Polo-like Kinase (PLK) Inhibitor

Poloxin-2 is a small molecule Plk1 PBD inhibitor that can effectively induce cell mitotic arrest with an EC50 of approximately 15 μM in HeLa cells. Poloxin-2HT was developed by conjugating a hydrophobic tag (HT) to Poloxin-2, a new application of inhibitors targeting protein-protein interactions. Poloxin-2HT significantly enhanced the effects on cell viability and apoptosis by selectively degrading Plk1 protein, and its effect was stronger than that of untagged Poloxin-2. These data validate hydrophobic tags as a new strategy for targeting and disrupting disease-associated proteins.

KBJK557 is a Plk1 PBD inhibitor with a human-derived IC₅₀ value of 3.05 μM. KBJK577 binds to Plk1 PBD through electrostatic interactions, π-π stacking, hydrogen bonds, salt bridges and hydrophobic interactions, thereby disrupting the subcellular localization and function of Plk1. KBJK557 induces mitotic arrest, S-phase delay, G2/M-phase arrest and apoptosis, and inhibits cancer cell proliferation. KBJK557 can be used in research related to cancer and non-small cell lung cancer.

PLK1-IN-9 (Compound M2) is an inhibitor for polo-like kinase 1 (PLK1), that inhibits PLK proteins modified with peptides 1010pT, cdc25c and PBIP, with IC₅₀s of 1.6, 0.8 and 1.4 μM, respectively. PLK1-IN-9 inhibits proliferations of cancer cells HeLa, HL60, SNU387/499, HepG2, exhibits cytotoxicity and induces apoptosis. PLK1-IN-9 inhibits tumor growth in HepG2 xenograft mouse model.

BI 2536 (Standard) is the analytical standard of BI 2536 (HY-50698). This product is intended for research and analytical applications. BI 2536 is a dual PLK1 and BRD4 inhibitor with IC₅₀s of 0.83 and 25 nM, respectively. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription.

CD 10899 is a hydroxylated metabolite of Volasertib (HY-12137). CD 10899 is pharmacologically active against Polo-like kinase 1 (PLK1) (IC₅₀: 6 nM). Volasertib is an orally active, highly potent and ATP-competitive PLK1 inhibitor. CD 10899 can be used for research of cancer.

ON1231320 (Standard) is the analytical standard of ON1231320 (HY-100789). This product is intended for research and analytical applications. ON1231320 is a highly specific polo like kinase 2 (PLK2) inhibitor with an IC50 of 0.31 μM. ON1231320 blocks tumor cell cycle progression in the G2/M phase in mitosis, causing apoptotic cell death. ON1231320, an arylsulfonyl pyrido-pyrimidinone, has antitumor activity.

Onvansertib (Standard) is the analytical standard of Onvansertib (HY-15828). This product is intended for research and analytical applications. NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with an IC₅₀ of 2 nM.

Volasertib (Standard) is the analytical standard of Volasertib. This product is intended for research and analytical applications. Volasertib (BI 6727) is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib induces mitotic arrest and apoptosis. Volasertib, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models.