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
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
All Histone Methyltransferase Isoforms
More
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 (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. Further protocols information, click here.
-
Cell Line:HepG2 cells
-
Concentration:10 μM
-
Incubation Time:72 h
-
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
-
Molecular Weight 482.39
-
Formula C16H15F5N6O4S
-
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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Liver Cancer Modeling
Liver cancer can be classified into primary liver cancer and secondary liver cancer. Secondary liver cancer is the metastatic liver cancer. Primary liver cancer includes hepatocellular carcinoma (HCC), intrahepatic cholangiocarcinoma (ICC) and fibrolamellar HCC, of which HCC is the most common form, accounting for approximately 90% of primary liver cancers[1]. HCC mouse models include chemical agent-induced models, transplanted tumor models, and genetic engineered models.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HK262 Related Classifications
HY-189248 Related Classifications
Powered by Bioz