5-pyrimidinecarboxamide

Synonyms:  ACY-63|Ricolinostat|Rocilinostat

Molecular weight: 433.5

CAS: 1316214-52-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Deacetylases||Research Area|Epigenetics, Transcription, & Translation|Erasers|Histone Deacetylation

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