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Bobcat339 is a novel cytosine-based TET enzyme inhibitor with IC50s of 33 and 73 uM for TET1/2, it does not inhibit the DNA methyltransferase DNMT3a. Bobcat339 (10 μM in 1% DMSO) treated 24 hrs significantly reduces global 5hmC levels by inhibiting TET enzyme function in HT-22 cells.
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Molecular Weight | 297.74 |
| Formula | C16H12ClN3O |
| CAS Number | 2280037-51-4 |
| Purity | 99.84% |
| Solubility | DMSO |
| Storage | at -20°C |
[1] Gabriella N L Chua, et al. ACS Med Chem Lett. Cytosine-Based TET Enzyme Inhibitors
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Procainamide is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1). Procainamide is a Class 1A antiarrhythmic agent. Procainamide has the potential for the research of cancer and arrhythmias. |
| GSK-3484862
GSK-3484862 is a non-covalent inhibitor for Dnmt1. GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates global demethylation in murine embryonic stem cells. |
| O6BTG-octylglucoside
O6BTG-octylglucoside is a potent O6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor, with IC50s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells. |
| Bobcat339 hydrochloride
Bobcat339 hydrochloride is a potent and selective cytosine-based inhibitor of TET enzyme, with the IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. |
| 5-Methyl-2'-deoxycytidine
5-Methyl-2'-deoxycytidine in single-stranded DNA can act in cis to signal de novo DNA methylation. |
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