Quisinostat
Based on 17 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.
For research use only. We do not sell to patients.
- Purity: 99.71%
- CAS No.: 875320-29-9
- Formula: C21H26N6O2
- Molecular Weight:394.47
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Quisinostat
More- Cancer Cell. 2024 Oct 14;42(10):1729-1746.e8. [Abstract]
- Nat Commun. 2024 Jul 2;15(1):5570. [Abstract]
- Nat Commun. 2020 Apr 14;11(1):1792. [Abstract]
- Adv Sci (Weinh). 2026 Jan 22:e17877. [Abstract]
- Exp Hematol Oncol. 2019 Nov 15;8:30. [Abstract]
- Theranostics. 2019 Jan 30;9(4):1096-1114. [Abstract]
- EMBO J. 2024 Nov;43(21):4954-4983. [Abstract]
- NPJ Precis Oncol. 2023 Jul 21;7(1):70. [Abstract]
- Blood Adv. 2024 Jun 25:bloodadvances.2024013047. [Abstract]
- Cancer Cell Int. 2025 Oct 8;25(1):340. [Abstract]
- Antimicrob Agents Chemother. 2025 Sep 3;69(9):e0181924. [Abstract]
- Toxicol Appl Pharmacol. 2021 Jan 1;410:115363. [Abstract]
- Patent. US20250161243A1.
- bioRxiv. 2025 January 15.
- bioRxiv. 2024 July 04.
- Albert-ludwigs-university Of Freiburg. 2019 Dec.
- Patent. US20180263995A1.
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Cell Proliferation/Viability Assay
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IHC
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In Vivo Efficacy Study
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WB
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IF
Biological Activity
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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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| D283 Med | IC50 |
<200 nM
Compound: Quisinostat
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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
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[PMID: 33636537] |
| D283 Med | CC50 |
11 nM
Compound: Quisinostat
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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
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[PMID: 38832890] |
| Daoy | IC50 |
<100 nM
Compound: Quisinostat
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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
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[PMID: 33636537] |
| HEK-293T | IC50 |
0.06 μM
Compound: Qui
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Cytotoxicity against HEK293T cells incubated for 72 hrs by CCK-8 assay
Cytotoxicity against HEK293T cells incubated for 72 hrs by CCK-8 assay
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[PMID: 35175762] |
| HepG2 | IC50 |
0.03 μM
Compound: Qui
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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
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[PMID: 35175762] |
| HuT78 | EC50 |
6.5 nM
Compound: 3
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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
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[PMID: 30122227] |
| Sf9 | IC50 |
0.11 nM
Compound: 6
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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
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[PMID: 27606546] |
| Sf9 | IC50 |
0.33 nM
Compound: 6
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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
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[PMID: 27606546] |
| Sf9 | IC50 |
4.86 nM
Compound: 6
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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
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[PMID: 27606546] |
| Sf9 | IC50 |
76.8 nM
Compound: 6
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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
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[PMID: 27606546] |
| Sf9 | IC50 |
0.00196 μM
Compound: JNJ-26481585
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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
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[PMID: 31938464] |
| Sf9 | IC50 |
0.00216 μM
Compound: JNJ-26481585
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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
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[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
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[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
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[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
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[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
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[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] |
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.
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Cell Line:Human A2780 ovarian carcinoma cells
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Concentration:30 nM, 100 nM, 300 nM, 1000 nM
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Incubation Time:24 hours
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Result:Induced H3 and H4 acetylation at concentrations as low as 30 to 100 nM.
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.
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Animal Model:NMRI nude mice, with HCT116 colon carcinoma cells xenografts[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection, once daily, for 14 days
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Result:Strongly inhibited the growth of large pre-established HCT116 colon xenografts.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 875320-29-9
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Appearance Solid
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Molecular Weight 394.47
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Formula C21H26N6O2
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Color Off-white to yellow
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SMILES
O=C(C1=CN=C(N2CCC(CNCC3=CN(C)C4=C3C=CC=C4)CC2)N=C1)NO
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Synonyms
JNJ-26481585
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (17)
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Journal Impact Factor
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Most Recent
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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
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.
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Adv Sci (Weinh)
Macrophage TRIM21 Inhibition Ameliorates Murine Acute Pancreatitis via PHB2-Mediated Mitochondrial Stabilization. [Abstract]2026 Jan 22:e17877. PMID: 41572443 -
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 -
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 -
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 -
Blood Adv
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
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 -
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Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
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:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (278 KB)
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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)
- Portuguese - PT (252 KB)
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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
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.
| 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 |