Biological Activity
High affinity and selective cell-permeable p300/CBP-associated factor (PCAF) inhibitor (Ki = 47 nM). Exhibits no significant activity against a panel of 48 other bromodomains except GCN5 (Kd = 600 nM). Exhibits >4500-fold selectivity for PCAF over BRD4. Also exhibits metabolic stability in mouse and human liver microsomes and no observable cytotoxicity in peripheral blood mononuclear cells (PBMC).
Licensing Information
This compound is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the L-Moses probe summary on the SGC website.
Technical Data
| M. Wt | 433.38 |
| Formula | C21H24N6.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| Smiles | C[C@@H]([C@H](C1=CC=CC=C1)N(C)C)NC2=NN3C(C)=NN=C3C4=CC=CC=C24 |
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
| Solubility | Soluble to 100 mM in water and to 100 mM in DMSO |
Preparing Stock Solutions
The following data is based on the product molecular weight 433.38. 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 | 2.31 mL | 11.54 mL | 23.07 mL |
| 5 mM | 0.46 mL | 2.31 mL | 4.61 mL |
| 10 mM | 0.23 mL | 1.15 mL | 2.31 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Moustakim et al (2017) Discovery of a PCAF bromodomain chemical probe. Angew.Chem.Int.Ed. 56 827 PMID: 27966810
Keywords: L Moses dihydrochloride, supplier, PCAF, p300/CBP-associated, factor, GCN5, general, control, non-derepressible, 5, inhibitors, inhibits, high, affinity, selective, cell-permeable, 2079885-05-3, Bromodomains, Bromodomains, Tocris Bioscience
