ML241 hydrochloride

ML241 hydrochloride

Catalog Number:
L002371444APE
Mfr. No.:
APE-B6122
Price:
$287
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      • Overview
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          Background

          IC50: 100 nMML241 is identified as a p97 ATPase inhibitor.The hexameric p97 protein belongs to the type II AAA (ATPase associated with diverse cellular activities) ATPase protein family and is conserved across all eukaryotes and is essential for lifep97 protein, a member of the type II AAA ATPase protein family, is reported to be conservative for nealy all eukaryotes. p97 is also known as valosin-containing protein and Cdc48p in mammals and yeast, respectively, playing key roles in various cellular processes, such as cell division, homotypic fusion of endoplasmic reticulum and Golgi membranes, as well as autophagosome maturations.In vitro: Both ML241 and its analog ML240 were found to be able to inhibit the degradation of proteasome substrate in a p97-dependent but not a p97-independent manner. ML241 and ML240 could also impaire the endoplasmic-reticulum (ER) associated degradation pathway. ML240 was able to stimulate accumulation of LC3-II potently, inhibit cancer cell growth, and also mobilize the executioner caspases 3 and 7 rapidly, but ML241 was not able to. Further investigation showed that ML240 had broad antiproliferative activity to the NCI-60 panel of cancer cell lines, but lower activity to normal cells. In addition, ML240 could synergize with proteasome inhibitor to inhibit the growth of various colon cancer cell lines. Moreover, both ML241 and ML240 had low off-target activity toward a panel of protein kinases as well as central nervous system targets [1]. In vivo: Currently, there is no animal in vivo data reported. Clinical trial: Up to now, ML241 is still in the preclinical development stage.

      • Properties
        • Alternative Name
          2-(2H-benzo[b][1,4]oxazin-4(3H)-yl)-N-benzyl-5,6,7,8-tetrahydroquinazolin-4-amine hydrochlorid
          CAS Number
          2070015-13-1
          Molecular Formula
          C23H25ClN4O
          Molecular Weight
          408.92
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          ≥40.9 mg/mL in DMSO; insoluble in H2O; ≥48.7 mg/mL in EtOH
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Zhang H, Read C, et al. "The Human Cytomegalovirus Nonstructural Glycoprotein UL148 Reorganizes the Endoplasmic Reticulum." mBio. 2019 Dec 10;10(6). pii: e02110-19. PMID:31822584

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