Biological Activity
High affinity CBX4 and CBX7 inhibitor (Ki values are 94 and 97 nM, respectively). Exhibits >6-fold selectivity for CBX4/7 over other CBX and CDY family members. Inhibits proliferation of PC3 cells in vitro.
Technical Data
| M. Wt | 795.02 |
| Formula | C43H66N6O8 |
| Storage | Store at -20°C |
| CAS Number | 1872382-47-2 |
| PubChem ID | 101043861 |
| InChI Key | UMRRDXVUROEIKJ-JCXBGQGISA-N |
| Smiles | CCN(CCCC[C@@H](C(N[C@H](C(OC)=O)CO)=O)NC([C@@H](NC([C@@H](NC([C@@H](NC(C1=CC=C(C(C)(C)C)C=C1)=O)CC2=CC=CC=C2)=O)C)=O)CC(C)C)=O)CC |
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 | 79.5 | 100 | |
| ethanol | 15.9 | 20mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 795.02. 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 | 1.26 mL | 6.29 mL | 12.58 mL |
| 5 mM | 0.25 mL | 1.26 mL | 2.52 mL |
| 10 mM | 0.13 mL | 0.63 mL | 1.26 mL |
| 50 mM | 0.03 mL | 0.13 mL | 0.25 mL |
Molarity Calculator
Reconstitution Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
Stuckey et al (2016) A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1. Nat.Chem.Biol. 12 180 PMID: 26807715
Barnash et al (2016) Chromodomain ligand optimization via target-class directed combinatorial repurposing. ACS Chem.Biol. 11 2475 PMID: 27356154
Stuckey et al (2016) Structure-activity relationships and kinetic studies of peptidic antagonists of CBX chromodomains. J.Med.Chem. 59 8913 PMID: 27571219
Keywords: UNC 3866, supplier, UNC3866, high, affinity, CBX4, CBX7, inhibitors, Lysine, Methyltransferases, Lysine, Methyltransferases, Lysine, Methyltransferases, Tocris Bioscience
