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5mg |
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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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Other Sizes |
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Purity: ≥98%
Bobcat339 is a novel and potent cytosine-based TET enzyme inhibitor with IC50 of 33 μM (TET1) and 73 μM (TET2). Bobcat339 has mid-μM inhibitor activity against TET1 and TET2, but does not inhibit the DNA methyltransferase, DNMT3a. In silico modeling of the TET enzyme active site is used to rationalize the activity of Bobcat339 and other cytosine-based inhibitors. These new molecular tools will be useful to the field of epigenetics and serve as a starting point for new therapeutics that target DNA methylation and gene transcription. It is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.
ln Vitro |
In HT-22 cells, Bobcat339 (10 μM; 24 hours) dramatically lowers total 5hmC levels by blocking TET enzyme activity [1].
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References |
[1]. Chua GNL, et, al. Cytosine-Based TET Enzyme Inhibitors. ACS Med Chem Lett. 2019 Jan 31; 10(2): 180-185.
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Molecular Formula |
C16H12CLN3O
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Molecular Weight |
297.7390
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CAS # |
2280037-51-4
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Related CAS # |
Bobcat339 hydrochloride;2436747-44-1
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SMILES |
O=C1N=C(N)C(Cl)=CN1C2=CC(C3=CC=CC=C3)=CC=C2
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Chemical Name |
1-([1,1'-biphenyl]-3-yl)-4-amino-5-chloropyrimidin-2(1H)-one
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Synonyms |
Bobcat339; Bobcat339 free base; Bobcat-339; Bobcat 339
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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 : ~5 mg/mL (~16.79 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 3.33 mg/mL (11.18 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication (<60°C).
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O 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 | 3.3586 mL | 16.7932 mL | 33.5864 mL | |
5 mM | 0.6717 mL | 3.3586 mL | 6.7173 mL | |
10 mM | 0.3359 mL | 1.6793 mL | 3.3586 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.