Bobcat 339 (Synonyms: BC339) |
| رقم الكتالوجGC46935 |
Bobcat 339 هو مثبط قوي وانتقائي قائم على السيتوزين من إنزيم TET ، مع IC50s من 33 ميكرومتر و 73 ميكرومتر لـ TET1 و TET2 ، على التوالي. يعتبر Bobcat 339 مفيدًا في مجال علم التخلق ويعمل كنقطة انطلاق للعلاجات الجديدة التي تستهدف مثيلة الحمض النووي ونسخ الجينات.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2280037-51-4
Sample solution is provided at 25 µL, 10mM.
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Bobcat 339 is a novel cytosine-based TET enzyme inhibitor with good selectivity, exhibiting IC50 values of 33μM for TET1 and 73μM for TET2 without inhibiting the DNA methyltransferase DNMT3a[1]. TET enzymes are key epigenetic modifiers that facilitate DNA demethylation and regulate cell differentiation and development[2]. By competitively inhibiting the TET-mediated oxidation of 5-methylcytosine (5mC), Bobcat 339 is particularly suitable for investigating TET functions in epigenetic studies and elucidating mechanisms in relevant disease models[3,4].
In vitro, treatment of mouse hippocampal neuronal HT-22 cells with 10μM Bobcat 339 (in 1%DMSO) for 24h significantly reduced global levels of 5-hydroxymethylcytosine (5hmC)[1]. Incubation of mouse hypothalamic GT1-7 neuronal cells with 10μM Bobcat 339 for 6h decreased TET3 protein expression without affecting its mRNA abundance[5]. Furthermore, 72h treatment of human breast cancer MDA-MB-231 cells with 25μM Bobcat 339 downregulated FANCA gene expression and significantly inhibited cell proliferation via TET inhibition[6].
In vivo, intraperitoneal injection of Bobcat 339 (2.5mg/kg) in mice with GFP-specific expression in agouti-related petide (AgRP) neurons of the hypothalamus resulted in a notable reduction in TET3-positive AgRP neurons within 2 days, accompanied by increased neuronal activation (indicated by elevated FOS protein expression)[5]. In C57BL/6 mice with transient middle cerebral artery occlusion (tMCAO) and a lipopolysaccharide (LPS)-induced (10mg/kg; i.p.) hyperinflammatory state, intravenous administration of Bobcat 339 (10mg/kg/day) for 3 consecutive days significantly reduced cerebral infarct volume and improved neurological functional recovery[7].
References:
[1] CHUA G N L, WASSARMAN K L, SUN H, et al. Cytosine-based TET enzyme inhibitors[J]. ACS Medicinal Chemistry Letters, 2019, 10(2): 180-185.
[2] WEIRATH N A, HURBEN A K, CHAO C, et al. Small molecule inhibitors of TET dioxygenases: Bobcat339 activity is mediated by contaminating copper (II)[J]. ACS Medicinal Chemistry Letters, 2022, 13(5): 792-798.
[3] FENG J, SHAO N, SZULWACH K E, et al. Role of Tet1 and 5-hydroxymethylcytosine in cocaine action[J]. Nature Neuroscience, 2015, 18(4): 536-544.
[4] XU Y, YANG Y, WANG Z, et al. ZNF397 deficiency triggers TET2-driven lineage plasticity and AR-targeted therapy resistance in prostate cancer[J]. Cancer Discovery, 2024, 14(8): 1496-1521.
[5] LV H, CATARINO J, LI D, et al. A small-molecule degrader of TET3 as treatment for anorexia nervosa in an animal model[J]. Proceedings of the National Academy of Sciences, 2023, 120(16): e2300015120.
[6] LUO L, YUAN F, PALOVCAK A, et al. Oncogenic properties of wild-type DNA repair gene FANCA in breast cancer[J]. Cell Reports, 2025, 44(4): 115480.
[7] WANG Y, ZHANG L, LYU T, et al. Association of DNA methylation/demethylation with the functional outcome of stroke in a hyperinflammatory state[J]. Neural Regeneration Research, 2024, 19(10): 2229-2239.
| Cell experiment [1]: | |
Cell lines | HT-22 (mouse hippocampal neuronal cell line) |
Preparation Method | HT-22 cells were treated with 10μM Bobcat 339 in 1% DMSO for 24h and lysed. DNA was extracted, and 5hmC levels were detected using a 5hmC-specific antibody, allowing for percent 5hmC of all cytosine species to be determined by colorimetric detection. |
Reaction Conditions | 10μM; 24h |
Applications | Cells treated with Bobcat 339 had significantly reduced global 5hmC levels as compared to the vehicle control, demonstrating its ability to reduce DNA 5hmC abundance by inhibiting TET enzyme function in living cells. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice with transient middle cerebral artery occlusion (tMCAO) and an LPS-induced (10mg/kg; i.p.) hyperinflammatory state |
Preparation Method | Bobcat 339 was dissolved in dimethylsulfoxide and diluted in saline at a concentration of 1mg/mL. Bobcat 339 (10mg/kg/day) was administrated by tail vein injection 3 days before surgery, followed by daily injection once a day until the date of surgery. All mice were subjected to intraperitoneal injections of LPS (10mg/kg) to induce hyperinflammation at the onset of tMCAO. Reagents were administered again at the onset of reperfusion to ensure the efficacy. All mice underwent behavioral testing at 24h after surgery. |
Dosage form | 10mg/kg/day; 3 days; i.v. |
Applications | Treatment with Bobcat 339 (10mg/kg/day; 3 days; i.v.) significantly reduced cerebral infarct volume and improved neurological and motor deficits in C57BL/6 mice subjected to tMCAO and LPS-induced (10mg/kg; i.p.) hyperinflammatory state. |
References: | |
| Cas No. | 2280037-51-4 | SDF | |
| المرادفات | BC339 | ||
| Canonical SMILES | O=C1N=C(C(Cl)=CN1C2=CC=CC(C3=CC=CC=C3)=C2)N | ||
| Formula | C16H12ClN3O | M.Wt | 297.7 |
| الذوبان | DMF: 1 mg/ml,DMSO: 1 mg/ml,DMSO:PBS (pH 7.2) (1:8): 0.11 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.3591 mL | 16.7954 mL | 33.5909 mL |
| 5 mM | 671.8 μL | 3.3591 mL | 6.7182 mL |
| 10 mM | 335.9 μL | 1.6795 mL | 3.3591 mL |
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
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