| Identification | Back Directory | [Name]
Deltazinone | [CAS]
894554-89-3 | [Synonyms]
Deltazinone
Deltazinone 1
(Deltazinone1)
6H-Pyrazolo[3,4-d]pyridazine-6-butanamide, 2,7-dihydro-3,4-dimethyl-2-(4-methylphenyl)-7-oxo-N-(2-phenylpropyl)- | [Molecular Formula]
C27H31N5O2 | [MOL File]
894554-89-3.mol | [Molecular Weight]
457.57 |
| Hazard Information | Back Directory | [Description]
Deltazinone is highly potent and selective PDEδ inhibitor. Deltazinone exhibits less unspecific cytotoxicity than the previously reported Deltarasin and demonstrates a high correlation with the phenotypic effect of PDEδ knockdown in a set of human pancreatic cancer cell lines. | [Uses]
Deltazinone 1, a pyrazolopyridazinone, is a highly selective PDEδ inhibitor with a KD of 8?nM. Deltazinone 1 inhibits the PDEδ-Ras interaction. Deltazinone 1 shows a dose-dependent inhibitory response on proliferation in oncogenic KRas-dependent cell lines[1][2]. | [IC 50]
PDEδ: 8 nM (Kd) | [References]
[1] Bj?rn Papke, et al. Identification of pyrazolopyridazinones as PDEδ inhibitors. Nat Commun. 2016 Apr 20;7:11360. DOI:10.1038/ncomms11360
[2] Pablo Martín-Gago, et al. Structure-based development of PDEδ inhibitors. Biol Chem. 2017 May 1;398(5-6):535-545. DOI:10.1515/hsz-2016-0272 |
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