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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
9 Results for "
PLK1 PBD
" in MedChemExpress (MCE) Product Catalog:
Products (9)
9 Results for "PLK1 PBD" in MCE Product Catalog:
Cat. No.: HY-161521
CAS No.: 2991469-21-5
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PLK1-IN-10 (Compound 4Bb) is an orally active PLK1 PBD (polo-box domain) inhibitor. PLK1-IN-10 blocks the interaction of PLK1 with the cell division regulator protein 1 (PRC1) and decreases the protein expression of the CDK1-Cyclin B1 complex. PLK1-IN-10 reacts with glutathione (GSH) to increase cellular oxidative stress, ultimately leading to cell death .
Cat. No.: HY-129265
CAS No.: 321695-37-8
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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.
Cat. No.: HY-188141
CAS No.: 3057557-03-3
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Allopole-A is a Plk1 inhibitor with an IC50 of 1.4-2.5 μM against human Plk1 PBD1. Allopole-A binds to the allosteric W-F pocket in Plk1 PBD1, displacing the L2 loop, thereby disrupting water-mediated phospho-ligand binding interactions and promoting inhibitory interactions between the kinase domain and PBD to suppress Plk1 kinase activity. Allopole-A can be used in studies of human cancers with plk1 overexpression .
Cat. No.: HY-125220
CAS No.: 2248068-54-2
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Poloppin II is an orally active PBD inhibitor that blocks the binding of phosphopeptide substrates to PLK1/PLK2 PBD, with IC50 values of 41 µM and 105 µM for human PLK1/PLK2 PBD, respectively. Poloppin II binds to PLK4 PBD to inhibit PLK4-dependent mitotic functions. Poloppin II can be used in research on kras-mutant colorectal cancer .
Cat. No.: HY-180990
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Cat. No.: HY-183427
CAS No.: 2660138-04-3
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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 .
Cat. No.: HY-187593
CAS No.: 1186496-84-3
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PLHSpT is an inhibitor of the Polo-box domain (PBD) of Polo-like kinase 1 (Plk1), with an IC50 of 36 μM. It binds to the PB1-PB2 cleft of the Plk1 PBD to block its interaction with phosphoprotein substrates, thereby inducing mitotic arrest and apoptosis in tumor cells. PLHSpT exerts antiglioma effects when delivered via liposomes, and it is applicable to research on glioblastoma multiforme and other human cancers .
Cat. No.: HY-W162436
CAS No.: 29115-34-2
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MCC1019 is a selective PLK1 PBD inhibitor with an IC50 of 16.4 μmol/L. MCC1019 inactivates the AKT signaling pathway in cancer cells, and induces Apoptosis, Necroptosis and Autophagy. MCC1019 exhibits anticancer activity against lung cancer and prostate cancer .
Cat. No.: HY-12135
CAS No.: 1239513-63-3
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Poloxipan is a pan-specific polo-like kinase (PLK) inhibitor that can inhibit a non-catalytic region at the C-terminus called the Polo-box domain (PBD) found in kinases. The IC50 values for Poloxipan against the PBDs of PLK-1/2/3 are 3.2 μM, 1.7 μM, and 3.0 μM, respectively. Poloxipan also inhibits other phospho-tyrosine binding domains, such as the forkhead-associated (FHA) domain of CHK-2, the WW domain of peptidyl-prolyl cis/trans isomerase (PIN1), and the phospho-tyrosine binding domains of STAT1/3/5 and lymphocyte-specific protein tyrosine kinase's SH2 domain. Poloxipan can be used in cancer research .
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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
