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CID755673 {[allProObj[0].p_purity_real_show]}

货号:A539848

CID-755673 is a potent and selective cell-active small molecule inhibitor for PKD with an IC50 of 182 nM and exhibits selective PKD1 inhibition when compared with AKT, PLK1, CAK, CAMKIIα, and PKC isoforms.

CID755673 化学结构 CAS号:521937-07-5
CID755673 化学结构
CAS号:521937-07-5
CID755673 3D分子结构
CAS号:521937-07-5
CID755673 化学结构 CAS号:521937-07-5
CID755673 3D分子结构 CAS号:521937-07-5
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CID755673 纯度/质量文件 产品仅供科研

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CID755673 生物活性

靶点
  • PKD

    PKD2, IC50:227 nM

    PKD1, IC50:180 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.

CID755673 动物研究

Dose Rat: 15 mg/kg[3] (i.p.); 10 mg/kg (i.v.) Mice: 1 mg/kg, 10 mg/kg[4] (i.p.)
Administration i.p., i.v.

CID755673 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.

CID755673 实验方案

计算器
存储液制备 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

CID755673 技术信息

CAS号521937-07-5
分子式C12H11NO3
分子量 217.221
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

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

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