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CAS No.: 521937-07-5

CID755673 Catalog No. CSN13787

Synonyms: CID-755673

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.

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400-920-2911

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实验方案

技术信息

生物活性

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.
动物研究
剂量
Rat: 15 mg/kg^[3] (i.p.); 10 mg/kg (i.v.) Mice: 1 mg/kg, 10 mg/kg^[4] (i.p.)

给药途径
i.p., i.v.
参考文献

动物研究
剂量	Rat: 15 mg/kg^[3] (i.p.); 10 mg/kg (i.v.) Mice: 1 mg/kg, 10 mg/kg^[4] (i.p.)
给药途径	i.p., i.v.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.6036 mL
- 23.0181 mL
- 46.0361 mL
- 5 mM
- 0.9207 mL
- 4.6036 mL
- 9.2072 mL
- 10 mM
- 0.4604 mL
- 2.3018 mL
- 4.6036 mL

技术信息

CAS号

521937-07-5

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H11NO3

运输

蓝冰

分子量

217.22

别名

CID-755673

溶解度

DMSO	50.0 mg/mL (230.2 mM)
Water	insoluble

动物实验配方

2%DMSO+30%peg300+2%t-80+ddawater

6 mg/mL

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