Referencia número: HY-111558

Bobcat339

26 Cited Publications

Revisión del cliente

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.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 99.44%
No. CAS: 2280037-51-4
Fòrmula: C₁₆H₁₂ClN₃O
Peso molecular:297.74

Almacenamiento:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Bobcat339 Chemical Structure

No. CAS: 2280037-51-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (26)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

TET1

33 μM (IC₅₀)

TET2

73 μM (IC₅₀)

Ver todos los productos específicos de isoformas DNA Methyltransferase :

Ver todos los productos específicos de isoformas TET Protein :

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	33 μM Compound: Bobcat339	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	[PMID: 30783500]
Sf9	IC₅₀	73 μM Compound: Bobcat339	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	[PMID: 30783500]

In Vitro

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

No. CAS 2280037-51-4
Appearance Solid
Peso molecular 297.74
Fòrmula C₁₆H₁₂ClN₃O
Color Off-white to light yellow
SMILES

NC1=NC(N(C2=CC=CC(C3=CC=CC=C3)=C2)C=C1Cl)=O
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (26)

All WBBio/Physico-chemical AssayIn Vivo Efficacy StudyCell Imaging/StainingHistological Imaging/StainingRT-PCR

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Journal Impact Factor

Nat Metab

Old mitochondria regulate niche renewal via α-ketoglutarate metabolism in stem cells. [Abstract]

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-EGFP^hi 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 ISCs^mito-O (O) and ISCs^mito-Y (Y) supplemented with Bobcat339 for 48 h.
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.
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.
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

TET3 is a regulator and can be targeted for the intervention of myocardial fibrosis. [Abstract]

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.
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
Aquaculture

2023: 739234.

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.
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

TET1-TRPV4 Signaling Contributes to Bone Cancer Pain in Rats. [Abstract]

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
Research Square Print

2023 Mar 14.
Research Square Print

November 29th, 2022.

Solvente y solubilidad

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (8.40 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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.

Protocol 1

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (276 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Bobcat339

26 Cited Publications

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Bobcat339

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Bobcat339

Ver todos los productos específicos de isoformas DNA Methyltransferase

Ver todos los productos específicos de isoformas TET Protein

Actividad biológica

Chemical Information

Publications (26)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Bobcat339

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Bobcat339

Ver todos los productos específicos de isoformas DNA Methyltransferase

Ver todos los productos específicos de isoformas TET Protein

Actividad biológica

Chemical Information

Publications (26)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Bobcat339 Related Classifications

HY-111558 Related Classifications