Quisinostat (JNJ-26481585) 2HCl

Catalog No.S1096

Quisinostat (JNJ-26481585) 2HCl Chemical Structure

Molecular Weight(MW): 467.39

Quisinostat (JNJ-26481585) 2HCl is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM in a cell-free assay, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. Phase 2.

Size Price Stock Quantity  
In DMSO USD 330 In stock
USD 210 In stock
USD 370 In stock
USD 970 In stock
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5 Customer Reviews

  • In vitro drug sensitivity of (C) quisinostat. Acute lymphoblastic leukemia cell lines (NALM-6, KOPN-30bi) and primary cultured cells established from patient 21 were cultured with the indicated concentrations of anticancer drugs, and viability was measured at 48 hours. Data are presented as percentages of dimethylsulfoxide (DMSO) control and depict the mean 6 standard deviation.

    J Clin Oncol, 2016, 34(28):3451-9.. Quisinostat (JNJ-26481585) 2HCl purchased from Selleck.

    (c) Acetylation site occupancies of histone H3 at positions K18 and K23 and (d) histone H4 at positions K5, K8, K12 and K16. Each bar graph represents the mean of two technical replicates with error bars showing the relative distance from the mean of the maximum and minimum values.

    Nat Commun, 2015, 6:8648.. Quisinostat (JNJ-26481585) 2HCl purchased from Selleck.

  • F, Cells were treated with 15 nM JNJ-26481585 for 6 hours. Protein expression of acetylated histone H3 (Ac-H3), H3 and α-Tubulin was assessed by Western blotting.

    Oncotarget, 2015, 6(35):37836-51.. Quisinostat (JNJ-26481585) 2HCl purchased from Selleck.

    WT ESCs were treated with varying concentrations of the HDAC1 specific inhibitor JNJ-26481585 for 24 h. Lysates were collected for ChIP experiments, and a H3K27ac antibody was used for immunoprecipitation (IP). qPCR was performed using primers specific for Hoxa1 RARE2. ChIP with an IgG antibody (negative control) is included in each panel. Error bars represent standard error of independent experiments where n = 3 for biological repeats. *, p < 0.05.

    J Biol Chem 2014 289(28), 19519-30. Quisinostat (JNJ-26481585) 2HCl purchased from Selleck.

  • Western blot analysis of Acetyl-H3 and H3. 0-10μM JNJ-26481585 was added.

     

     

    Dr. Zhang of Tianjin Medical University. Quisinostat (JNJ-26481585) 2HCl purchased from Selleck.

Purity & Quality Control

Choose Selective HDAC Inhibitors

Biological Activity

Description Quisinostat (JNJ-26481585) 2HCl is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM in a cell-free assay, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. Phase 2.
Features An orally bioavailable, second-generation, hydroxamic acid-based HDAC inhibitor.
Targets
HDAC1 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
HDAC11 [1]
(Cell-free assay)
HDAC10 [1]
(Cell-free assay)
HDAC4 [1]
(Cell-free assay)
0.11 nM 0.33 nM 0.37 nM 0.46 nM 0.64 nM
In vitro

JNJ-26481585 exhibits broad spectrum antiproliferative activity in solid and hematologic cancer cell lines, such as all lung, breast, colon, prostate, brain, and ovarian tumor cell lines, with IC50 ranging from 3.1-246 nM, which is more potent than vorinostat, R306465, panobinostat, CRA-24781, or mocetinostat in various human cancer cell lines tested. [1] A recent study shows that JNJ-26481585 promotes myeloma cell death at low nanomolar concentrations by resulting in Mcl-1 depletion and Hsp72 induction. [2]

In vivo In an HDAC1-responsive A2780 ovarian tumor screening model, JNJ-26481585 dosing at its maximal tolerated dose (10 mg/kg i.p. and 40 mg/kg p.o.) for 3 days leads to an HDAC1-regulated fluorescence , which predicts tumor growth inhibition. Furthermore, JNJ-26481585 also shows more potent inhibitory effects on the growth of C170HM2 colorectal liver metastases than 5-fluorouracil/Leucovorin. [1]

Protocol

Kinase Assay:[1]
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HDAC activity assays :

In all cases, full-length HDAC proteins are expressed using baculovirus-infected Sf9 cells. In addition, HDAC3 is coexpressed as a complex with human NCOR2. For assessing activity of HDAC1-containing cellular complexes, immunoprecipitated HDAC1 complexes are incubated with an [3H]acetyl- labeled fragment of histone H4 peptide [biotin-(6-aminohexanoic)Gly-Ala-(acetyl[3H])Lys-Arg-His-Arg-Lys-Val-NH2] in a total volume of 50μL enzyme assay buffer (25mM HEPES (pH 7.4), 1 M sucrose, 0.1 mg/mL BSA and 0.01% (v/v) Triton X-100). Incubation is performed for 45 minutes at 37 °C (immunoprecipitates) or 30 min at room temperature. Before addition of substrate, HDAC inhibitors are added at increasing concentrations and preincubated for 10 minutes at room temperature. After incubation, the reaction is quenched with 35μL stop buffer (1 M HCl and 0.4 M acetic acid). Released [3H]acetic acid is extracted with 800μL ethyl acetate and quantified by scintillation counting. Equal amounts of HDAC1 are immunoprecipitated as indicated by Western blot analysis. HDAC1 activity results are presented as mean ± SD of three independent experiments on a single lysate.
Cell Research:Cell proliferation assays
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  • Cell lines: NCL-H2106, Colo699 and LNCAP cells
  • Concentrations: 0-300 nM
  • Incubation Time: 24 hours
  • Method: All cell lines are obtained from American Type Culture Collection and cultured according to instructions. The effect of HDAC inhibitors on cell proliferation is measured using an MTT. Proliferation of non–small cell lung carcinoma (NSCLC) cell lines is assessed using an Alamar Blue–based assay. For proliferation of hematologic cell lines, cells are incubated for 72 hours and the cytotoxic activity is evaluated by MTS assay. Data are presented as mean IC50 or IC40 ± SD of at least three independent experiments.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: HCT116 human colon carcinoma cells are injected s.c. into the inguinal region of athymic male NMRI nu/nu mice, C170HM2 cell suspensions are injected into the peritoneal cavity of male MFI nude mice.
  • Formulation: JNJ-26481585 is formulated at 2 mg/mL in 20% hydroxypropyl-β-cyclodextrin (final pH 8.7).
  • Dosages: ≤10 mg/kg
  • Administration: Administered via both p.o. and i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 79 mg/mL (169.02 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
15% Captisol
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 467.39
Formula

C21H28Cl2N6O2

CAS No. 875320-31-3
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02948075 Active, not recruiting Ovarian Cancer NewVac LLC|Janssen Pharmaceutica N.V., Belgium September 2015 Phase 2
NCT02728492 Completed Non-small Cell Lung Cancer|Epithelial Ovarian Cancer NewVac LLC|Janssen Pharmaceutica N.V., Belgium August 2013 Phase 1
NCT01486277 Completed Lymphoma, T-Cell, Cutaneous Janssen Research & Development, LLC November 2011 Phase 2
NCT00676728 Terminated Advanced or Refractory Leukemia|Myelodysplastic Syndromes Johnson & Johnson Pharmaceutical Research & Development, L.L.C. December 2008 Phase 1
NCT00677105 Completed Lymphoma|Neoplasms Johnson & Johnson Pharmaceutical Research & Development, L.L.C.|Janssen Pharmaceutica N.V., Belgium August 2007 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID