2660138-04-3
Chemical Structure
KBJK557
- CAS No.: 2660138-04-3
- Formula:C24H22N6O4
- Molecular Weight:458.47
InChIKey: WEWSXPJRYDQPAO-UHFFFAOYSA-N
SMILES: O=C1NC(/C(C(N1)=O)=C/C2=CN(CCNC(C3=CC=C(NC)C=C3)=O)N=C2C4=CC=CC=C4)=O
Biological Activity: 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[1][2][3][4].
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KBJK557 | 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. | |||||||||||||||||||||
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References
- [1]. Gunasekaran P, et al. Development of a Polo-like Kinase-1 Polo-Box Domain Inhibitor as a Tumor Growth Suppressor in Mice Models. Journal of medicinal chemistry. 2020 Dec 10;63(23):14905-14920. [Content Brief]
- [2]. Stafford JM, et al. Inhibitors of the PLK1 polo-box domain: drug design strategies and therapeutic opportunities in cancer. Expert opinion on drug discovery. 2023 Jan;18(1):65-81. [Content Brief]
- [3]. Jin H, et al. Leveraging the Fragment Molecular Orbital Method to Explore the PLK1 Kinase Binding Site and Polo-Box Domain for Potent Small-Molecule Drug Design. International journal of molecular sciences. 2023 Oct 27;24(21):15639. [Content Brief]
- [4]. Gunasekaran P, et al. An investigation of Plk1 PBD inhibitor KBJK557 as a tumor growth suppressor in non-small cell lung cancer. J Anal Sci Technol. 2022;13:36.
