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Merck
CN

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:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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Quality Level

assay

≥98% (HPLC)

form

powder

color

, white to yellow to light brown

solubility

DMSO: 5 mg/mL, clear (warmed)

storage temp.

2-8°C

SMILES string

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)

InChI key

NHAMBLRUUJAFOY-UHFFFAOYSA-N

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



历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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商品

DISCOVER Bioactive Small Molecules for Nitric Oxide & Cell Stress Research


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



全球贸易项目编号

货号GTIN
SML1071-25MG04061833224977
SML1071-5MG04061833224984