Ricolinostat

SKU: orb1305408

Description

Ricolinostat

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 1316214-52-4
• MW: 433.5
• Purity: 99.57% (May vary between batches)
• Formula: C₂₄H₂₇N₅O₃
• SMILES: ONC(=O)CCCCCCNC(=O)c1cnc(nc1)N(c1ccccc1)c1ccccc1
• Target: Apoptosis|||HDAC
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.61 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:127.5 mg/mL (294.12 mM)

Bioactivity

• Target IC50:
  HDAC3:51 nM|HDAC6:4.7 nM|HDAC8:100 nM|HDAC2:48 nM|HDAC4:7000 nM|HDAC1:58 nM|HDAC5:5000 nM|HDAC7:1400 nM
• In Vivo:
  ACY-1215, at very low dosages, significantly induces acetylation of α-tubulin while at higher dosages, it leads to the acetylation of lysine residues on histone proteins H3 and H4. ACY-1215 demonstrates slight activity against HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1, and Sirtuin2, with an IC50 of 0.1 μM specifically for HDAC8.
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• In Vitro:
  ACY-1215 is readily absorbed by tumor tissues and does not accumulate within them in both multiple myeloma models and diffuse MM models, effectively inhibiting tumor growth.
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• Cell Research:
  ACY-1215 is dissolved in DMSO (10 mM) and stored, and then in diluted with appropriate culture medium before use. 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ricolinostat, Rocilinostat, Apoptosis, ACY 1215, ACY1215, ACY-1215, Histone deacetylases, Inhibitor, HDAC, HDAC1, HDAC3, HDAC2, HDAC6, HDAC8, inhibit

Compound Identifiers

PubChem CID

53340666