Biological Activity
Potent class I and IIb HDAC inhibitor (IC50 values are 7, 20, 40, 100, 110 and 610 nM for HDAC6, HDAC3, HDAC10, HDAC1, HDAC2 and HDAC8, respectively). Suppresses proliferation and induces apoptosis of sarcoma cancer stem cells (CSCs) at concentrations >500 nM. Also induces osteogenesis in sarcoma CSCs at concentrations of 25 - 500 nM.
Technical Data
| M. Wt | 395.47 |
| Formula | C21H21N3O3S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1776116-74-5 |
| PubChem ID | 49769453 |
| InChI Key | AOFVDNFTELWRHV-UHFFFAOYSA-N |
| Smiles | O=C(NC(SCCCCC(NO)=O)=N1)C=C1C(C=C2)=CC=C2C3=CC=CC=C3 |
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 | 39.55 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 395.47. 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 | 2.53 mL | 12.64 mL | 25.29 mL |
| 5 mM | 0.51 mL | 2.53 mL | 5.06 mL |
| 10 mM | 0.25 mL | 1.26 mL | 2.53 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
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References
References are publications that support the products' biological activity.
Di Pompo et al (2015) Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells. J.Med.Chem. 58 4073 PMID: 25905694
Mai et al (2008) Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities. Bioorg.Med.Chem.Lett. 18 2530 PMID: 18381238
Mai et al (2006) Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors. J.Med.Chem. 49 6046 PMID: 17004718
Keywords: MC 1742, supplier, MC1742, HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, HDAC10, inhibitors, inhibits, histone, deacetylases, class, II, IIa, epigenetics, cancer, stem, cells, CSCs, osteogenic, differentiation, Histone, Deacetylases, Cancer, Stem, Cells, Histone, Deacetylases, Tocris Bioscience
