- Cat. No.
- A10134
BI 2536
BI 2536 is a selective inhibitor of Plk1, which inhibits Plk1 enzyme activity at low nanomolar concentrations.
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PLK inhibitors act on polo-like kinases (PLKs), serine/threonine kinases that coordinate mitosis and cytokinesis. The founding gene, polo, was described in Drosophila in 1991 as a protein kinase homolog required for mitosis. In PLK1, the most widely studied human member, a C-terminal polo-box domain (PBD) binds phosphorylated partner proteins and directs the kinase to its sites of action. BI 2536, reported in 2007, competes with adenosine triphosphate (ATP) and arrests cells in prometaphase. Volasertib, GSK461364 and TAK-960 are further ATP-competitive inhibitors used to study PLK1 in mitosis. Poloxin, described in 2008, works differently by blocking protein interactions that depend on the PBD.
BI 2536 is a selective inhibitor of Plk1, which inhibits Plk1 enzyme activity at low nanomolar concentrations.
Synonyms: BI6727
BI6727 is a highly potent and selective polo-like kinase (PLK) 1 inhibitor (enzyme IC50 = 0.87 nM, EC50 = 11-37 nM on a panel of cancer cell lines).
Synonyms: IVX-214
HMN-214 inhibits polo-like and cyclin-dependent kinase activity, has potent antimicrotubular effects and results in profound apoptosis and antitumor activity in a broad spectrum of human xenografts.
GW843682X is a selective inhibitor of polo-like kinase 1 (PLK1) and polo-like kinase 3 (PLK3) (IC50 values are 2.2 and 9.1 nM respectively).
MLN0905 is a potent, selective small-molecule PLK1 inhibitor. MLN0905 inhibits cell proliferation in a broad range of human tumor cells including DLBCL cell lines.
GSK461364 is an ATP-competitive inhibitor of polo-like kinase 1 (Plk1).
Synonyms: Estybon; Novonex; (E/Z)-ON-01910 sodium; (E/Z)-ON-01910
ON-01910 is selectively cytotoxic for chronic lymphocytic leukemia cells through a dual mechanism of action involving PI3K/AKT inhibition and induction of oxidative stress.
TAK-960 is a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity.
Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1) inhibitor that targets the polo-box domain, with an IC50 of appr 4.8 μM.
Poloxime, a hydrolysis product of poloxin, is a non-ATP-competitive Plk1 inhibitor, with moderate Plk1 inhibitory activity.
Synonyms: NMS-P937
NMS-1286937 is an orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity.
RO3280 is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM.
Synonyms: SBE-13
SBE 13 HCl is a selective inhibitor of PLK1 (IC50 values are 200 pM, 875 nM and 66 μM for PLK1, PLK3 and PLK2 respectively).
Synonyms: LFM A13
LFM-A13 is a potent and selective inhibitor of Btk with IC50 of 17.2 uM; also inhibits PLK3 with IC50 of 7.2 uM.
AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3Ser10 phosphorylation and followed by a surge in apoptosis.
TC-S 7005 is a Polo-like kinases (Plks) inhibitor with IC50s of 4 nM, 24 nM and 214 nM for Plk2, Plk3, and Plk1, respectively.
Synonyms: LCR-323
Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM.
Synonyms: LCR-263
Centrinone (LCR-263) is a selective and reversible inhibitor of polo-like kinase 4 (PLK4) with a Ki of 0.16 nM.
SBE13 is a potent and selective Plk1 inhibitor, with an IC50 of 200 pM; SBE13 poorly inhibits Plk2 (IC50>66 μM) or Plk3 (IC50=875 nM).
Synonyms: TAK 960
TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM at 10 μM ATP; TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively.
Synonyms: ON-01910
Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle.
Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC50 and a Kd of 145 nM and 12 nM for Mps1 and a Kd of 61 nM for Plk1.
CFI-400945 is an orally active, potent and selective polo-like kinase 4(PLK4) inhibitor with Ki value of 0.26 nM.
Synonyms: CFI-400437 hydrochloride; CFI-400437 dihydrochloride; CFI-400437
CFI-400437 is a potent and selective inhibitor of polo-like kinase 4 (PLK4).
ON1231320 is a selective inhibitor of polo-like kinase 2 (PLK2), exhibiting an IC50 of 0.31 μM. This compound disrupts tumor cell cycle progression specifically at the G2/M phase during mitosis, leading to apoptotic cell death. The arylsulfonyl pyrido-pyrimidinone structure contributes to its significant antitumor activity, making ON1231320 a valuable tool for research in cancer biology and therapeutic development.