GSK461364 analogue 1

Cat. No.: HY-111090: Fiche technique Instruction de manipulation
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GSK461364 analogue 1 is a thiophene-based PLK1 inhibitor with a PLK1 IC₅₀ of 2 nM and a PLK3 IC₅₀ of 630 nM. GSK461364 analogue 1 also acts as an inhibitor of Nek2 kinase (IC₅₀: 21 nM). GSK461364 analogue 1 has a solubility of ≥190 μM in pH 7.4 PBS and a human plasma protein binding rate of 91.5%. GSK461364 analogue 1 can be used in studies related to colon cancer, lung cancer, breast cancer and ovarian cancer.

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GSK461364 analogue 1 Chemical Structure

CAS No. : 929095-23-8

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Recommandations en vedette

•Related Small Molecules:

•Related Proteins:

Voir tous les produits spécifiques à Isoform Polo-like Kinase (PLK):

Voir toutes les isoformes

PLK1 PLK2 PLK3 PLK4

Voir tous les produits spécifiques à Isoform NEKs:

Voir toutes les isoformes

NEK1 NEK2 NEK4 NEK6 NEK7

Activité biologique
Pureté et documentation
Références
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Description

IC₅₀ & Target^[1]

PLK1

2 nM (IC₅₀)

PLK3

630 nM (IC₅₀)

NEK2

21 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	11 nM Compound: 25	Antiproliferative activity against human A549 cells after 72 hrs by luminescence-based cell viability assay Antiproliferative activity against human A549 cells after 72 hrs by luminescence-based cell viability assay	[PMID: 19237286]
COLO 205	IC₅₀	5 nM Compound: 25	Antiproliferative activity against human COLO205 cells after 72 hrs by luminescence-based cell viability assay Antiproliferative activity against human COLO205 cells after 72 hrs by luminescence-based cell viability assay	[PMID: 19237286]
HCT-116	IC₅₀	11 nM Compound: 25	Antiproliferative activity against human HCT116 cells after 72 hrs by luminescence-based cell viability assay Antiproliferative activity against human HCT116 cells after 72 hrs by luminescence-based cell viability assay	[PMID: 19237286]
HT-29	IC₅₀	3 nM Compound: 25	Antiproliferative activity against human HT-29 cells after 72 hrs by luminescence-based cell viability assay Antiproliferative activity against human HT-29 cells after 72 hrs by luminescence-based cell viability assay	[PMID: 19237286]
MX1	IC₅₀	9 nM Compound: 25	Antiproliferative activity against human MX1 cells after 72 hrs by luminescence-based cell viability assay Antiproliferative activity against human MX1 cells after 72 hrs by luminescence-based cell viability assay	[PMID: 19237286]
SK-OV-3	IC₅₀	11 nM Compound: 25	Antiproliferative activity against human SKOV3 cells after 72 hrs by luminescence-based cell viability assay Antiproliferative activity against human SKOV3 cells after 72 hrs by luminescence-based cell viability assay	[PMID: 19237286]

In Vitro

GSK461364 analogue 1 (2 h) inhibits the proliferation of HCT116 colorectal cancer cells, with an IC₅₀ of 11 nM^[1].
GSK461364 analogue 1 (72 h) potently inhibits the proliferation of various human tumor cell lines (colon, lung, breast, ovary), with an IC₅₀ value ranging from 3 to 11 nM^[1].

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

Cell Viability Assay^[1]

Cell Line:	COLO205, HT29, A549, MX-1, SKOV-3
Concentration:	/
Incubation Time:	72 h
Result:	Had IC₅₀ of 5 nM (COLO205 ), 3 nM (HT29), 11 nM (A549), 9 nM (MX-1), 11 nM (SKOV-3).

Masse moléculaire

511.04

Formule

C₂₆H₂₇ClN₄O₃S

CAS No.

929095-23-8

SMILES

O(C=1C=C2N(C=NC2=CC1)C3=CC(O[C@H](C)C4=C(Cl)C=CC=C4)=C(C(N)=O)S3)C5CCN(C)CC5

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Emmitte KA, et al. Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding. Bioorg Med Chem Lett. 2009;19(6):1694-1697. [Content Brief]