M-31850 是一种有效，选择性和竞争性的 β-己糖胺酶 (β-hexosaminidase (Hex)) 抑制剂，对人 HexA 和 HexB 的 IC50 分别为 6.0 µM 和 3.1 µM。M-31850 还以 Ki 为 2.5 μM 来竞争性抑制 β-N-acetyl-D-hexosaminidase OfHex2。
货号:ajcx34928
CAS:281224-40-6
分子式:C28H21N3O4
分子量：463.48
溶解度:DMSO : 5 mg/mL (10.79 mM; ultrasonic and adjust pH to 6 with HCl)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

[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.