| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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KDM5-C70 is a novel and potent JARID1 (Jumonji AT-Rich Interactive Domain 1) Histone Demethylases Inhibitor with anticancer activity. It is an ethyl ester prodrug of KDM5-C49 with enhanced cellular permeability.
| ln Vitro |
After 7 days of treatment at increasing concentrations, KDM5-C70 (10-9-10-5 M; 7 days; MM.1S myeloma cells) therapy demonstrated antiproliferative effects (expectedly, KDM5-C70 lowered viability/proliferation at ~20 50%) micron)[1]. Treatment with KDM5-C70 (50 μM; 7 days; MM.1S myeloma cells) reduced retinoblastoma protein (Rb) phosphorylation levels, but did not affect overall levels of phosphorylated Rb (pRb), suggesting poor cell cycle progress [1]. At a 50 μM inhibitor dose, chromatin immunoprecipitation and next-generation sequencing revealed an increase in H3K4me3 levels surrounding the KDM5-C70 transcription start site, although GSK467A did not alter appreciably [1].
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|---|---|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: MM.1S Myeloma Cells Tested Concentrations: 10-9-10-5 M Incubation Duration: 7 days Experimental Results: Antiproliferative effect was shown after 7 days of treatment at increasing concentrations. Western Blot Analysis[1] Cell Types: MM.1S Myeloma Cells Tested Concentrations: 50 μM Incubation Duration: 7 days Experimental Results: diminished phosphorylation levels of retinoblastoma protein (Rb). |
| References |
[1]. Johansson C, et al. Structural analysis of human KDM5B guides histone demethylase inhibitor development. Nat Chem Biol. 2016 Jul;12(7):539-45.
[2]. Blair LP, et al. KDM5 lysine demethylases are involved in maintenance of 3'UTR length. Sci Adv. 2016 Nov 18;2(11):e1501662. |
| Molecular Formula |
C17H28N4O3
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|---|---|
| Molecular Weight |
336.436
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| Exact Mass |
336.2161
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| CAS # |
1596348-32-1
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| SMILES |
O=C(C([H])([H])N([H])C([H])([H])C1C([H])=C(C(=O)OC([H])([H])C([H])([H])[H])C([H])=C([H])N=1)N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H]
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| Synonyms |
KDM5 C70 KDM5C70 KDM5-C70
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~297.24 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.43 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.43 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9723 mL | 14.8615 mL | 29.7230 mL | |
| 5 mM | 0.5945 mL | 2.9723 mL | 5.9446 mL | |
| 10 mM | 0.2972 mL | 1.4861 mL | 2.9723 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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