2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Polo-like Kinase (PLK)
  5. PLK1 Isoform

PLK1

PLK1 is a serine/threonine Polo-like kinase that orchestrates cell division through mitotic entry, spindle-pole functions, and cytokinesis[1]. Mechanistically, mammalian PLK1 controls centrosome maturation, spindle assembly, and microtubule attachment to kinetochores in early mitosis[2]. This mitotic role makes PLK1 relevant to cancer biology, because dysfunction may promote cancerous transformation and drive progression, and overexpression occurs in diverse human cancers with poor prognosis[3]. Compared with related isoforms, PLK1-PLK4 participate in cell-cycle processes, but reported functional emphasis differs: PLK2 and PLK4 regulate centriole duplication, PLK3 regulates DNA replication, and PLK1 regulates centrosome separation and maturation[4]. For experimental applications, PLK1 inhibition provides a direct way to perturb mitosis, because BI 2536 inhibits mammalian PLK1 at low nanomolar concentrations, induces mitotic arrest and apoptosis in human cancer cell lines, and inhibits human tumor xenograft growth in nude mice[5].

PLK1 관련 제품 (54):

Cat. No. 상품명 효과 Purity
  • HY-12137
    Volasertib
    		Inhibitor 99.97%
    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.
  • HY-50698
    BI 2536
    		Inhibitor 99.95%
    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.
  • HY-15828
    Onvansertib
    		Inhibitor 99.86%
    NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with an IC50 of 2 nM.
  • HY-50877
    GSK461364
    		Inhibitor 99.82%
    GSK461364 is a selective, reversible and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with a Ki value of 2.2 nM.
  • HY-12037A
    Rigosertib
    		Inhibitor 99.01%
    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. Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM.
  • HY-179560
    PMV6-PEG4-BI2536
    		Inhibitor 98.47%
    PMV6-PEG4-BI2536 is a p53-Y220C-PLK1 dual-functional compound, composed of a high-affinity p53-Y220C mutant binder (Kd ≈ 2.5 nM) and a potent PLK1 kinase inhibitor (IC50 = 0.83 nM). PMV6-PEG4-BI2536 triggers TP53Y220C cell G2/M arrest and apoptosis through PLK1 mislocalization and kinase inhibition, independent of p53 transcriptional reactivation. PMV6-PEG4-BI2536 can be used for the study of TP53 mutant cancers.
  • HY-180989
    PROTAC PLK1 Degrader-2
    		Degrader 99.48%
    PROTAC PLK1 Degrader-2 (Compound NC1) is a PLK1 PROTAC degrader with an Kd of 6.06 μM. PROTAC PLK1 Degrader-2 significantly inhibits the proliferation of HeLa cells, induces cell cycle arrest and apoptosis. PROTAC PLK1 Degrader-2 exhibits significant anti-tumor activity in a HeLa cell xenograft tumor mouse model. PROTAC PLK1 Degrader-2 can be used for the study of cervical cancer.
  • HY-181000
    PROTAC PLK1 Degrader-3
    		Degrader
    PROTAC PLK1 Degrader-3 (Compound DD-1) is a PLK1 PROTAC degrader based on the N-deglycosylation pathway, with a Kd value of 2.2 μM. The cell penetration ability of PROTAC PLK1 Degrader-3 is limited and a higher concentration is required to achieve significant degradation effects. PROTAC PLK1 Degrader-3 can be used for research on non-small cell lung cancer.
  • HY-100789
    ON1231320
    		Inhibitor 99.90%
    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.
  • HY-12045
    HMN-214
    		Inhibitor 99.94%
    HMN-214, an orally bioavailable proagent of HMN-176, is an inhibitor of polo-like kinase-1 (plk1), with antitumor activity.
  • HY-15160
    TAK-960
    		Inhibitor 99.75%
    TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
  • HY-11003
    GW843682X
    		Inhibitor 99.89%
    GW843682X is a selective, ATP-competitive inhibitor of PLK1 and PLK3, with IC50s of 2.2 nM and 9.1 nM, respectively, and is also >100-fold selective against ～30 other kinases.
  • HY-15161
    Ro3280
    		Inhibitor 99.46%
    Ro3280 is a potent, highly selective inhibitor of PLK1 with an IC50 and a Kd of 3 nM and 0.09 nM, respectively, and nearly has no effect on PLK2 and PLK3.
  • HY-15155
    MLN0905
    		Inhibitor 99.94%
    MLN0905 is a potent, orally active Polo-like kinase 1 (PLK1) inhibitor. MLN0905 has inhibitory potency against PLK1 with an IC50 value of 2 nM. MLN0905 can be used for the research of cancer.
  • HY-12037
    Rigosertib sodium
    		Inhibitor 99.57%
    Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle. Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM.
  • HY-W286743
    Nε-(Carboxymethyl)-L-lysine
    		Activator 99.70%
    Nε-(Carboxymethyl)-L-lysine (CML) is an orally active advanced glycation end product. Nε-(Carboxymethyl)-L-lysine upregulates the expression of PLK1 and CEP20, and induces the activation of RAGE and ERK/NFκB. Nε-(Carboxymethyl)-L-lysine drives centrosome amplification. Nε-(Carboxymethyl)-L-lysine induces malignant transformation of hepatocytes and promotes the development of hepatocellular carcinoma. Nε-(Carboxymethyl)-L-lysine induces epithelial-mesenchymal transition in osteosarcoma cells and enhances their migration and invasion properties.
  • HY-108597
    TC-S 7005
    		Inhibitor 99.68%
    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.
  • HY-12134
    Poloxin
    		Inhibitor 98.05%
    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.
  • HY-N0885
    Telocinobufagin
    		Inhibitor 99.93%
    Telocinobufagin (Telobufotoxin; Telocinobufogenin) is an orally active bufadienolide with potential anti-tumor effects. Telocinobufagin exerts its anti-cancer effects on non-small cell carcinoma, osteosarcoma, thyroid cancer, breast cancer and head and neck squamous cell carcinoma by inhibiting the STAT3, JAK2/STAT3, LARP1-mTOR, PI3K/Akt/Snail and PLK1 pathways, and can also induce tumor cell apoptosis. Telocinobufagin enhances the Th1 immune response and protects against Salmonella typhimurium infection. Telocinobufagin has a strong cardiac-stimulating effect by inhibiting the activity of Na+/K+-ATPase, and it can promote renal fibrosis. Telocinobufagin demonstrates non-opioid analgesic effects in various acute pain models.
  • HY-147298
    Plogosertib
    		Inhibitor 98.59%
    Plogosertib (CYC140) is a selective, potent, and orally active ATP-competitive PLK1 inhibitor (IC50: 3 nM). Plogosertib is an anti-cancer agent with anti-proliferative activity. Plogosertib can be used in the research of several tumors, including esophageal, gastric, leukemia, non–small cell lung cancer, ovarian, and squamous cell cancers.
Cat. No. 상품명 / Synonyms Application Reactivity