Description
Product Usage Information
ML-241 is supplied as a lyophilized powder. For a 15 mM stock, reconstitute 5 mg of powder in 0.89 mL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.
Storage
Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 4 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles .
Background
ML-241 is an inhibitor of valosin-containing protein (VCP, p97), which is part of an ATPase protein complex that regulates several critical cellular processes, including the proteasomal degradation of ubiquitinated proteins and autophagosome maturation. ML-241 inhibits VCP (IC of approximately 100 nM), blocks degradation of p97-dependent proteasome substrates (IC of approximately 3,500 nM), and impairs the endoplasmic reticulum (ER)-associated degradation pathway (1). VCP forms a hexamer with a pair of ATPase domains (D1 and D2) and an N-terminal domain that binds numerous cofactor proteins. Both ML-241 and the related inhibitor ML-240 specifically bind the D2 ATPase domain, while a second pair of inhibitors (DBeQ and NMS-873) are capable of binding and inhibiting both D1 and D2 ATPase domains (2). The p47 cofactor of VCP is shown to attenuate ML-241 inhibition of VCP by a factor of approximately 50-fold (3).
Alternate Names
CID49830260; N-Benzyl-2-(2,3-dihydro-1,4-benzoxazin-4-yl)-5,6,7,8-tetrahydroquinazolin-4-amine
