Cas No.: | 484049-04-9 |
Chemical Name: | 5-(3-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl)imidazolidine-2,4-dione |
Synonyms: | 5-(3-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl)imidazolidine-2,4-dione;DPH;5-[3-(4-fluorophenyl)-1-phenylpyrazol-4-yl]imidazolidine-2,4-dione;5-[3-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl]-2,4-imidazolidinedione;5-[3-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl]imidazolidine-2,4-dione;HMS2301N21;5-(1,3-diaryl-1H-pyrazol-4-yl)hydantoin |
SMILES: | O=C1NC(C(N1)C2=CN(N=C2C3=CC=C(C=C3)F)C4=CC=CC=C4)=O |
Formula: | C18H13N4O2F |
M.Wt: | 336.31982 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | A cell-permeable, small-molecule c-Abl kinase activator with pEC50 of 6.1(EC50=794 nM); binds to the myristoyl binding site, also stimulates in vitro c-Abl phosphorylation; induces both pY245 (pEC50=5.6) and pY412 c-Abl phosphorylation; dose dependently induces Crk-L pY207 in KG-1 cells; the first small-molecule tool compound for c-Abl activation. |
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. |