ML241 (1346528-06-0) is a potent and selective p97 AAA ATPase inhibitor, IC50=100 nM. Inhibits degradation of a p97-dependent but not p97-independent proteasome substrate in a dual-reporter cell line.1 It impairs the endoplasmic reticulum-associated degradation (ERAD) pathway.1 ML241 and related inhibitors (DBeQ for example) have differential responses to p97 mutants as well as the presence of cofactors suggesting the possibility of context-dependent p97 inhibitors.2,3 ML241(1346528-06-0)是一种有效的选择性p97 AAA atp酶抑制剂,IC50=100 nM。 在双报告细胞系中抑制p97依赖但不独立的蛋白酶体底物的降解 它破坏内质网相关降解(ERAD)途径 ML241和相关抑制剂(如DBeQ)对p97突变体的反应不同,辅助因子的存在表明可能存在环境依赖的p97抑制剂
References/Citations:
1) Chou et al. (2013), Structure-activity relationship study reveals ML240 and ML241 as potent and selective inhibitors of p97 ATPase; Chem. Med. Chem., 8 297 2) Chou et al. (2014) Specific inhibition of p97/VCP ATPase and kinetic analysis demonstrate interaction between D1 and D2 ATPase domains; J. Mol. Biol. 426 2886 3) Fang et al. (2015) Evaluating p97 inhibitor analogues for their domain selectivity and potency against the p97-p47 complex; Chem. Med. Chem. 10 52
CAS:
1346528-06-0
Catalog Number:
10-1555
Activity:
p97 AAA ATPase inhibitor
Chemical Name:
N-Benzyl-2-(2,3-dihydro-1,4-benzoxazin-4-yl)-5,6,7,8-tetrahydroquinazolin-4-amine
Alternate Name:
CID49830260
Molecular Weight:
372.46
Molecular Formula:
C23H24N4O
Solubility:
Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 14 mg/ml with warming).
Physical Properties:
Pale yellow solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
Shipping Code:
RT