NEKs Inhibitor

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.

PPARγ agonist-21 (Compound 9a) is a PPARγ agonist with an EC₅₀ of 3.12 μM. PPARγ agonist-21 activates PPAR-γ to inhibit NF-κB and attenuate NLRP3 inflammasome assembly. PPARγ agonist-21 blocks NLRP3-ASC and NLRP3-NEK7 interaction. PPARγ agonist-21 attenuates the severity of gouty arthritis.

PLK1-IN-17 is a potent PLK1 inhibitor with an IC₅₀ of 2 nM. PLK1-IN-17 shows high selectivity for PLK2 and CDK2/A, moderate selectivity for PLK3, only weak activity against CK2, FLT3 and NEK6, and no activity against PDGFR, ALK and another 37 kinases. PLK1-IN-17 inhibits the proliferation of ovarian cancer cells and can be used in ovarian cancer-related research.

MBM-55 (Standard) is the analytical standard of MBM-55 (HY-101029). This product is intended for research and analytical applications. MBM-55 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55 shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice.

CK7 (Standard) is the analytical standard of CK7 (HY-103646). This product is intended for research and analytical applications. CK7, a Cdk2/9 inhibitor, can be used for the synthesis of Nek1 inhibitor BSc5231 and BSc5367.