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ZINC05007751 is a potent NIMA-related kinase NEK6 inhibitor with an IC50 of 3.4 μM. ZINC05007751 shows antiproliferative activity against a panel of human cancer cell lines, and displays a synergistic effect with Cisplatin and Paclitaxel in a BRCA2 mutated ovarian cancer cell line. ZINC05007751 is very selective against NEK1 and NEK6 with no significant activity was observed against NEK2, NEK7, and NEK9.

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ZINC05007751 Chemical Structure

ZINC05007751 Chemical Structure

CAS No. : 591239-68-8

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Based on 1 publication(s) in Google Scholar

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Description

ZINC05007751 is a potent NIMA-related kinase NEK6 inhibitor with an IC50 of 3.4 μM. ZINC05007751 shows antiproliferative activity against a panel of human cancer cell lines, and displays a synergistic effect with Cisplatin and Paclitaxel in a BRCA2 mutated ovarian cancer cell line. ZINC05007751 is very selective against NEK1 and NEK6 with no significant activity was observed against NEK2, NEK7, and NEK9[1].

In Vitro

ZINC05007751 (6 μM-190 μM; 24 hours) inhibits the growth of MDA-MB-231, PEO1, NCI-H1299 and HCT-15 with IC50 below 100 µM[1].
ZINC05007751 induces perturbation of PEO1 cell cycle[1].
ZINC05007751 (ovarian cancer cells PEO1) shows synergism with Cisplatin, resulting in a significant reduction of Cisplatin IC50 from 7.9 to 0.1  µM, with combination ZINC05007751 (44 µM) + Cisplatin (10 µM) exhibiting the greatest synergistic effect[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: MDA-MB-231, PEO1, NCI-H1299 and HCT-15 cells
Concentration: 6 μM-190 μM
Incubation Time: 24 hours
Result: Inhibited the growth of MDA-MB-231, PEO1, NCI-H1299 and HCT-15.
Molecular Weight

304.30

Formula

C18H12N2O3

CAS No.
Appearance

Solid

Color

Brown to black

SMILES

N#CC(C1=O)=C(C)/C(C(N1)=O)=C/C2=CC=C(C3=CC=CC=C3)O2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : 8.33 mg/mL (27.37 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2862 mL 16.4312 mL 32.8623 mL
5 mM 0.6572 mL 3.2862 mL 6.5725 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2862 mL 16.4312 mL 32.8623 mL 82.1558 mL
5 mM 0.6572 mL 3.2862 mL 6.5725 mL 16.4312 mL
10 mM 0.3286 mL 1.6431 mL 3.2862 mL 8.2156 mL
15 mM 0.2191 mL 1.0954 mL 2.1908 mL 5.4771 mL
20 mM 0.1643 mL 0.8216 mL 1.6431 mL 4.1078 mL
25 mM 0.1314 mL 0.6572 mL 1.3145 mL 3.2862 mL
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ZINC05007751 Related Classifications

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  • 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.

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ZINC05007751
Cat. No.:
HY-122639
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