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Quisinostat dihydrochloride

Catalog No. T6865   CAS 875320-31-3
Synonyms: Quisinostat 2HCl, Quisinostat (JNJ-26481585) 2HCl, JNJ26854165(Quisinostat) 2HCl, JNJ-26481585 2HCl

Quisinostat dihydrochloride (JNJ26854165(Quisinostat) 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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Quisinostat dihydrochloride Chemical Structure
Quisinostat dihydrochloride, CAS 875320-31-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 59.00
5 mg In stock $ 129.00
10 mg In stock $ 227.00
25 mg In stock $ 349.00
50 mg In stock $ 457.00
100 mg In stock $ 659.00
1 mL * 10 mM (in DMSO) In stock $ 132.00
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Purity: 98.5%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Quisinostat dihydrochloride (JNJ26854165(Quisinostat) 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.
Targets&IC50 HDAC1:0.11 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]
Kinase Assay 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 (25 mM 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 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)
Synonyms Quisinostat 2HCl, Quisinostat (JNJ-26481585) 2HCl, JNJ26854165(Quisinostat) 2HCl, JNJ-26481585 2HCl
Molecular Weight 467.39
Formula C21H28Cl2N6O2
CAS No. 875320-31-3

Storage

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

Solubility Information

DMSO: 73 mg/mL (156.2 mM)

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

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Arts J, et al. Clin Cancer Res, 2009, 15(22), 6841-6851. 2. Stühmer T, et al. Br J Haematol 2010, 149(4), 529-536

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library NF-κB Signaling Compound Library Bioactive Compounds Library Max Anti-Lung Cancer Compound Library Inhibitor Library Apoptosis Compound Library Histone Modification Compound Library Epigenetics Compound Library

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Keywords

Quisinostat dihydrochloride 875320-31-3 Apoptosis Autophagy Chromatin/Epigenetic DNA Damage/DNA Repair HDAC Histone deacetylases deacetylase Quisinostat JNJ26481585 Quisinostat 2HCl JNJ26854165(Quisinostat) histone Quisinostat (JNJ-26481585) 2HCl inhibit JNJ26854165(Quisinostat) 2HCl Inhibitor Quisinostat Dihydrochloride malignancies JNJ-26481585 2HCl hematologic JNJ-26481585 Quisinostat (JNJ-26481585) JNJ 26481585 inhibitor

 

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