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CID755673

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Chemical Structure| 521937-07-5 同义名 : -
CAS号 : 521937-07-5
货号 : A539848
分子式 : C12H11NO3
纯度 : 99%+
分子量 : 217.221
MDL号 : MFCD03828155
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(483.38 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2%DMSO+30%peg300+2%t-80+ddawater 6 mg/mL

生物活性
靶点

  • PKD

    PKD1, IC50:180 nM

    PKD2, IC50:227 nM
描述 CID755673 is the first potent and selective cell-active small molecule PKD inhibitor with IC50 value of 182nM for inhibition of PKD1 enzyme activity. Pretreatment with CID755673 for 45min at 50μM blocked PMA-induced endogenous PKD1 activation shown by phosphorylation at Ser742 and Ser916 in LNCaP cells. Further study showed that CID755673 inhibited the known biological actions of PKD1 including PMA- induced class IIa histone deacetylase 5 nuclear exclusion, vesicular stomatitis virus glycoprotein transport from the Golgi to the plasma membrane, and the ilimaquinone-induced Golgi fragmentation. Significant inhibition of prostate cancer cell proliferation, cell migration, and invasion could be observed post treatment with 25μM CID755673. Treatment with CID755673 at concentration ranging in 10-200μM indeed resulted in a significant dose-dependent reduction of NK cell degranulation markers and cytokine release in freshly isolated Peripheral blood mononuclear cell populations from healthy blood donors.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.60mL

0.92mL

0.46mL

23.02mL

4.60mL

2.30mL

46.04mL

9.21mL

4.60mL
参考文献

[1]Sharlow ER, Giridhar KV, et al. Potent and selective disruption of protein kinase D functionality by a benzoxoloazepinolone. J Biol Chem. 2008 Nov 28;283(48):33516-26.

[2]Scheiter M, Bulitta B, et al. Protein Kinase Inhibitors CK59 and CID755673 Alter Primary Human NK Cell Effector Functions. Front Immunol. 2013 Mar 18;4:66.