M-31850 是一种竞争性的 β-己糖胺酶选择性抑制剂,能够抑制人HexA (IC50:6.0 μM) 及HexB (IC50:3.1 μM)。它还能够竞争性抑制 β-N-acetyl-D-hexosaminidaseOfHex2 (Ki:2.5 μM)。
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M-31850 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.
体外活性
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.M-31850 shows some activity towards Jack Bean Hex (JBHex) and bacterial Hex from Streptomyces plicatus (SpHex) (IC50 of 280 M and >500 M for JBHex and SpHex, respectively)[1]
Cas No.
281224-40-6
分子式
C28H21N3O4
分子量
463.493
别名
1H-Benz[de]isoquinoline-1,3(2H)-dione, 2,2'-(iminodi-2,1-ethanediyl)bis-;M-31850
储存和溶解度
DMSO:5 mg/mL (10.79 mM),ultrasonic and adjust pH to 6 with HCl
Powder: -20°C for 3 years
In solvent: -80°C for 2 years