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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
138 Results for "
PLK1
" in MedChemExpress (MCE) Product Catalog:
Products (138)
138 Results for "PLK1" in MCE Product Catalog:
185
185 Publications Verification
Synonyms: SL-2052; KY-12420
63
63 Cited Publications
Cat. No.: HY-50698
CAS No.: 755038-02-9
Domaines de recherche:
BI 2536 is a dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively [1]. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription .
40
Target:
Domaines de recherche:
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 [1] .
40
Target:
Domaines de recherche:
Volasertib (BI 6727) trihydrochloride is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib trihydrochloride inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models [1] .
37
37 Cited Publications
Cat. No.: HY-16954
CAS No.: 1818885-28-7
Target:
PROTACs Epigenetic Reader Domain c-Myc Polo-like Kinase (PLK) CDK JAK STAT Pim Bcl-2 Family PAK Wnt β-catenin Caspase PARP Reactive Oxygen Species (ROS) Apoptosis
Domaines de recherche:
ARV-825 is a BET protein PROTAC degrader that recruits cereblon, and it targets BRD2, BRD3, and BRD4 for degradation via the ubiquitin-proteasome pathway. ARV-825 downregulates c-MYC, PLK1, MYCN, CDK4/6, JAK2, pSTAT3/5, PIM1, and Bcl-xL, upregulates p21 and p27, and modulates H3K27Ac-mediated transcription, the G2/M checkpoint, the Wnt/β-catenin pathway, and amino acid transport pathways. ARV-825 induces G1 phase cell cycle arrest, caspase 3/PARP-mediated apoptosis, DNA damage, and reactive oxygen species (ROS) production, reduces mitochondrial respiration, and simultaneously inhibits cell proliferation, clonogenic growth, and cell migration. ARV-825 is used in research on gastric cancer, leukemia, neuroblastoma, and cholangiocarcinoma [1] .
31
31 Cited Publications
Synonyms: PF-00299804 hydrate; PF-299804 hydrate
Domaines de recherche:
Dacomitinib hydrate (PF-00299804 hydrate; PF-299804 hydrate) is an orally active irreversible pan-ERBB receptor tyrosine kinase inhibitor with inhibitory activity against HER1/EGFR, HER2, and HER4 . Dacomitinib hydrate exerts antitumor effects in various tumor cells, inhibiting tumor cell proliferation, migration, and invasion, inducing cell cycle arrest and apoptosis, regulating the expression of molecules related to the cell cycle, apoptosis, and epithelial-mesenchymal transition, and it can also reverse partial drug resistance, producing synergistic effects when combined with chemotherapy. Dacomitinib hydrate inhibits key signaling pathways such as PI3K‑AKT‑mTOR and PLK1‑FOXM1. Dacomitinib hydrate ameliorates pathological changes associated with pulmonary arterial hypertension in rats. Dacomitinib hydrate can be used in research on breast cancer, bladder cancer, epithelial ovarian cancer, and pulmonary arterial hypertension [1] .
31
31 Cited Publications
Synonyms: PF-00299804; PF-299804
Domaines de recherche:
Dacomitinib (PF-00299804; PF-299804) is an orally active irreversible pan-ERBB receptor tyrosine kinase inhibitor with inhibitory activity against HER1/EGFR, HER2, and HER4 . Dacomitinib exerts antitumor effects in various tumor cells, inhibiting tumor cell proliferation, migration, and invasion, inducing cell cycle arrest and apoptosis, regulating the expression of molecules related to the cell cycle, apoptosis, and epithelial-mesenchymal transition, and it can also reverse partial drug resistance, producing synergistic effects when combined with chemotherapy. Dacomitinib inhibits key signaling pathways such as PI3K‑AKT‑mTOR and PLK1‑FOXM1. Dacomitinib ameliorates pathological changes associated with pulmonary arterial hypertension in rats. Dacomitinib can be used in research on breast cancer, bladder cancer, epithelial ovarian cancer, and pulmonary arterial hypertension [1] .
22
Target:
Domaines de recherche:
GSK461364 is a selective, reversible and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with a Ki value of 2.2 nM.
21
21 Cited Publications
Domaines de recherche:
CC-885, a cereblon (CRBN) modulator, acts as a molecular glue degrader targeting GSPT1 with a Kd of 350 nM. CC-885 binds to CRBN to alter the substrate specificity of the CRL4 E3 ligase, promoting the ubiquitination and proteasomal degradation of GSPT1, BNIP3L, PLK1, CDK4, IKZF1/3, GSPT2, WIZ, CHD7, GOLM1, CK1α and ETS1. CC-885 induces apoptosis, cell cycle arrest, transcriptional downregulation and antiproliferation in cancer cells. CC-885 is applicable to research related to relapsed/refractory acute myeloid leukemia, MYC-driven tumors, metastatic castration-resistant prostate cancer, multiple myeloma, hepatocellular carcinoma, glioblastoma, VHL-deficient clear cell renal cell carcinoma and non-small cell lung cancer [1] .
10
10 Cited Publications
Synonyms: NMS-1286937; NMS-P937
Target:
Domaines de recherche:
NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with an IC50 of 2 nM.
8
Target:
Domaines de recherche:
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.
6
Target:
Domaines de recherche:
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 [1] . Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM .
6
6 Cited Publications
Synonyms: ON-01910 sodium
Target:
Domaines de recherche:
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 [1] . Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM .
5
5 Cited Publications
Target:
Domaines de recherche:
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 [1] .
4
4 Cited Publications
Target:
Domaines de recherche:
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.
4
4 Cited Publications
Target:
Domaines de recherche:
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 [1].
4
Target:
PROTACs FKBP Epigenetic Reader Domain HDAC Histone Methyltransferase c-Myc Polo-like Kinase (PLK) Ras MHC
Domaines de recherche:
FKBP12 PROTAC dTAG-7 (dTAG-7) is a FKBP12 F36V PROTAC degrader. FKBP12 PROTAC dTAG-7 binds FKBP12 F36V and CRBN to form a complex, mediating degradation via the ubiquitin-proteasome system. FKBP12 PROTAC dTAG-7 mediates the degradation of FKBP12 F36V-tagged nuclear and cytoplasmic proteins, including BRD4, HDAC1, EZH2, MYC, PLK1, KRAS G12V, and antigen fusion proteins. FKBP12 PROTAC dTAG-7 enhances MHC class I antigen presentation. FKBP12 PROTAC dTAG-7 is applicable to leukemia-related research [1] .
3
Target:
Domaines de recherche:
HMN-214, an orally bioavailable proagent of HMN-176, is an inhibitor of polo-like kinase-1 (plk1), with antitumor activity.
3
3 Cited Publications
Target:
Domaines de recherche:
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.
3
3 Cited Publications
Cat. No.: HY-P76550
Pureté: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: PLK1; STPK13; Prev. PLK; Cell Cycle Regulated Protein Kinase; Serine/Threonine-Protein Kinase PLK1; Polo-Like Kinase (Drosophila); Polo-Like Kinase 1; Polo (Drosophia)-Like Kinase; Serine/Threonine-Protein Kinase 13; Polo Like Kinase 1; PLK-1
Species:
Human
Source:
Sf9 insect cells
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
