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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1186496-84-3
- 分子式: C24H40N7O11P
- 分子量:633.59
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
PLK1 PBD 36 μM (IC50) |
体外実験
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.
化学情報
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CAS 番号 1186496-84-3
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分子量 633.59
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分子式 C24H40N7O11P
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配列
Pro-Leu-His-Ser-{pThr}
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シーケンスの短縮
PLHS-{pThr}
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
PLHSpT 関連分類
HY-187593 関連分類
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