1186496-84-3
Chemical Structure
PLHSpT
- CAS No.: 1186496-84-3
- Formula:C24H40N7O11P
- Molecular Weight:633.59
InChIKey: WXGBWHLFXXMZRD-PFFQMSPKSA-N
SMILES: O=C([C@@H]1CCCN1)N[C@@H](CC(C)C)C(N[C@H](C(N[C@@H](CO)C(N[C@H](C(O)=O)[C@@H](C)OP(O)(O)=O)=O)=O)CC2=CN=CN2)=O
Biological Activity: 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[1][2][3].
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PLHSpT | 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. | |||||||||||||||||||||
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References
- [1]. Berg A, et al. Inhibitors of the Polo-Box Domain of Polo-Like Kinase 1. Chembiochem : a European journal of chemical biology. 2016 Apr 15;17(8):650-6.
- [2]. Liao C, et al. Exploring Potential Binding Modes of Small Drug-like Molecules to the Polo-Box Domain of Human Polo-like Kinase 1. ACS Med Chem Lett. 2010;1(3):110-114.
- [3]. Yim, M, et al. A TAT-conjugated peptide inhibitor of polo-like kinase 1 for in vivo tumor imaging. J Anal Sci Technol 10, 26 (2019).
