Deltazinone 1

Research use only, not for human use.

Deltazinone 1 (Deltazinone1)?is a novel highly selective PDEδ inhibitor that inhibits PDEδ/Ras interaction with Kd of 8±4 nM.

Deltazinone 1 (Deltazinone1)?is a novel highly selective PDEδ inhibitor that inhibits PDEδ/Ras interaction with Kd of 8±4 nM; displays excellent selectivity against a broad panel of pharmacologically relevant proteins; inhibits the PDEδ-Ras interaction in in-cell measurement with Kd of 58±17 nM, exhibits less unspecific cytotoxicity than Deltarasin in a set of human pancreatic cancer cell lines, including KRas mutation and oncogenic KRas-dependence, decreases Ras-mediated signalling in pancreatic cancer cells.

Cell Viability Assay Cell Line:Panc-Tu-I, MIA PaCa-2, Capan-1 cells Concentration:0.375, 0.75, 1.5, 3, 6, 12, 24 μM Incubation Time:0-120 h Result:Inhibited cell growth in a dose-dependent manner already observable at sub-μM concentrations. At doses higher than 3?μM decreasing cell indices indicated cell death ～30?h in Panc-Tu-I cells and after ～40?h in MIA PaCa-2. Doses up to 24?μM led to strong growth inhibition but not cell death in the Capan-1 cell line.Western Blot Analysis Cell Line:Panc-Tu-I cells Concentration:20?μM Incubation Time:1?hResult:Reduced S6P phosphorylation in the KRas-dependent Panc-Tu-I cells.

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Deltazinone1

MAPK/ERK Signaling

Ras

Ras

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894554-89-3

457.578

C27H31N5O2

>98% (HPLC)

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O=C(NCC(C1=CC=CC=C1)C)CCCN2N=C(C)C3=C(C)N(C4=CC=C(C)C=C4)N=C3C2=O

4-(3,4-dimethyl-7-oxo-2-(p-tolyl)-2,7-dihydro-6H-pyrazolo[3,4-d]pyridazin-6-yl)-N-(2-phenylpropyl)butanamide

(-20℃)

With Ice Pack

≥ 2 years