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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- CAS No.: 1186496-84-3
- Formule: C24H40N7O11P
- Masse moléculaire:633.59
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
PLK1 PBD 36 μM (IC50) |
In Vitro
PLHSpT binds specifically and with high affinity (KD = 0.445 μM) to the Plk1 PBD, disrupts Plk1 PBD-substrate complexes, and exhibits no significant binding to Plk2 or Plk3 PBDs[1].
PLHSpT inhibits Plk1 PBD binding in an ELISA-based assay with an IC50 of 36 μM[1].
PLHSpT (0.03-300 μM) potently inhibits binding of human Plk1 PBD to the p-T78 motif of PBIP1 with a Kd of 0.445 μM[2].
PLHSpT binds to the polo-like kinase 1 polo-box domain with a Kd of 0.445 μM[3].
PLHSpT induces apoptosis in cancer cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:C6 glioma cells
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Concentration:2.0 μg/mL
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Incubation Time:24 h
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Result:Resulted in the shortest migration distance and lowest migration rate among all PLHSpT-containing formulations for Ang-cubs-(GNA + PLHSpT), followed by cubs-(GNA + PLHSpT), cubs-PLHSpT, and free PLHSpT.
Chemical Information
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CAS No. 1186496-84-3
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Masse moléculaire 633.59
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Formule C24H40N7O11P
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Sequence
Pro-Leu-His-Ser-{pThr}
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Sequence Shortening
PLHS-{pThr}
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PLHSpT Related Classifications
HY-187593 Related Classifications
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