Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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GSK-3484862 (GSK3484862) is a novel, potent and non-covalent Dnmt1 (DNA methyltransferase) inhibitor with potential anticancer activity. It induces DNA hypomethylation in cancer cells.
ln Vitro |
Significant reduction of DNA methylation is caused by GSK-3484862 (0-10 μM, 6 or 14 days) [2]. GSK-3484862 (0-10 μM, 4 days) results in a slight reduction in the levels of DNMT1 protein [2].
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Cell Assay |
Cell Viability Assay[2]
Cell Types: Mouse Embryonic Stem Cells (mESC, Wild Type (WT) or Dnmt1/3a/3b Triple Knockout (TKO)) Tested Concentrations: 2 µM and 10 µM Incubation Duration: 6 or 14 days Experimental Results: Result There was a dramatic loss of DNA methylation, with overall CpG methylation levels in WT mESCs falling from nearly 70% to less than 18% after 6 days. Western Blot Analysis[2] Cell Types: Mouse Embryonic Stem Cells (mESC, Wild Type (WT) or Dnmt1/3a/3b Triple Knockout (TKO)) Tested Concentrations: 2 µM and 10 µM Incubation Duration: 4 days Experimental Results: Production of DNMT1 Protein levels are moderately diminished. |
References |
[1]. Keystone Symposia 2019 - Epigenetics and Human Disease
[2]. Nathalia Azevedo Portilho, et al. The DNMT1 inhibitor GSK-3484862 mediates global demethylation in murine embryonic stem cells. |
Molecular Formula |
C₁₉H₁₉N₅OS
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Molecular Weight |
365.45
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CAS # |
2170136-65-7
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Related CAS # |
(Rac)-GSK-3484862;2170136-02-2
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(N)[C@H](SC1=NC(N(C)C)=C(C#N)C(CC)=C1C#N)C2=CC=CC=C2
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InChi Key |
KIEQQZZDWUNUQK-MRXNPFEDSA-N
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InChi Code |
InChI=1S/C19H19N5OS/c1-4-13-14(10-20)18(24(2)3)23-19(15(13)11-21)26-16(17(22)25)12-8-6-5-7-9-12/h5-9,16H,4H2,1-3H3,(H2,22,25)/t16-/m1/s1
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Chemical Name |
(R)-2-((3,5-dicyano-6-(dimethylamino)-4-ethylpyridin-2-yl)thio)-2-phenylacetamide
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Synonyms |
GSK3484862GSK-3484862 GSK 3484862
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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 : ~20.83 mg/mL (~57.00 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (5.69 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: 2.08 mg/mL (5.69 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7364 mL | 13.6818 mL | 27.3635 mL | |
5 mM | 0.5473 mL | 2.7364 mL | 5.4727 mL | |
10 mM | 0.2736 mL | 1.3682 mL | 2.7364 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.