GSK461364 analogue 1 

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^[1].

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.

511.04

C₂₆H₂₇ClN₄O₃S

929095-23-8

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

Room temperature in continental US; may vary elsewhere.

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

• [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]