KN-92 phosphate

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Chemical Structure| 1135280-28-2 同义名 : -
CAS号 : 1135280-28-2
货号 : A349509
分子式 : C24H28ClN2O7PS
纯度 : 99%+
分子量 : 554.98
MDL号 : MFCD24369012
存储条件：

Pure form Inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
生物活性
描述 KN-92 phosphate is an inactive derivative of KN-93, without CaM kinase inhibitory activity[3]. Incubation of 10 micromol/L KN-93 induced the cell growth reduction in a time-dependent manner from 78.27% at 8 h to 11.48% at 48 h. However, KN-92, an inactive derivative of KN-93, did not inhibit cell proliferation effectively[4]. Inhibition of Ca2+/calmodulin kinase (KN-63, KN-92; 5 microM) reduced Cl--conductance in 50% of the cells investigated without affecting [Ca2+]i[5]. The CaMKII inhibitor, KN-93 (N-[2-(N-(4-Chlorocinnamyl)-N-methylaminomethyl)phenyl]-N-[2-hydroxyethyl]-4-methoxybenzenesulfonamide), but not the inactive isomer, KN-92 (2-[N-(4-Methoxybenzenesulfonyl)]amino-N-(4-chlorocinnamyl)-N-methylbenzylamine, phosphate), blocked clozapine's augmenting effect on NMDA-evoked responses in pyramidal cells of the rat mPFC. KN-93 also inhibited the facilitatory effect of clozapine on electrically evoked responses in the pyramidal cells, while KN-92 did not show any effect[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.80mL

0.36mL

0.18mL

9.01mL

1.80mL

0.90mL

18.02mL

3.60mL

1.80mL
参考文献

[1]Rokhlin OW, Guseva NV, et al. KN-93 inhibits androgen receptor activity and induces cell death irrespective of p53 and Akt status in prostate cancer. Cancer Biol Ther. 2010 Feb;9(3):224-35.

[2]An P, Zhu JY, et al. KN-93, a specific inhibitor of CaMKII inhibits human hepatic stellate cell proliferation in vitro. World J Gastroenterol. 2007 Mar 7;13(9):1445-8.

[3]Smyth JT, Abbott AL, Lee B, Sienaert I, Kasri NN, De Smedt H, Ducibella T, Missiaen L, Parys JB, Fissore RA. Inhibition of the inositol trisphosphate receptor of mouse eggs and A7r5 cells by KN-93 via a mechanism unrelated to Ca2+/calmodulin-dependent protein kinase II antagonism. J Biol Chem. 2002 Sep 20;277(38):35061-70

[4]An P, Zhu JY, Yang Y, Lv P, Tian YH, Chen MK, Luo HS. KN-93, a specific inhibitor of CaMKII inhibits human hepatic stellate cell proliferation in vitro. World J Gastroenterol. 2007 Mar 7;13(9):1445-8

[5]Strauss O, Steinhausen K, Mergler S, Stumpff F, Wiederholt M. Involvement of protein tyrosine kinase in the InsP3-induced activation of Ca2+-dependent Cl- currents in cultured cells of the rat retinal pigment epithelium. J Membr Biol. 1999 Jun 1;169(3):141-53

[6]Ninan I, Jardemark KE, Liang X, Wang RY. Calcium/calmodulin-dependent kinase II is involved in the facilitating effect of clozapine on NMDA- and electrically evoked responses in the medial prefrontal cortical pyramidal cells. Synapse. 2003 Mar 15;47(4):285-94