| Description | M-31850 (1H-Benz[de]isoquinoline-1,3(2H)-dione, 2,2'-(iminodi-2,1-ethanediyl)bis-) is a potent, selective and competitive β-hexosaminidase (Hex) inhibitor(human HexA and human HexB with IC50s of 6.0 μM and 3.1 μM, respectively). IT also competitively inhibits β-N-acetyl-D-hexosaminidase OfHex2 with a Ki of 2.5 μM. |
| In vitro | M-31850能够使得成人型Tay-Sachs病(ATSD)细胞中的突变Hex A的半衰期在44°C条件下相比于在DMSO存在下加热的酶增加两倍以上。M-31850作为典型的竞争性抑制剂对Hex产生影响（随着M-31850量的增加Km增加而Vmax不受影响），其Ki为0.8 μM。M-31850对Jack Bean Hex (JBHex)和来自Streptomyces plicatus的细菌Hex (SpHex)也显示出一定的活性（分别对JBHex和SpHex的IC50为280 M和>500 M）[1]。 |
| Target activity | HexB (human):3.1 µM (IC50), HexA (human):6.0 µM (IC50), OfHex2:2.5 μM (Ki) |
| Synonyms | 1H-Benz[de]isoquinoline-1,3(2H)-dione, 2,2'-(iminodi-2,1-ethanediyl)bis- |
| molecular weight | 463.48 |
| Molecular formula | C28H21N3O4 |
| CAS | 281224-40-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 5 mg/mL (10.79 mM), when pH is adjusted to 6 with HCl. Sonication is recommended. |
| References | 1. Michael B Tropak, et al. High-throughput screening for human lysosomal beta-N-Acetyl hexosaminidase inhibitors acting as pharmacological chaperones. Chem Biol. 2007 Feb;14(2):153-64. 2. Qi Chen, et al. Exploring unsymmetrical dyads as efficient inhibitors against the insect β-N-acetyl-D-hexosaminidase OfHex2. Biochimie. 2014 Feb;97:152-62. |