HK262
HK262 is a METTL21A inhibitor, with an IC50 of 1.10 μM against human METTL21A. HK262 reduces the enzymatic activity of the protein lysine methyltransferase METTL21A. HK262 can be used in studies of hepatocellular carcinoma.
For research use only. We do not sell to patients.
- Formula: C16H15F5N6O4S
- Molecular Weight:482.39
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Histone Methyltransferase Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
METTL21A 1.10 μM (IC50) |
In Vitro
HK262 (compound 6n) is the most potent METTL21A inhibitor identified in this series, with an IC50 of 1.10 μM for the purified recombinant human METTL21A enzyme[1].
HK262 (100 μM; 2 h) displays favorable kinetic solubility of 85 μM in pH 7.4 phosphate-buffered saline[1].
HK262 (120 min) exhibits high stability in both human and mouse plasma following 120 min of incubation[1].
HK262 (45 min) displays high metabolic stability in vitro in both human liver microsomes and mouse liver microsomes after 45 min of incubation[1].
HK262 (50 μM; 60 min) achieves high intracellular accumulation of 1824 μM in HepG2 cells following 60 min of exposure to an initial 50 μM extracellular concentration[1].
HK262 (10 μM; 72 h) does not reduce the viability of HepG2 cells after 72 h of exposure at 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:10 μM
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Incubation Time:72 h
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Result:Resulted in HepG2 cell viability of 102% of the untreated control value after 72 h of exposure, with no observable reduction in cell viability.
Chemical Information
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Molecular Weight 482.39
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Formula C16H15F5N6O4S
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SMILES
O[C@H]1[C@@H](O)[C@H](N2C=NC3=C(N)N=CN=C23)O[C@@H]1C(NC4=CC=C(S(F)(F)(F)(F)F)C=C4)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)