1. Cell Cycle/DNA Damage
    Epigenetics
    Apoptosis
    Autophagy
  2. HDAC
    Apoptosis
    Autophagy
  3. Quisinostat

Quisinostat (Synonyms: JNJ-26481585)

Cat. No.: HY-15433 Purity: 98.02%
Handling Instructions

Quisinostat (JNJ-26481585) is a potent, second-generation and orally active pan-HDAC inhibitor (HDACi), with IC50 values ranging from 0.11 nM to 0.64 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11. Quisinostat has a broad spectrum antitumoral activity. Quisinostat can induce autophagy in neuroblastoma cells.

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

Quisinostat Chemical Structure

Quisinostat Chemical Structure

CAS No. : 875320-29-9

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 158 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 252 In-stock
Estimated Time of Arrival: December 31
50 mg USD 504 In-stock
Estimated Time of Arrival: December 31
100 mg USD 744 In-stock
Estimated Time of Arrival: December 31
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Based on 4 publication(s) in Google Scholar

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Description

Quisinostat (JNJ-26481585) is a potent, second-generation and orally active pan-HDAC inhibitor (HDACi), with IC50 values ranging from 0.11 nM to 0.64 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11. Quisinostat has a broad spectrum antitumoral activity[1]. Quisinostat can induce autophagy in neuroblastoma cells[2].

IC50 & Target[1]

HDAC1

0.11 nM (IC50)

HDAC2

0.33 nM (IC50)

HDAC4

0.64 nM (IC50)

HDAC10

0.46 nM (IC50)

HDAC11

0.37 nM (IC50)

HDAC3

4.86 nM (IC50)

HDAC5

3.69 nM (IC50)

HDAC8

4.26 nM (IC50)

HDAC9

32.1 nM (IC50)

HDAC6

76.8 nM (IC50)

HDAC7

119 nM (IC50)

In Vitro

Quisinostat inhibits HDAC isozymes in vitro[1].
Quisinostat (30-1000 nM; 24 hours) is a potent pan-HDAC inhibitor in tumor cells[1].
Quisinostat has a broad spectrum antiproliferative activity against solid and hematologic cancer cell lines and induces apoptosis[1].

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

Western Blot Analysis[1]

Cell Line: Human A2780 ovarian carcinoma cells
Concentration: 30 nM, 100 nM, 300 nM, 1000 nM
Incubation Time: 24 hours
Result: Induced H3 and H4 acetylation at concentrations as low as 30 to 100 nM.
In Vivo

Quisinostat (40 mg/kg; p.o.; once daily; for 3 days) acts as a potent HDAC1 inhibitor p21waf1,cip1 ZsGreen tumors in vivo[1].
Quisinostat induces continuous H3 acetylation in tumor tissue in vivo[1].
Quisinostat (10 mg/kg; once daily; i.p.; for 14 days) strongly inhibits the growth of large pre-established HCT116 colon xenografts[1].

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

Animal Model: NMRI nude mice, with HCT116 colon carcinoma cells xenografts[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection, once daily, for 14 days
Result: Strongly inhibited the growth of large pre-established HCT116 colon xenografts.
Clinical Trial
Molecular Weight

394.47

Formula

C₂₁H₂₆N₆O₂

CAS No.

875320-29-9

SMILES

O=C(C1=CN=C(N2CCC(CNCC3=CN(C)C4=C3C=CC=C4)CC2)N=C1)NO

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (126.75 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5350 mL 12.6752 mL 25.3505 mL
5 mM 0.5070 mL 2.5350 mL 5.0701 mL
10 mM 0.2535 mL 1.2675 mL 2.5350 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 (6.34 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

QuisinostatJNJ-26481585JNJ26481585JNJ 26481585HDACApoptosisAutophagyHistone deacetylaseshistonedeacetylasehematologicmalignanciesInhibitorinhibitorinhibit

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