Chemical Name: 2-Methyl-5-[(4-methylphenyl)amino]-4,7-benzothiazoledione
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Inhibitor of SETD8 protein lysine methyltransferase (PKMT) (IC50 = 0.5 μM); suppresses H4K20 monomethylation in vitro. Also inhibits cyclin-dependent kinase (CDK) 4 (IC50 = 6.0 μM at CDK4/cyclin D1). Induces S phase accumulation in HEK293T cells. Cytotoxic against a range of human cancer cells.
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Technical Data
M. Wt
284.33
Formula
C15H12N2O2S
Storage
Store at +4°C
Purity
≥98% (HPLC)
CAS Number
265312-55-8
PubChem ID
481747
InChI Key
HFPLHASLIOXVGS-UHFFFAOYSA-N
Smiles
CC1=NC2=C(S1)C(=O)C=C(NC1=CC=C(C)C=C1)C2=O
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
5.69
20
ethanol
1.42
5
Preparing Stock Solutions
The following data is based on the product molecular weight 284.33. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
3.52 mL
17.59 mL
35.17 mL
5 mM
0.7 mL
3.52 mL
7.03 mL
10 mM
0.35 mL
1.76 mL
3.52 mL
50 mM
0.07 mL
0.35 mL
0.7 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Ryuet al (2000) 5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents. Bioorg.Med.Chem.Lett. 10 461 PMID: 10743948
Blumet al (2014) Small-molecule inhibitors of SETD8 with cellular activity. ASC.Chem.Biol. [Epub ahead of print] 9 2471 PMID: 25137013