Art. -Nr.: HY-15433

Quisinostat

(Synonyms: JNJ-26481585)

18 Cited Publications

Kundenbewertung

Based on 18 publication(s) in Google Scholar

Quisinostat (JNJ-26481585) is a potent 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.

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Reinheit: 99.71%
CAS. Nr.: 875320-29-9
Formel: C₂₁H₂₆N₆O₂
Molecular Weight:394.47

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Quisinostat Chemical Structure

CAS. Nr.: 875320-29-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (18)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Quisinostat (JNJ-26481585) is a potent 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)

Alle HDAC Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
D283 Med	IC₅₀	<200 nM Compound: Quisinostat	Antiproliferative activity against human D283 Med cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human D283 Med cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33636537]
D283 Med	CC₅₀	11 nM Compound: Quisinostat	Cytotoxicity against human D283 Med cells assessed as reduction in cell viability incubated for 1 hr by CellTiter-Glo analysis Cytotoxicity against human D283 Med cells assessed as reduction in cell viability incubated for 1 hr by CellTiter-Glo analysis	[PMID: 38832890]
Daoy	IC₅₀	<100 nM Compound: Quisinostat	Antiproliferative activity against human Daoy cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human Daoy cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33636537]
HEK-293T	IC₅₀	0.06 μM Compound: Qui	Cytotoxicity against HEK293T cells incubated for 72 hrs by CCK-8 assay Cytotoxicity against HEK293T cells incubated for 72 hrs by CCK-8 assay	[PMID: 35175762]
HepG2	IC₅₀	0.03 μM Compound: Qui	Cytotoxicity against human HepG2 cells incubated for 72 hrs by CCK-8 assay Cytotoxicity against human HepG2 cells incubated for 72 hrs by CCK-8 assay	[PMID: 35175762]
HuT78	EC₅₀	6.5 nM Compound: 3	Pro-apoptotic activity in human HUT78 cells after 18 hrs by caspase-Glo 3/7 assay Pro-apoptotic activity in human HUT78 cells after 18 hrs by caspase-Glo 3/7 assay	[PMID: 30122227]
Sf9	IC₅₀	0.11 nM Compound: 6	Inhibition of full length recombinant human HDAC1 expressed in baculovirus infected Sf9 cells using RHKK-Ac as substrate by fluorescence analysis Inhibition of full length recombinant human HDAC1 expressed in baculovirus infected Sf9 cells using RHKK-Ac as substrate by fluorescence analysis	[PMID: 27606546]
Sf9	IC₅₀	0.33 nM Compound: 6	Inhibition of full length recombinant human HDAC2 expressed in baculovirus infected Sf9 cells using RHKK-Ac as substrate by fluorescence analysis Inhibition of full length recombinant human HDAC2 expressed in baculovirus infected Sf9 cells using RHKK-Ac as substrate by fluorescence analysis	[PMID: 27606546]
Sf9	IC₅₀	4.86 nM Compound: 6	Inhibition of full length recombinant human HDAC3/NCOR2 expressed in baculovirus infected Sf9 cells using RHKK-Ac as substrate by fluorescence analysis Inhibition of full length recombinant human HDAC3/NCOR2 expressed in baculovirus infected Sf9 cells using RHKK-Ac as substrate by fluorescence analysis	[PMID: 27606546]
Sf9	IC₅₀	76.8 nM Compound: 6	Inhibition of full length recombinant human HDAC6 expressed in baculovirus infected Sf9 cells using RHKK-Ac as substrate by fluorescence analysis Inhibition of full length recombinant human HDAC6 expressed in baculovirus infected Sf9 cells using RHKK-Ac as substrate by fluorescence analysis	[PMID: 27606546]
Sf9	IC₅₀	0.00196 μM Compound: JNJ-26481585	Inhibition of recombinant full length human HDAC10 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay Inhibition of recombinant full length human HDAC10 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay	[PMID: 31938464]
Sf9	IC₅₀	0.00216 μM Compound: JNJ-26481585	Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay	[PMID: 31938464]
Sf9	IC₅₀	0.00404 μM Compound: JNJ-26481585	Inhibition of recombinant full length human HDAC7 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay Inhibition of recombinant full length human HDAC7 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay	[PMID: 31938464]
Sf9	IC₅₀	0.00461 μM Compound: JNJ-26481585	Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay	[PMID: 31938464]
Sf9	IC₅₀	0.00595 μM Compound: JNJ-26481585	Inhibition of recombinant full length human HDAC5 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay Inhibition of recombinant full length human HDAC5 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay	[PMID: 31938464]
Sf9	IC₅₀	0.0067 μM Compound: JNJ-26481585	Inhibition of recombinant human HDAC9 (604-1066 residues) expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay Inhibition of recombinant human HDAC9 (604-1066 residues) expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay	[PMID: 31938464]
Sf9	IC₅₀	0.61 nM Compound: JNJ-26481585	Inhibition of recombinant full length human HDAC1 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay Inhibition of recombinant full length human HDAC1 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay	[PMID: 31938464]

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].

MedChemExpress (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 that inhibits 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].

MedChemExpress (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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 875320-29-9
Appearance Solid
Molecular Weight 394.47
Formel C₂₁H₂₆N₆O₂
Color Off-white to yellow
SMILES

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

JNJ-26481585
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (18)

All Cell Proliferation/Viability AssayIHCIn Vivo Efficacy StudyWBIF

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Journal Impact Factor

Cancer Cell

Fusobacterium nucleatum facilitates anti-PD-1 therapy in microsatellite stable colorectal cancer. [Abstract]

2024 Oct 14;42(10):1729-1746.e8. PMID: 39303724
Nat Commun

Epigenetic-based differentiation therapy for Acute Myeloid Leukemia. [Abstract]

2024 Jul 2;15(1):5570. PMID: 38956053
Nat Commun

Selective inhibition of cancer cell self-renewal through a Quisinostat-histone H1.0 axis. [Abstract]

2020 Apr 14;11(1):1792. PMID: 32286289

Quisinostat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Apr 14;11(1):1792. [Abstract]

Quisinostat (25–50 nM; 7 d) blocked proliferation without inducing substantial death of HCC1569 cells.

Quisinostat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Apr 14;11(1):1792. [Abstract]

Quisinostat (4 mg/kg; i.p.; 21 d) caused reduced fractions of proliferating Ki67⁺ cells and no increase in apoptotic TUNEL⁺ cells in NSG mice to generate orthotopic xenografts, confirming that Quisinostat treatment induced cytostasis, not cell death, in vivo.

Quisinostat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Apr 14;11(1):1792. [Abstract]

Quisinostat (4 mg/kg; i.p.; once daily) strongly inhibited tumor maintenance in the three PDX models of lung, pancreas and breast cancer.

Quisinostat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Apr 14;11(1):1792. [Abstract]

Quisinostat (100 nM; 24 h) decreased total and phosphorylated SMAD2 (p-SMAD2) in HCC1569 cells.

Quisinostat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Apr 14;11(1):1792. [Abstract]

Quisinostat (4 mg/kg; i.p.; 21 d) treatment increased the levels of E-cadherin of HCC1569-induced orthotopic xenografts in NSG mice, indicating a reversion to a more epithelial phenotype.
Exp Hematol Oncol

A high-throughput screening identifies histone deacetylase inhibitors as therapeutic agents against medulloblastoma. [Abstract]

2019 Nov 15;8:30. PMID: 31788346
Theranostics

Interaction between p53 and Ras signaling controls cisplatin resistance via HDAC4- and HIF-1α-mediated regulation of apoptosis and autophagy. [Abstract]

2019 Jan 30;9(4):1096-1114. PMID: 30867818
Adv Sci (Weinh)

Macrophage TRIM21 Inhibition Ameliorates Murine Acute Pancreatitis via PHB2-Mediated Mitochondrial Stabilization. [Abstract]

2026 Jan 22:e17877. PMID: 41572443
NPJ Precis Oncol

Tackling FGFR3-driven bladder cancer with a promising synergistic FGFR/HDAC targeted therapy. [Abstract]

2023 Jul 21;7(1):70. PMID: 37479885
EMBO J

Acetylation of TIR domains in the TLR4-Mal-MyD88 complex regulates immune responses in sepsis. [Abstract]

2024 Nov;43(21):4954-4983. PMID: 39294473
Blood Adv

Utilizing Epigenetic Regulators to improve HSC-based lentiviral gene therapy. [Abstract]

2024 Jun 25:bloodadvances.2024013047. PMID: 38916861
Cancer Cell Int

Epigenetic potentiation of 5-fluorouracil by HDAC inhibitor quisinostat enhances antitumor effects in colorectal cancer. [Abstract]

2025 Oct 8;25(1):340. PMID: 41063169
Antimicrob Agents Chemother

In vitro and in vivo activity of quisinostat against Toxoplasma gondii. [Abstract]

2025 Sep 3;69(9):e0181924. PMID: 40741955
Toxicol Appl Pharmacol

Death by histone deacetylase inhibitor quisinostat in tongue squamous cell carcinoma via apoptosis, pyroptosis, and ferroptosis. [Abstract]

2021 Jan 1;410:115363. PMID: 33290780
Int J Parasitol Drugs Drug Resist

2026 May 17;31:100649.
Patent

US20250161243A1.
bioRxiv

2025 January 15.
bioRxiv

2024 July 04.
Albert-ludwigs-university Of Freiburg

2019 Dec.
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 41.67 mg/mL (105.64 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Arts J, et al. JNJ-26481585, a novel "second-generation" oral histone deacetylase inhibitor, shows broad-spectrum preclinical antitumoral activity. Clin Cancer Res. 2009 Nov 15;15(22):6841-51. [Content Brief]

[2]. Vamsi Krishna Kommalapati, et al. Inhibition of JNJ-26481585-mediated autophagy induces apoptosis via ROS activation and mitochondrial membrane potential disruption in neuroblastoma cells. Mol Cell Biochem. 2020 May;468(1-2):21-34. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5350 mL	12.6752 mL	25.3505 mL	63.3762 mL
	5 mM	0.5070 mL	2.5350 mL	5.0701 mL	12.6752 mL
	10 mM	0.2535 mL	1.2675 mL	2.5350 mL	6.3376 mL
	15 mM	0.1690 mL	0.8450 mL	1.6900 mL	4.2251 mL
	20 mM	0.1268 mL	0.6338 mL	1.2675 mL	3.1688 mL
	25 mM	0.1014 mL	0.5070 mL	1.0140 mL	2.5350 mL
	30 mM	0.0845 mL	0.4225 mL	0.8450 mL	2.1125 mL
	40 mM	0.0634 mL	0.3169 mL	0.6338 mL	1.5844 mL
	50 mM	0.0507 mL	0.2535 mL	0.5070 mL	1.2675 mL
	60 mM	0.0423 mL	0.2113 mL	0.4225 mL	1.0563 mL
	80 mM	0.0317 mL	0.1584 mL	0.3169 mL	0.7922 mL
	100 mM	0.0254 mL	0.1268 mL	0.2535 mL	0.6338 mL

Keywords

Quisinostat

18 Cited Publications

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Quisinostat

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Epigenetics Compound Library

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Bioactive Compound Library

Anti-Brain Cancer Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Quisinostat

Alle HDAC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (18)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Quisinostat Related Classifications

HY-15433 Related Classifications