DPH

Names

[ Name ]:
DPH

[Synonym ]:
5-[3-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl]imidazolidine-2,4-dione
HMS2301N21
5-[3-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl]-2,4-imidazolidinedione
DPH

Biological Activity

[Description]:

DPH is a potent cell permeable c-Abl activator, which displays potent enzymatic and cellular activity in stimulating c-Abl activation.

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Bcr-Abl

Research Areas >> Cancer

[In Vitro]

DPH binds to the myristoyl binding site and prevents the formation of the bent conformation of the αI helix through steric hindrance, a mode of action distinct from the previously identified allosteric c-Abl inhibitor, GNF-2, that also binds to the myristoyl binding site. DPH represents the first cell-permeable, small-molecule tool compound for c-Abl activation[1].

[References]

[1]. Yang J, et al. Discovery and characterization of a cell-permeable, small-molecule c-Abl kinase activator that binds to the myristoyl binding site. Chem Biol. 2011 Feb 25;18(2):177-86

[2]. Shapiro LP, et al. Corticosteroid-induced dendrite loss and behavioral deficiencies can be blocked by activation of Abl2/Arg kinase. Mol Cell Neurosci. 2017 Oct 26;85:226-234.

[Related Small Molecules]

Nocodazole | Asciminib | Degrasyn(WP1130) | Bafetinib (INNO-406) | DCC-2036 (Rebastinib) | KW-2449 | AST 487 | PD173955 | XL228 | GNF-2 | GNF-7 | GZD824 | Flumatinib | GNF-5 | Radotinib

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₈H₁₃FN₄O₂

[ Molecular Weight ]:
336.32000

[ Exact Mass ]:
336.10200

[ PSA ]:
83.00000

[ LogP ]:
2.47480

[ Storage condition ]:
2-8℃

MSDS

Click to get detail MSDS

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Articles

Regulation of SREBPs by Sphingomyelin in Adipocytes via a Caveolin and Ras-ERK-MAPK-CREB Signaling Pathway.

PLoS ONE 10 , e0133181, (2015)

Sterol response element binding protein (SREBP) is a key transcription factor in insulin and glucose metabolism. We previously demonstrated that elevated levels of membrane sphingomyelin (SM) were rel...

The direct anti-MRSA effect of emodin via damaging cell membrane.

Appl. Microbiol. Biotechnol. 99 , 7699-709, (2015)

Methicillin-resistant Staphylococcus aureus (MRSA) has become an important bacterium for nosocomial infection. Only a few antibiotics can be effective against MRSA. Therefore, searching for new drugs ...

Antioxidant comparative effects of two grape pomace Mexican extracts from vineyards on erythrocytes.

Food Chem. 194 , 1081-8, (2015)

Maceration and Soxhlet methods were used to obtain methanol extracts from a Mexican grape (Ruby Cabernet) pomace and the biological activity and phenolic profiles were compared. The antioxidant capaci...

DPH