SML1071
ML240
≥98% (HPLC)
别名:
2-(2-Amino-1H-benzimidazol-1-yl)-8-methoxy-N-(phenylmethyl)-4-quinazolinamine, CID-49830258
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关于此项目
经验公式（希尔记法）:
C23H20N6O
化学文摘社编号:
分子量:
396.44
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
InChI
1S/C23H20N6O/c1-30-19-13-7-10-16-20(19)27-23(28-21(16)25-14-15-8-3-2-4-9-15)29-18-12-6-5-11-17(18)26-22(29)24/h2-13H,14H2,1H3,(H2,24,26)(H,25,27,28)
SMILES string
NC1=NC2=C(C=CC=C2)N1C3=NC4=C(OC)C=CC=C4C(NCC5=CC=CC=C5)=N3
InChI key
NHAMBLRUUJAFOY-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
, white to yellow to light brown
solubility
DMSO: 5 mg/mL, clear (warmed)
storage temp.
2-8°C
Quality Level
相关类别
Application
ML240 has been used as an inhibitor of D2 ATPase activity of valosin-containing protein.
Biochem/physiol Actions
ML240 is a selective, ATP-competetive inhibitor of AAA ATPase p97, also called valosine containing protein (VCP).
ML240 is a selective, ATP-competetive inhibitor of AAA ATPase p97, also called valosine containing protein (VCP). The IC50 for p97 inhibition is 110 nM. ML240 rapidly induces activity of Caspases 3 and 7, leading to apoptosis. ML240 has potent antiproliferative activity towards NCI-60 cancer cell lines.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Specific mutations in the D1?D2 linker region of VCP/p97 enhance ATPase activity and confer resistance to VCP inhibitors.
Bastola P, et al.
Cell Death & Disease, 3, 17065-17065 (2017)
Feng Wang et al.
ChemMedChem, 15(8), 685-694 (2020-03-13)
A major challenge of targeted cancer therapy is the selection for drug-resistant mutations in tumor cells leading to loss of treatment effectiveness. p97/VCP is central regulator of protein homeostasis and a promising anticancer target because of its vital role in
Pratikkumar H Vekaria et al.
Leukemia, 33(7), 1675-1686 (2019-01-22)
p97 is an ATPase that works in concert with histone deacetylase 6 (HDAC6), to facilitate the degradation of misfolded proteins by autophagosomes. p97 has also been implicated in DNA repair and maintaining genomic stability. In this study, we determined the
Jasmine Harley et al.
Brain communications, 3(3), fcab166-fcab166 (2021-08-17)
RNA binding proteins have been shown to play a key role in the pathogenesis of amyotrophic lateral sclerosis (ALS). Mutations in valosin-containing protein (VCP/p97) cause ALS and exhibit the hallmark nuclear-to-cytoplasmic mislocalization of RNA binding proteins (RBPs). However, the mechanism
Xiaojun Wu et al.
Cell chemical biology, 27(5), 571-585 (2020-04-04)
Interferon-induced transmembrane protein 3 (IFITM3) is a key interferon effector that broadly prevents infection by diverse viruses. However, the cellular factors that control IFITM3 homeostasis and antiviral activity have not been fully elucidated. Using site-specific photo-crosslinking and quantitative proteomic analysis
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