1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC
  3. Ricolinostat

Ricolinostat (Synonyms: ACY-1215; Rocilinostat)

Cat. No.: HY-16026 Purity: 99.70%
Handling Instructions

Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor, with an IC50 of 5 nM. ACY-1215 also inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively.

For research use only. We do not sell to patients.

Ricolinostat Chemical Structure

Ricolinostat Chemical Structure

CAS No. : 1316214-52-4

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 70 In-stock
Estimated Time of Arrival: December 31
50 mg USD 90 In-stock
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100 mg USD 130 In-stock
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Customer Review

Based on 15 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Ricolinostat purchased from MCE. Usage Cited in: Med Oncol. 2016 May;33(5):50.

    H460 cells are treated with 0.5 μM Aorafenib and indicated concentration of HDAC6 inhibitors, CAY10603 (CAY, 0.05 μM) or ACY1215 (ACY,1 μM). The cleavage of PARP and caspase 3 also increased after cotreatment.

    Ricolinostat purchased from MCE. Usage Cited in: Cancer Lett. 2016 Aug 28;379(1):134-142.

    Inhibition of HDAC6 by HDAC6-selective inhibitors impairs the proliferation of glioblastoma cells. U87 and U251 cells are treated with HDAC6 selective inhibitors and the cells are harvested for subsequent western blot analysis.

    Ricolinostat purchased from MCE. Usage Cited in: Oncol Rep. 2017 Feb;37(2):1270-1276.

    A375 cells are treated with indicated concentrations of ACY-1215. After 72 h, Western blotting assay are utilized to detect apoptosis.

    Ricolinostat purchased from MCE. Usage Cited in: Oncogene. 2018 Nov;37(45):5952-5966.

    Mouse CAFs are treated with increasing concentrations of ACY1215 for 24 h. Western blot analysis of tubulin, histone H3, histone H4, acetylated tubulin, acetylated histone H3, and acetylated histone H4.

    Ricolinostat purchased from MCE. Usage Cited in: Biomed Pharmacother. 2019 Jan;109:2464-2471.

    The expression of IL-1β and IL-6 in human primary chondrocytes and C28/I2 cells is tested by western blot analysis with the treatment of IL-1β, DMSO and ACY-1215.

    Ricolinostat purchased from MCE. Usage Cited in: Biomed Pharmacother. 2019 Jan;109:2464-2471.

    The expression of MMP-1, MMP-13 and COL2 A1 in C28/I2 cells is tested by western blot analysis with the treatment of IL-1β, DMSO and ACY-1215.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor, with an IC50 of 5 nM. ACY-1215 also inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively.

    IC50 & Target

    HDAC6

    4.7 nM (IC50)

    HDAC2

    48 nM (IC50)

    HDAC3

    51 nM (IC50)

    HDAC1

    58 nM (IC50)

    HDAC8

    100 nM (IC50)

    HDAC7

    1400 nM (IC50)

    HDAC5

    5000 nM (IC50)

    HDAC4

    7000 nM (IC50)

    In Vitro

    Ricolinostat (ACY-1215) has slight activity against HDAC8 (IC50=0.1 μM), and has minimal activity (IC50>1 μM) against HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1, and Sirtuin2. The effect of Ricolinostat (ACY-1215) on multiple myeloma (MM) cell viability is determined with MTT assays using MM cell lines. Exposure of MM cell lines for 48 hours results in dose-dependent decreased viability, with IC50 values ranging from 2-8μM. Ricolinostat (ACY-1215) demonstrates significant activity in the MM Bortezomib-resistant cell line (ANBL-6.BR), demonstrating the ability of Ricolinostat (ACY-1215) to overcome Bortezomib resistance[1].

    In Vivo

    Mice treated with Ricolinostat (ACY-1215), Bortezomib, or Ricolinostat plus Bortezomib show a significant delay in tumor growth (P=0.01, P=0.006, and P<0.0001, respectively). Combined treatment with Ricolinostat and Bortezomib shows significant suppression of tumor growth and significantly prolonged overall survival (OS) compare with the control group (17 days in the control vs 40 days in the combination-treated group, P<0.0001) and the Ricolinostat (ACY-1215)-treated group (22 days in the Bortezomib group vs 40 days in the combination-treated group, P<0.0001). Weight loss in the combination-treated group is between 4% and 12% compare with the same-day control group values during treatment, with complete recovery after the last injection. As is observed in the plasmacytoma model, a significant therapeutic advantage is found by combining Ricolinostat with Bortezomib compare with either agent alone[1].

    Clinical Trial
    Molecular Weight

    433.50

    Formula

    C₂₄H₂₇N₅O₃

    CAS No.

    1316214-52-4

    SMILES

    O=C(C1=CN=C(N(C2=CC=CC=C2)C3=CC=CC=C3)N=C1)NCCCCCCC(NO)=O

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (115.34 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3068 mL 11.5340 mL 23.0681 mL
    5 mM 0.4614 mL 2.3068 mL 4.6136 mL
    10 mM 0.2307 mL 1.1534 mL 2.3068 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    The effect of Ricolinostat 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 Ricolinostat (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 Ricolinostat (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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Mice[1]
    To evaluate the in vivo anti-MM activity of Ricolinostat, male SCID mice are inoculated subcutaneously with 5×106 MM.1S cells in 100 μL of serum-free RPMI 1640 medium. When tumors are measurable, mice are treated IP with Ricolinostat 50 mg/kg dissolved in 10% DMSO in 5% dextrose in water consecutively for 5 days a week for 3 weeks; Bortezomib 0.5 mg/kg dissolved in 0.9% saline solution biweekly (IV) for 3 consecutive weeks; or combination with the same dosing regimen used for the individual agents. The control group receive the carrier alone at the same schedule as the combination group. Tumor size is measured every other day in 2 dimensions using calipers, and tumor volume is calculated with the formula: V=0.5(a×b2) where a is the long diameter of the tumor and b is the short diameter of the tumor. Mice are killed when the tumor reaches 2 cm3 or is ulcerated. Survival and tumor growth are evaluated from the first day of treatment until death.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.70%

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    Product Name:
    Ricolinostat
    Cat. No.:
    HY-16026
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