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Chemical Structure| 2280037-51-4 Chemical Structure| 2280037-51-4

Structure of Bobcat339
CAS No.: 2280037-51-4

Chemical Structure| 2280037-51-4

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Bobcat339 is a potent and selective cytosine-based TET enzyme inhibitor, with IC50 values of 33 μM and 73 μM for TET1 and TET2, respectively. It is valuable in epigenetics research and serves as a starting point for developing new therapeutics targeting DNA methylation and gene transcription.

Synonyms: BC339

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Product Details of Bobcat339

CAS No. :2280037-51-4
Formula : C16H12ClN3O
M.W : 297.74
SMILES Code : ClC(C(N)=N1)=CN(C2=CC(C3=CC=CC=C3)=CC=C2)C1=O
Synonyms :
BC339
MDL No. :MFCD32644557
InChI Key :QMGYGOOYCNTEQO-UHFFFAOYSA-N
Pubchem ID :138319673

Safety of Bobcat339

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of Bobcat339

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
PCBC-CMs 150 μM 14 days AA significantly increased MLC2v expression in PCBC-CMs and promoted hiPSC-CMs maturation through DNA demethylation. PMC10334833
DP3-CMs 150 μM 14 days AA significantly increased MLC2v expression in DP3-CMs and promoted hiPSC-CMs maturation through DNA demethylation. PMC10334833
MLC2v-CMs 150 μM 14 days AA significantly increased MLC2v expression in MLC2v-CMs and promoted hiPSC-CMs maturation through DNA demethylation. PMC10334833
RA induced atrial-like PCBC-CMs 150 μM 14 days AA significantly increased MLC2v expression in RA induced atrial-like PCBC-CMs and promoted hiPSC-CMs maturation through DNA demethylation. PMC10334833
Swine Scattered Tubular-like Cells (STCs) 10μM 24 hours Bobcat339 decreased the expression of inflammatory genes in RAS-STCs and reduced the protein expression of pro-inflammatory cytokines TNF-α, IL-6, and IF-γ. PMC10644845
HT-22 cells 10 μM 24 hours To evaluate the ability of Bobcat339 to reduce 5hmC levels in live cells, results showed that Bobcat339 significantly reduced global 5hmC levels PMC6378777
KGN cells 40 nM 24 hours To explore the reversal effect of Bobcat339 on Fer-1 in Hcy-induced KGN cell injury PMC8867468
Porcine oocytes 100 µM, 200 µM, 400 µM 24 hours, 36 hours, 44 hours Bobcat339 treatment significantly reduced the first polar body extrusion rate and triggered early apoptosis. PMC10419807
MCF-7 33 µM and 75 µM 24, 48, and 72 hours Bobcat339 was able to revert IL-1β-induced proliferation of MCF-7 cells and inhibit IL-1β-induced accelerated wound closure. PMC9741332
Porcine oocytes 200 µM 44 hours Bobcat339 treatment caused abnormal spindle architecture and chromosome alignment. PMC10419807
SH-SY5Y cells 10 μM 48 hours Bobcat339 stimulated the expression of AGRP, NPY, and SLC32A1 in a TET3-dependent manner PMC10120042
Human monocyte-derived macrophages (MDMs) 10 μM 48 hours Bobcat339 induces TET3 degradation, leading to apoptosis in TET3-overexpressing macrophages. PMC11527447
Mouse RAW 264.7 macrophages 10 μM 48 hours Bobcat339 induces TET3 degradation, leading to apoptosis in TET3-overexpressing macrophages. PMC11527447
Huh-7 cells 40 µM 48 hours Bobcat339 significantly reduced the expression of DNA repair-related genes PMC11335208
Huh-7 cells 80 µM 48 hours Bobcat339 significantly reduced the expression of DNA repair-related genes PMC11335208
Hep3B cells 50 μM 48 hours To assess the effect of Bobcat339 on 5hmC levels in Hep3B cells, results showed that Cu(II)-contaminated MedKoo-Bobcat339 significantly reduced 5hmC levels, while Sigma-Bobcat339 did not show a reduction in 5hmC levels. PMC9109264
GT1-7 cells 10 μM 6 hours Bobcat339 decreased TET3 protein levels without affecting its mRNA expression PMC10120042

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice activity-based anorexia (ABA) model intraperitoneal injection 2.5 mg/kg once a week for 3 weeks Bobcat339 increased food intake, decreased compulsive running, and diminished lethality in the ABA model by reducing TET3 protein expression in AgRP neurons PMC10120042
Mice Endometriosis model Intraperitoneal injection 3 mg/kg Once a week for 6 weeks Bobcat339 significantly reduced the volume of endometriosis lesions and decreased the number of TET3-overexpressing macrophages in the lesions by degrading TET3. PMC11527447
BALB/c Nude mice HCC model intraperitoneal injection 2.5 mg/kg every 2 days for 3 weeks Combined treatment with Bobcat339 and sorafenib almost completely halted HCC growth PMC11335208
Pig Parthenogenetic embryos In vitro culture 25 µM, 50 µM, 100 µM Cultured until day 6 Bobcat339 treatment significantly reduced the blastocyst rate of parthenogenetic embryos and arrested embryo growth at the 4-cell stage. PMC10419807

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.36mL

0.67mL

0.34mL

16.79mL

3.36mL

1.68mL

33.59mL

6.72mL

3.36mL

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