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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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[2]

PDEδ

8 nM (Kd)

Cellular Effect

Cell Line	Type	Value	Description	References
CAPAN-1	IC₅₀	48 μM Compound: 2	Antiproliferative activity against KRAS-dependent human Capan1 cells after 48 hrs by CCK8 assay Antiproliferative activity against KRAS-dependent human Capan1 cells after 48 hrs by CCK8 assay	[PMID: 29510040]
CAPAN-1	IC₅₀	56.9 μM Compound: S2	Antiproliferative activity against KRAS-dependent human Capan1 cells after 48 hrs by CCK8 assay Antiproliferative activity against KRAS-dependent human Capan1 cells after 48 hrs by CCK8 assay	[PMID: 28929751]
HCT-116	IC₅₀	74 μM Compound: 2	Antiproliferative activity against human HCT116 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HCT116 cells incubated for 72 hrs by CCK8 assay	[PMID: 32603594]
HCT-116	IC₅₀	82.4 μM Compound: 1	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition and measured after 72 hrs by CCK8 assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition and measured after 72 hrs by CCK8 assay	[PMID: 35178186]
SW480	IC₅₀	18.3 μM Compound: 1	Antiproliferative activity against human SW480 cells assessed as cell growth inhibition and measured after 72 hrs by CCK8 assay Antiproliferative activity against human SW480 cells assessed as cell growth inhibition and measured after 72 hrs by CCK8 assay	[PMID: 35178186]
SW480	IC₅₀	56 μM Compound: 2	Antiproliferative activity against human SW480 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human SW480 cells incubated for 72 hrs by CCK8 assay	[PMID: 32603594]

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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