SML2186
Poloppin
≥98% (HPLC)
别名:
5-(4-Bromophenyl)-1-[2-(trifluoromethyl)phenyl]-1H-pyrrole-2-propanoic acid, Polo protein-protein interaction inhibitor
InChI
1S/C20H15BrF3NO2/c21-14-7-5-13(6-8-14)17-11-9-15(10-12-19(26)27)25(17)18-4-2-1-3-16(18)20(22,23)24/h1-9,11H,10,12H2,(H,26,27)
InChI key
OCUKOJUZSNFVFQ-UHFFFAOYSA-N
SMILES string
OC(CCC1=CC=C(C2=CC=C(Br)C=C2)N1C3=CC=CC=C3C(F)(F)F)=O
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
Poloppin is a cell penetrant and potent inhibitor of mitotic Polo-like kinases (PLKs) that binds to the Polo-box domain (PBD) and prevents PLKs interaction with pSer/pThr phosphopeptide substrates. Poloppin induces mitotic arrest and apoptosis in cancer cells expressing mutant KRAS in 2D and organoid cultures. It also sensitizes mutant KRAS-expressing cancer cells to Crizotinib.
cell penetrant and potent inhibitor of PLKs that binds to the Polo-box domain (PBD) and prevents PLKs interaction with phosphopeptide substrates
存储类别
11 - Combustible Solids
wgk
WGK 3
Ana J Narvaez et al.
Cell chemical biology, 24(8), 1017-1028 (2017-08-16)
Mutations activating KRAS underlie many forms of cancer, but are refractory to therapeutic targeting. Here, we develop Poloppin, an inhibitor of protein-protein interactions via the Polo-box domain (PBD) of the mitotic Polo-like kinases (PLKs), in monotherapeutic and combination strategies to
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