Bobcat339
Based on 26 publication(s) in Google Scholar
Bobcat339 is a potent and selective cytosine-based inhibitor of TET enzyme, with IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.
For research use only. We do not sell to patients.
- Purity: 99.44%
- CAS No.: 2280037-51-4
- Formula: C16H12ClN3O
- Molecular Weight:297.74
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Epigenetics Compound Library
HY-L005
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Immunology/Inflammation Compound Library
HY-L007
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Reprogramming Compound Library
HY-L039
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Anti-Blood Cancer Compound Library
HY-L079
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Transcription Factor-Targeted Library
HY-L090
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Highly Selective Inhibitors Library
HY-L158
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Anti-Hematopathy Compound Library
HY-L171
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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Epigenetics Compound Library Mini
HY-L005M
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Methylation Compound Library
HY-L203
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High-Throughput Bioactive Compound Library
HY-L205
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Anti-Rheumatic Arthritis Compound Library
HY-L210
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Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) Bobcat339
More- Nat Metab. 2025 Jul;7(7):1344-1357. [Abstract]
- Cell Death Differ. 2026 May 25. [Abstract]
- J Clin Invest. 2023 Oct 16;133(20):e170173. [Abstract]
- Theranostics. 2021 Jun 11;11(16):7640-7657. [Abstract]
- J Exp Clin Cancer Res. 2025 Jul 15;44(1):206. [Abstract]
- Environ Sci Technol. 2021 Mar 2;55(5):3144-3155. [Abstract]
- Cell Death Dis. 2024 Jun 1;15(6):387. [Abstract]
- EMBO Mol Med. 2025 Oct;17(10):2809-2826. [Abstract]
- Sci Total Environ. 2024 Apr 1:919:170905. [Abstract]
- Br J Pharmacol. 2026 May 5. [Abstract]
- Br J Pharmacol. 2024 Oct;181(20):3886-3907. [Abstract]
- Clin Sci. 2023 Aug 31;137(16):1265-1283. [Abstract]
- Biomed Pharmacother. 2026 Jun:199:119505. [Abstract]
- Commun Biol. 2026 May 14. [Abstract]
- mBio. 2026 Jan 26:e0356225. [Abstract]
- Eur J Pharmacol. 2024 Aug 23:176931. [Abstract]
- Neuropharmacology. 2024 Feb 15:244:109799. [Abstract]
- Bioelectrochemistry. 2023 Aug:152:108433. [Abstract]
- Clin Epigenetics. 2024 Oct 2;16(1):136. [Abstract]
- Cancers (Basel). 2022 Jun 16;14(12):2983. [Abstract]
- Aquaculture. 2023: 739234.
- J Pharm Biomed Anal. 2021 Sep 5:203:114228. [Abstract]
- Brain Sci. 2023 Apr 10;13(4):644. [Abstract]
- Mol Pain. 2022 Apr;18:17448069221143671. [Abstract]
- Research Square Print. 2023 Mar 14.
- Research Square Print. November 29th, 2022.
Customer Validation & Images
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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RT-PCR
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In Vivo Efficacy Study
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Histological Imaging/Staining
All DNA Methyltransferase Isoforms
More
Biological Activity
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TET1 33 μM (IC50) |
TET2 73 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| Sf9 | IC50 |
33 μM
Compound: Bobcat339
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Inhibition of recombinant human N-terminal FLAG-tagged TET1 (1418 to 2136 residues) expressed in baculovirus infected sf9 cells assessed as reduction in oxidation of methylated dsDNA after 2 hrs by chemiluminescence assay
Inhibition of recombinant human N-terminal FLAG-tagged TET1 (1418 to 2136 residues) expressed in baculovirus infected sf9 cells assessed as reduction in oxidation of methylated dsDNA after 2 hrs by chemiluminescence assay
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[PMID: 30783500] |
| Sf9 | IC50 |
73 μM
Compound: Bobcat339
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Inhibition of recombinant human C-terminal His/N-terminal FLAG-tagged TET2 (1129 to 2002 residues) expressed in baculovirus infected sf9 cells assessed as reduction in oxidation of methylated dsDNA after 2 hrs by chemiluminescence assay
Inhibition of recombinant human C-terminal His/N-terminal FLAG-tagged TET2 (1129 to 2002 residues) expressed in baculovirus infected sf9 cells assessed as reduction in oxidation of methylated dsDNA after 2 hrs by chemiluminescence assay
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[PMID: 30783500] |
Bobcat339 (10 μM; 24 hours) significantly reduces global 5hmC levels by inhibiting TET enzyme function in HT-22 cells[1].
Nicholas A Weirath, et al. found that the inhibitory activity of Bobcat339 is directly related to the Cu(II) content. The inhibitory activity of Bobcat339-copper mixture on TET is much higher than that of Bobcat339 or Cu(II) alone[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2280037-51-4
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Appearance Solid
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Molecular Weight 297.74
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Formula C16H12ClN3O
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Color Off-white to light yellow
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SMILES
NC1=NC(N(C2=CC=CC(C3=CC=CC=C3)=C2)C=C1Cl)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (26)
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Journal Impact Factor
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Most Recent
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Nat Metab
2025 Jul;7(7):1344-1357. PMID: 40659911
Bobcat339 purchased from MedChemExpress. Usage Cited in: Nat Metab. 2025 Jul;7(7):1344-1357. [Abstract]
PC emergence in niche-independent culture of Lgr5-EGFPhi ISCs supplemented with dm-aKG and Bobcat339 hydrochloride (0-10 μM) for 48 h.
Bobcat339 purchased from MedChemExpress. Usage Cited in: Nat Metab. 2025 Jul;7(7):1344-1357. [Abstract]
PC emergence from ISCsmito-O (O) and ISCsmito-Y (Y) supplemented with Bobcat339 for 48 h.
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Cell Death Differ
GSDME acts as an epigenetic modifier to promote melanoma development via centriole biogenesis regulator PLK4. [Abstract]2026 May 25. PMID: 42185629 -
J Clin Invest
The CTBP2-PCIF1 complex regulates m6Am modification of mRNA in head and neck squamous cell carcinoma. [Abstract]2023 Oct 16;133(20):e170173. PMID: 37643007 -
Theranostics
Silencing of METTL3 effectively hinders invasion and metastasis of prostate cancer cells. [Abstract]2021 Jun 11;11(16):7640-7657. PMID: 34335955
Bobcat339 purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Jun 11;11(16):7640-7657. [Abstract]
PCa cells were treated with Bobcat339 hydrochloride at 50 μM for 48 h. The METTL3 mRNA levels in PCa cells were determined by qRT-PCR.
Bobcat339 purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Jun 11;11(16):7640-7657. [Abstract]
PCa cells were treated with Bobcat339 hydrochloride at 50 μM for 48 h. The METTL3 protein levels in PCa cells were determined by wb.
Bobcat339 purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Jun 11;11(16):7640-7657. [Abstract]
Bobcat339 effectively decreased migratroy and invasive capacitivities of PCa cells.
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J Exp Clin Cancer Res
CCNY-mediated phosphorylation and TET2-BACH1-driven DNA demethylation activate PRC1 to augment NSCLC progression. [Abstract]2025 Jul 15;44(1):206. PMID: 40665337
Bobcat339 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jul 15;44(1):206. [Abstract]
PRC1 mRNA expression in H1299 cells after treatment with different concentrations of Bobcat339 determined by qPCR analysis.
Bobcat339 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jul 15;44(1):206. [Abstract]
H1299 cells were subcutaneously injected into nude mice to construct xenografts, followed by intratumoral injections (10 mg/kg; Bobcat339, HPPE, or PLK1-IN-10) starting from day 7. Volume of xenograft tumors by week.
Bobcat339 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jul 15;44(1):206. [Abstract]
(Bobcat339: 10 mg/kg). Immunohistochemistry (IHC) was used to detect positive staining of C-Cas3 in tumor tissue.
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Environ Sci Technol
Graphene Quantum Dots Disrupt Embryonic Stem Cell Differentiation by Interfering with the Methylation Level of Sox 2. [Abstract]2021 Mar 2;55(5):3144-3155. PMID: 33569944 -
Cell Death Dis
Obesity-driven mitochondrial dysfunction in human adipose tissue-derived mesenchymal stem/stromal cells involves epigenetic changes. [Abstract]2024 Jun 1;15(6):387. PMID: 38824145 -
EMBO Mol Med
2025 Oct;17(10):2809-2826. PMID: 40921878
Bobcat339 purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2025 Oct;17(10):2809-2826. [Abstract]
Human primary cardiac fibroblasts were treated with TGF-β (5 ng/ml) for 24 hours with or without Bobcat 339 (50/100 μM). Piezo2 expression was detected by Western blotting.
Bobcat339 purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2025 Oct;17(10):2809-2826. [Abstract]
Human primary cardiac fibroblasts were treated with TGF-β (5 ng/ml) for 24 hours with or without Bobcat 339 (50/100 μM). Piezo2 expression was detected by qPCR.
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Sci Total Environ
Reprogramming of DNA methylation patterns mediates perfluorooctane sulfonate-induced fetal cardiac dysplasia. [Abstract]2024 Apr 1:919:170905. PMID: 38350568 -
Br J Pharmacol
VEGFR-2 blocker induces pulmonary vascular disease in rats with CRISPR-edited human non-deficient G6PD polymorphism: role of 3D genomic modifications and DNA methylation. [Abstract]2026 May 5. PMID: 42083756 -
Br J Pharmacol
HSP90β shapes the fate of Th17 cells with the help of glycolysis-controlled methylation modification. [Abstract]2024 Oct;181(20):3886-3907. PMID: 38881036 -
Clin Sci
Renal ischemia alters the transcriptomic and epigenetic profile of inflammatory genes in swine scattered tubular-like cells. [Abstract]2023 Aug 31;137(16):1265-1283. PMID: 37606084 -
Biomed Pharmacother
DNA hydroxymethylation of NCX1 heart promoter by GATA6/TET3 epigenetic complex participates in neuroprotection induced by hypoxic preconditioning. [Abstract]2026 Jun:199:119505. PMID: 42127639 -
Commun Biol
Pyruvate carboxylase promotes SREBP1a-mediated lipid synthesis in epithelial ovarian cancer. [Abstract]2026 May 14. PMID: 42129486 -
mBio
Intestinal epithelial Tet2 deficiency reprograms the gut microbiota through bile acid metabolic alterations. [Abstract]2026 Jan 26:e0356225. PMID: 41586521 -
Eur J Pharmacol
METTL3 aggravates renal fibrogenesis in obstructive nephropathy via the miR-199a-3p/PAR4 axis. [Abstract]2024 Aug 23:176931. PMID: 39182553 -
Neuropharmacology
Specific inhibition of TET1 in the spinal dorsal horn alleviates inflammatory pain in mice by regulating synaptic plasticity. [Abstract]2024 Feb 15:244:109799. PMID: 38008374 -
Bioelectrochemistry
A highly sensitive signal-on biosensor based on restriction enzyme-mediated molecular switch for detection of TET1. [Abstract]2023 Aug:152:108433. PMID: 37031472 -
Clin Epigenetics
Enzymatic TET-1 inhibition highlights different epigenetic behaviours of IL-1β and TNFα in tumour progression of OS cell lines. [Abstract]2024 Oct 2;16(1):136. PMID: 39358792 -
Cancers (Basel)
α-Ketoglutarate-Mediated DNA Demethylation Sustains T-Acute Lymphoblastic Leukemia upon TCA Cycle Targeting. [Abstract]2022 Jun 16;14(12):2983. PMID: 35740646 -
Bobcat339 purchased from MedChemExpress. Usage Cited in: Aquaculture. 2023: 739234.
Bobcat 339 (4 mM; every 48 h for a total of 7 injections) inject into the molluscum of the oyster utilizing a syringe, the expression levels of Sox-like and Sox8 are significantly increased, which are 1.93 and 1.47 times higher than the control group, respectively.
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J Pharm Biomed Anal
Assay for TET1 activity and its inhibitors screening with signal amplification by both nanoparticles and Ru(III) redox recycling. [Abstract]2021 Sep 5:203:114228. PMID: 34182409 -
Brain Sci
2023 Apr 10;13(4):644. PMID: 37190609 -
Mol Pain
Increased ten-eleven translocation methylcytosine dioxygenase one in dorsal root ganglion contributes to inflammatory pain in CFA rats. [Abstract]2022 Apr;18:17448069221143671. PMID: 36411533 -
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Solvent & Solubility
DMSO : 100 mg/mL (335.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (8.40 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (8.40 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 3.33 mg/mL (11.18 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Chua GNL, et, al. Cytosine-Based TET Enzyme Inhibitors. ACS Med Chem Lett. 2019 Jan 31; 10(2): 180-185. [Content Brief]
[2]. Weirath NA, et al. Small Molecule Inhibitors of TET Dioxygenases: Bobcat339 Activity Is Mediated by Contaminating Copper(II). ACS Med Chem Lett. 2022 Apr 21;13(5):792-798. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3586 mL | 16.7932 mL | 33.5864 mL | 83.9659 mL |
| 5 mM | 0.6717 mL | 3.3586 mL | 6.7173 mL | 16.7932 mL | |
| 10 mM | 0.3359 mL | 1.6793 mL | 3.3586 mL | 8.3966 mL | |
| 15 mM | 0.2239 mL | 1.1195 mL | 2.2391 mL | 5.5977 mL | |
| 20 mM | 0.1679 mL | 0.8397 mL | 1.6793 mL | 4.1983 mL | |
| 25 mM | 0.1343 mL | 0.6717 mL | 1.3435 mL | 3.3586 mL | |
| 30 mM | 0.1120 mL | 0.5598 mL | 1.1195 mL | 2.7989 mL | |
| 40 mM | 0.0840 mL | 0.4198 mL | 0.8397 mL | 2.0991 mL | |
| 50 mM | 0.0672 mL | 0.3359 mL | 0.6717 mL | 1.6793 mL | |
| 60 mM | 0.0560 mL | 0.2799 mL | 0.5598 mL | 1.3994 mL | |
| 80 mM | 0.0420 mL | 0.2099 mL | 0.4198 mL | 1.0496 mL | |
| 100 mM | 0.0336 mL | 0.1679 mL | 0.3359 mL | 0.8397 mL |
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