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SML1071

Sigma-Aldrich

ML240

≥98% (HPLC)

Synonyme(s) :

2-(2-Amino-1H-benzimidazol-1-yl)-8-methoxy-N-(phenylmethyl)-4-quinazolinamine, CID-49830258

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About This Item

Formule empirique (notation de Hill):
C23H20N6O
Numéro CAS:
1346527-98-7
Poids moléculaire :
396.44
Numéro MDL:
MFCD28137687
Code UNSPSC :
12352200
ID de substance PubChem :
329825650
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Couleur

, white to yellow to light brown

Solubilité

DMSO: 5 mg/mL, clear (warmed)

Température de stockage

2-8°C

Chaîne SMILES 

NC1=NC2=C(C=CC=C2)N1C3=NC4=C(OC)C=CC=C4C(NCC5=CC=CC=C5)=N3

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)

Clé InChI

NHAMBLRUUJAFOY-UHFFFAOYSA-N

Application

ML240 has been used as an inhibitor of D2 ATPase activity of valosin-containing protein.

Actions biochimiques/physiologiques

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.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

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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)
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
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
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
Richard S Marshall et al.
Cell, 177(3), 766-781 (2019-04-09)
During autophagy, vesicle dynamics and cargo recruitment are driven by numerous adaptors and receptors that become tethered to the phagophore through interactions with lipidated ATG8/LC3 decorating the expanding membrane. Most currently described ATG8-binding proteins exploit a well-defined ATG8-interacting motif (AIM
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