KPZ560
Based on 1 Customer Validation
KPZ560 is a potent inhibitor of HDAC1 and HDAC2, with IC50s of 12 nM and 68 nM, respectively. KPZ560 can increase in the spine density of granule neuron dendrites of mice and inhibitor cell growth of breast cancer cell line MCF.
For research use only. We do not sell to patients.
- Purity: 99.72%
- CAS No.: 2397562-43-3
- Formula: C26H21N5O3S2
- Molecular Weight:515.61
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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HDAC1 12 nM (IC50) |
HDAC2 68 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HMEC | IC50 |
9.85 μM
Compound: KPZ560
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Cytotoxicity against human HMEC cells assessed as inhibition of cell viability incubated for 3 days by AlamarBlue based fluorescence analysis
Cytotoxicity against human HMEC cells assessed as inhibition of cell viability incubated for 3 days by AlamarBlue based fluorescence analysis
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[PMID: 37847303] |
| MCF7 | GI50 |
0.043 μM
Compound: KPZ560
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Anticancer activity against human MCF7 cells overexpressing HDAC1 and HDAC2 assessed as inhibition of cell growth incubated for 48 hrs by sulforhodamine B assay
Anticancer activity against human MCF7 cells overexpressing HDAC1 and HDAC2 assessed as inhibition of cell growth incubated for 48 hrs by sulforhodamine B assay
|
[PMID: 37847303] |
Chemical Information
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CAS No. 2397562-43-3
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Appearance Solid
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Molecular Weight 515.61
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Formula C26H21N5O3S2
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Color White to light yellow
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SMILES
NC1=C(C=C(C=C1)C2=CC=CS2)NC(C3=CC=C(C=C3)C4=CN(N=N4)CS(C5=CC=CC=C5)(=O)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (193.95 mM; Need ultrasonic; 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 (4.85 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.
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 (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Yukihiro Itoh, et al. Discovery of Selective Histone Deacetylase 1 and 2 Inhibitors: Screening of a Focused Library Constructed by Click Chemistry, Kinetic Binding Analysis, and Biological Evaluation. J Med Chem. 2023 Oct 17. doi: 10.1021/acs.jmedchem.3c01095. Online ahead of print. [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 | 1.9395 mL | 9.6973 mL | 19.3945 mL | 48.4863 mL |
| 5 mM | 0.3879 mL | 1.9395 mL | 3.8789 mL | 9.6973 mL | |
| 10 mM | 0.1939 mL | 0.9697 mL | 1.9395 mL | 4.8486 mL | |
| 15 mM | 0.1293 mL | 0.6465 mL | 1.2930 mL | 3.2324 mL | |
| 20 mM | 0.0970 mL | 0.4849 mL | 0.9697 mL | 2.4243 mL | |
| 25 mM | 0.0776 mL | 0.3879 mL | 0.7758 mL | 1.9395 mL | |
| 30 mM | 0.0646 mL | 0.3232 mL | 0.6465 mL | 1.6162 mL | |
| 40 mM | 0.0485 mL | 0.2424 mL | 0.4849 mL | 1.2122 mL | |
| 50 mM | 0.0388 mL | 0.1939 mL | 0.3879 mL | 0.9697 mL | |
| 60 mM | 0.0323 mL | 0.1616 mL | 0.3232 mL | 0.8081 mL | |
| 80 mM | 0.0242 mL | 0.1212 mL | 0.2424 mL | 0.6061 mL | |
| 100 mM | 0.0194 mL | 0.0970 mL | 0.1939 mL | 0.4849 mL |