Quisinostat (JNJ-26481585) 2HCl

For research use only.

Catalog No.S1096

34 publications

Quisinostat (JNJ-26481585) 2HCl Chemical Structure

CAS No. 875320-31-3

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.

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Selleck's Quisinostat (JNJ-26481585) 2HCl has been cited by 34 publications

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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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HuT78 M4HTSmZ2dmO2aX;uJIF{e2G7 NUjKVWY2OTBibl2= Mn7IbY5kemWjc3XzJJRp\SCuZY\lcEBw\iCjY3X0fYxifGWmIHz5d4lv\SCNMUCgc4YhcGm|dH;u[UBJOw>? MmD2N|AxOTJ2MUi=
HepG2 NHm3WXZE\WyuII\pZYJqdGm2eTDhd5NigQ>? MXe1MEAyOCxiMkCsJFQxNCB6MDygNVYxKGGwZDCzNlAhdk1? NVy1b4xNOjRuIES4MEA4OiCq MmLKWIhmKEmFNUCgeoFtfWW|IH;mJINmdGy|IH\vdkByfWm|aX7vd5RifCC2cnXheI1mdnRiYYSgOFgh[W6mIEeyJIghf2W{ZTC4NU4zKGGwZDCzNE45KG6PLDDy[ZNx\WO2aY\lcJkv NFPGfZEzQDh2OUC4NC=>
RD cells MW\GeY5kfGmxbjDhd5NigQ>? NV;EOW1vOTVibl2= MX6yOEBpKGGwZDCzNEBp NXe4dpF6T1ONNkmwJIFv\CCMTlqtNlY1QDF3OEWgZ49weGW{YYTl[EB1dyCrbnT1Z4Uh[2ynYY\h[4Uhd2ZidHjlJIlvcXSrYYTvdkBk[XOyYYPlMVkhcW62bzDpeJMh[WO2aY\lJJA{PSCjbnSgdFM4KG[{YXft[Y51eyCjbnSgc4YhfGinIHXm[oVkfG:{IHPhd5Bie2VvMzDpcpRwKGm2czDhZ5RqfmVicEGyJIFv\CCyMUeg[pJi\22nboTz NYi1WWpZOjh4MUe0OFE>
RH30 cells NIfiN|dHfW6ldHnvckBie3OjeR?= M{DyflE2KG6P M{fXOFI1KGhiYX7kJFMxKGh? NHXBVnZIW0t4OUCgZY5lKEqQSj2yOlQ5OTV6NTDjc49x\XKjdHXkJJRwKGmwZIXj[UBkdGWjdnHn[UBw\iC2aHWgbY5qfGmjdH;yJINie3Cjc3WtPUBqdnSxIHn0d{Bi[3SrdnWgdFM2KGGwZDDwN|ch\nKjZ33lcpR{KGGwZDDv[kB1cGViZX\m[YN1d3JiY3HzdIF{\S1|IHnueI8hcXS|IHHjeIl3\SCyMUKgZY5lKHBzNzDmdoFodWWwdIO= M1zxdFI5PjF5NESx
A549 cells MV3D[YxtKH[rYXLpcIl1gSCjc4PhfS=> MmHVNlQtKDR6LDDvdkA4OiCq M1:4SJRp\SCLQ{WwJJZidHWnczDv[kBk\WyuczDmc5IhPDhiYX7kJFczKGhib3[gdZVqe2mwb4P0ZZQhfHKnYYTt[Y51KHencnWgPFIvPCCjbnSgOFIvOCCwTTygdoV{eGWldHn2[Yx6Ng>? NWf0bVNMOjd2MkO0OVQ>

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
HDAC1 / HDAC2 / HDAC4; 

PubMed: 30443188     


The effects of quisinostat on the expressions of HDACs in HCC cells. The expression levels of HDAC1, HDAC2 and HDAC4 were suppressed in both HCCLM3 and SMMC-7721 cell lines. Images were photographed with confocal microscope under ×200 magnification. Scale bar, 100 μm. Data were shown as mean ± SD. n = 3; * P < 0.05, ** P < 0.01 and *** P < 0.001 compared with DMSO group.

p21 / CDK2 / CDK4 / CDK6 / Cyclin D1 / Cyclin E1 / Cyclin A2; 

PubMed: 30443188     


Western blot analysis of p21, cdk2, cdk4, cdk6, cyclinD1, cyclinE1 and cyclinA2 proteins after quisinostat treatment. 

Caspase-3/ Cleaved caspase-3 / caspase-9 / Cleaved caspase-9 / PARP / Cleaved PARP / Bcl-xl / Bcl2 / Bax / Survivin; 

PubMed: 30443188     


Western blot analysis of Caspase-3, cleaved-Caspase-3, Caspase-9, cleaved-Caspase-9, PARP, cleaved-PARP, Bcl-xl, Bcl2, Bax and survivin protein were carried out after quisinostat treatment. 

PI3K-p110 / PI3K-p85 / p-AKT / JNK / p-JNK / p-c-Jun ; 

PubMed: 30443188     


HCCLM3 and SMMC-7721 cells were treated with quisinostat (12.5, 25.0 and 50.0nM) for 48 h. Western blot analysis was used to evaluate expressions of PI3K-p110, PI3K-p85, phosphorylation of AKT473, JNK, phosphorylation of JNK and c-Jun.

30443188
Growth inhibition assay
Cell viability; 

PubMed: 30443188     


Quisinostat inhibited cell proliferation in HCCLM3, Sk-hep-1, Hep-3B, Huh7 and SMMC-7721 cells as a concentration-dependent manner verified by CCK8 assay. 

30443188
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]
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  • 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.
  • 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 to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing. 		5mg/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
Smiles CN1C=C(C2=CC=CC=C21)CNCC3CCN(CC3)C4=NC=C(C=N4)C(=O)NO.Cl.Cl

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Frequently Asked Questions

  • Question 1:

    I was thinking of resuspending the powder in 10% hydroxy-propyl-β-cyclodextrin, 25mg/ml mannitol, in sterile water (final pH 8.7). Is this a good vehicle to use? What is the solubility of this chemical in such a vehicle?

  • Answer:

    This vehicle can be used for in vivo studies. The following papers also used this vehicle: 1. http://www.nature.com/leu/journal/v23/n10/full/leu2009121a.html; 2. http://cancerres.aacrjournals.org/content/69/13/5307.long (The solvent contains 10% hydroxypropyl-β-cyclodextrin, 0.8% HCl (0.1 N), 0.9 % NaOH (0.1 N), 3.4% mannitol and pyrogen-free water). The solubility is 2mg/ml.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID