| Bioactivity | M-31850 is a potent, selective and competitive β-hexosaminidase (Hex) inhibitor with IC50s of 6.0 µM and 3.1 µM for human HexA and human HexB, respectively. M-31850 also competitively inhibits β-N-acetyl-D-hexosaminidase OfHex2 with a Ki of 2.5 μM[1][2]. |
| Target | IC50: 6.0 µM (human HexA) and 3.1 µM (human HexB). Ki: 2.5 μM (OfHex2) |
| Invitro | M-31850 shows some activity towards Jack Bean Hex (JBHex) and bacterial Hex from Streptomyces plicatus (SpHex) (IC50 of 280 µM and >500 µM for JBHex and SpHex, respectively)[1]. M-31850 produces a dose dependent increase in MUG hydrolysis (Hex S levels) in lysates from treated infantile Sandhoff disease (ISD) cells[1]. M-31850 increases the half-life of the mutant Hex A from Adult forms of Tay-Sachs (ATSD) cells more than two-fold at 44° C, relative to the enzyme heated in the presence of DMSO. M-31850 acts as a classic competitive inhibitor of Hex (Km increases and Vmax is unaffected by increasing amounts of M-31850), with a Ki of 0.8 μM[1]. |
| Name | M-31850 |
| CAS | 281224-40-6 |
| Formula | C28H21N3O4 |
| Molar Mass | 463.48 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [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. |