Biological Activity
Potent and selective SUV420H1/H2 inhibitor (IC50 values are 25 and 144 nM respectively). Exhibits 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. Inhibits the di- and tri-methylation of H4K20me in multiple cell lines (IC50 < 1 μM).
Licensing Information
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the A-196 probe summary on the SGC website.
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of A196 is reviewed on the Chemical Probes website.
Technical Data
| M. Wt | 359.25 |
| Formula | C18H16Cl2N4 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1982372-88-2 |
| Smiles | ClC1=CC2=C(C(C3=CC=NC=C3)=NN=C2NC4CCCC4)C=C1Cl |
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 | 7.18 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 359.25. 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 | 2.78 mL | 13.92 mL | 27.84 mL |
| 5 mM | 0.56 mL | 2.78 mL | 5.57 mL |
| 10 mM | 0.28 mL | 1.39 mL | 2.78 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Bromberg et al (2017) The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity. Nat.Chem.Biol. 13 317 PMID: 28114273
Keywords: A 196, supplier, A196, methyltransferases, histones, inhibitors, inhibits, HMTs, MLL, leukemia, mll-rearranged, H4K20me, potent, selective, Lysine, Methyltransferases, Tocris Bioscience
