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Ricolinostat

Catalog No. T2489   CAS 1316214-52-4
Synonyms: ACY-1215, Rocilinostat

Ricolinostat (Rocilinostat) is an orally bioavailable, specific inhibitor of histone deacetylase 6 (HDAC6) with potential antineoplastic activity.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Ricolinostat Chemical Structure
Ricolinostat, CAS 1316214-52-4
Pack Size Availability Price/USD Quantity
5 mg In stock $ 43.00
10 mg In stock $ 61.00
50 mg In stock $ 79.00
100 mg In stock $ 116.00
1 mL * 10 mM (in DMSO) In stock $ 48.00
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Purity: 99.57%
Purity: 99.57%
Purity: 99.21%
Purity: 98.90%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Ricolinostat (Rocilinostat) is an orally bioavailable, specific inhibitor of histone deacetylase 6 (HDAC6) with potential antineoplastic activity.
Targets&IC50 HDAC6:4.7 nM, HDAC8:100 nM, HDAC1:58 nM, HDAC3:51 nM, HDAC2:48 nM
Kinase Assay ACY-1215 is dissolved and subsequently diluted in assay buffer [50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA, and 20 μM tris(2-carboxyethyl)phosphine] to 6-fold the final concentration. HDAC enzymes are diluted to 1.5-fold of the final concentration in assay buffer and pre-incubated with ACY-1215 for 10 minutes before the addition of the substrate. The amount of FTS (HDAC1, HDAC2, HDAC3, and HDAC6) or MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9) used for each enzyme is equal to the Michaelis constant (Km), as determined by a titration curve. FTS or MAZ-1675 is diluted in assay buffer to 6-fold the final concentration with 0.3 μM sequencing grade trypsin. The substrate/trypsin mix is added to the enzyme/compound mix and the plate is shaken for 60 seconds and then placed into a SpectraMax M5 microtiter plate reader. The enzymatic reaction is monitored for release of 7-amino-4-methoxy-coumarin over 30 minutes, after deacetylation of the lysine side chain in the peptide substrate, and the linear rate of the reaction is calculated[1].
Cell Research ACY-1215 is dissolved in DMSO (10 mM) and stored, and then in diluted with appropriate culture medium before use[1]. The effect of ACY-1215 with or without Bortezomib on the viability of MM cell lines, patient MM cells, and PBMCs is assessed by measuring MTT dye absorbance. PBMCs from healthy donors are isolated and stimulated with 2.5 μg/mL of phytohemagglutinin (PHA) for 48 hours in the presence of increasing concentrations of ACY-1215. DNA synthesis is measured by tritiated thymidine uptake. CD4+ T cells are purified from human blood with the Rosette Sep negative-selection kit. Cells are stimulated by CD3/CD28 Dynabeads for 7 days in the presence of compounds. Cell viability is assessed using alamarBlue. MM cells (2-3×104 cells/well) are incubated in 96-well culture plates with medium and different concentrations of ACY-1215, Bortezomib, and/or recombinant IL-6 (10 ng/mL) or insulin-like growth factor-1 (IGF-1; 50 ng/mL) for 24 hours at 37°C, and tritiated thymidine incorporation is measured[1].
Synonyms ACY-1215, Rocilinostat
Molecular Weight 433.5
Formula C24H27N5O3
CAS No. 1316214-52-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 80 mg/mL (184.5 mM)

TargetMolReferences and Literature

1. Santo L, et al. Blood, 2012, 119(11), 2579-2589.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Target-Focused Phenotypic Screening Library NF-κB Signaling Compound Library Human Metabolite Library Anti-Cancer Compound Library ReFRAME Related Library Drug Repurposing Compound Library Inhibitor Library

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Keywords

Ricolinostat 1316214-52-4 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair HDAC inhibit ACY 1215 ACY1215 Inhibitor ACY-1215 Histone deacetylases Rocilinostat inhibitor

 

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