KDM5-IN-1
Based on 2 publication(s) in Google Scholar
KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.52%
- CAS No.: 1628210-26-3
- Formule: C17H20N6O
- Masse moléculaire:324.38
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Orally Active Compound Library
HY-L061
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Anti-Cancer Metabolism Compound Library
HY-L083
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Targeted Diversity Library
HY-L099
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Heterocyclic Compound Library
HY-L138
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
HY-L181
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HY-L001V
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Bioactive Compound Library
HY-L001
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HY-L203
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HY-L205
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Posttranslational Modification Library
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Publications Citing Use of MedChemExpress (MCE) KDM5-IN-1
More
Activité biologique
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KDM5 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PC-9 | EC50 |
0.18 μM
Compound: 121
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Inhibition of KDM5A in human PC9 cells assessed as reduction in demethylation of H3K4me3 after 120 hrs by AlphaLisa assay
Inhibition of KDM5A in human PC9 cells assessed as reduction in demethylation of H3K4me3 after 120 hrs by AlphaLisa assay
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[PMID: 26710088] |
| PC-9 | EC50 |
0.18 μM
Compound: 121
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Inhibition of KDM5B in human PC9 cells assessed as reduction in demethylation of H3K4me3 after 120 hrs by AlphaLisa assay
Inhibition of KDM5B in human PC9 cells assessed as reduction in demethylation of H3K4me3 after 120 hrs by AlphaLisa assay
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[PMID: 26710088] |
| Sf9 | IC50 |
0.014 μM
Compound: 121
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Inhibition of recombinant full length FLAG-tagged KDM5A (unknown origin) expressed in sf9 cells using biotin-H3K4me3 (1 to 21 residues as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by mass spetcrometric analys
Inhibition of recombinant full length FLAG-tagged KDM5A (unknown origin) expressed in sf9 cells using biotin-H3K4me3 (1 to 21 residues as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by mass spetcrometric analys
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[PMID: 26710088] |
KDM5-IN-1 is found to potently inhibit KDM5B and KDM5C isoforms (IC50 of 4.7 and 65.5 nM, respectively). It is significantly less potent against other KDM enzymes (1A, 2B, 3B, 4C, 5A, 6A, 7B), inhibiting KDM4C the strongest with an IC50 of 1.9 μM. KDM5-IN-1 still displays more than 100-fold selectivity for KDM4C vs. KDM5A[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1628210-26-3
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Appearance Solid
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Masse moléculaire 324.38
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Formule C17H20N6O
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Color White to off-white
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SMILES
N#CC1=C2NC(C3=CN(C(C)(C)C)N=C3)=C(C(C)C)C(N2N=C1)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273 -
Clin Exp Med
Corin: a dual inhibitor for KDM1A/HDAC1, suppresses hepatocellular carcinoma by triggering cuproptosis. [Abstract]2025 Nov 25;26(1):33. PMID: 41286164
Solvant et solubilité
DMSO : ≥ 30 mg/mL (92.48 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.08 mg/mL (6.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0828 mL | 15.4140 mL | 30.8280 mL | 77.0701 mL |
| 5 mM | 0.6166 mL | 3.0828 mL | 6.1656 mL | 15.4140 mL | |
| 10 mM | 0.3083 mL | 1.5414 mL | 3.0828 mL | 7.7070 mL | |
| 15 mM | 0.2055 mL | 1.0276 mL | 2.0552 mL | 5.1380 mL | |
| 20 mM | 0.1541 mL | 0.7707 mL | 1.5414 mL | 3.8535 mL | |
| 25 mM | 0.1233 mL | 0.6166 mL | 1.2331 mL | 3.0828 mL | |
| 30 mM | 0.1028 mL | 0.5138 mL | 1.0276 mL | 2.5690 mL | |
| 40 mM | 0.0771 mL | 0.3854 mL | 0.7707 mL | 1.9268 mL | |
| 50 mM | 0.0617 mL | 0.3083 mL | 0.6166 mL | 1.5414 mL | |
| 60 mM | 0.0514 mL | 0.2569 mL | 0.5138 mL | 1.2845 mL | |
| 80 mM | 0.0385 mL | 0.1927 mL | 0.3854 mL | 0.9634 mL |
KDM5-IN-1 Related Classifications
HY-100422 Related Classifications
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