Deltazinone 1

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Deltazinone 1, a pyrazolopyridazinone, is a highly selective PDEδ inhibitor with a K_D 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.

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Deltazinone 1 Chemical Structure

CAS No. : 894554-89-3

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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Purity & Documentation
References
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Description

IC₅₀ & Target^[2]

PDEδ

8 nM (Kd)

In Vitro

Deltazinone 1 (0.375-24 μM; 0-120 h) inhibits cell growth in a dose-dependent manner^[1].
Deltazinone 1 (20 μM; 1 h) reduces S6P phosphorylation in the KRas-dependent Panc-Tu-I cells^[1].
Deltazinone 1 (10 μM) shows cell death for oncogenic KRas-dependent Panc-Tu-I cells but not for oncogenic KRas-independent PANC-1 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

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^[1]

Cell Line:	Panc-Tu-I cells
Concentration:	20 μM
Incubation Time:	1 h
Result:	Reduced S6P phosphorylation in the KRas-dependent Panc-Tu-I cells. Did not significantly affect Erk response to EGF.

Molecular Weight

457.57

Formula

C₂₇H₃₁N₅O₂

CAS No.

894554-89-3

SMILES

CC1=CC=C(N2C(C)=C(C(C)=NN(CCCC(NCC(C)C3=CC=CC=C3)=O)C4=O)C4=N2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Björn Papke, et al. Identification of pyrazolopyridazinones as PDEδ inhibitors. Nat Commun. 2016 Apr 20;7:11360. [Content Brief]

[2]. Pablo Martín-Gago, et al. Structure-based development of PDEδ inhibitors. Biol Chem. 2017 May 1;398(5-6):535-545. [Content Brief]

Deltazinone 1 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Deltazinone 1894554-89-3Deltazinone1Deltazinone-1Phosphodiesterase (PDE)pyrazolopyridazinonePDEδPDEδ-RasKRasPanc-Tu-IMIA PaCa-2Capan-1S6PInhibitorinhibitorinhibit

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