Quisinostat (Synonyms: JNJ-26481585)

Name: Quisinostat
Brand: MedChemExpress
SKU: HY-15433
Rating: 5.0 (17 reviews)

Cat. No.: HY-15433 Purity: 99.71%: Data Sheet
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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.

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

CAS No. : 875320-29-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of Quisinostat:

Quisinostat dihydrochloride In-stock
Quisinostat hydrochloride Get quote

17 Publications Citing Use of MCE Quisinostat

Cell Proliferation/Viability Assay

IHC

In Vivo Efficacy Study

: 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.

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

Biological Activity
Purity & Documentation
References
Customer Review

Description

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)

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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	0.00061 μM 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]
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	0.11 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]

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

Molecular Weight

394.47

Formula

C₂₁H₂₆N₆O₂

CAS No.

875320-29-9

Appearance

Solid

Color

Off-white to yellow

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
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

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)

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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:

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.71%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (249 KB) HNMR (327 KB) RP-HPLC (259 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

Quisinostat Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Quisinostat875320-29-9JNJ-26481585JNJ26481585JNJ 26481585HDACAutophagyHistone deacetylaseshistonedeacetylasehematologicmalignanciesInhibitorinhibitorinhibit

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Quisinostat (Synonyms: JNJ-26481585)

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Other Forms of Quisinostat:

Quisinostat Related Antibodies

17 Publications Citing Use of MCE Quisinostat

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Customer Review

Quisinostat Related Antibodies

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Complete Stock Solution Preparation Table

Quisinostat Related Classifications

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