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K-252c
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
K-252c图片
CAS NO:85753-43-1
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议
5mg电议
25mg电议

产品介绍
K-252c，一种从诺卡氏菌属分离的星形孢菌素类似物。
Cas No.85753-43-1
别名孢菌素甙元,Staurosporinone
化学名6,7,12,13-tetrahydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-5-one
Canonical SMILESO=C1C2=C(C3=CC=CC=C3N4)C4=C(NC5=CC=CC=C65)C6=C2CN1
分子式C20H13N3O
分子量311.34
溶解度≥ 15.55mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

K-252c is a cell-permeable, reversible, and ATP-competitive inhibitor of protein kinase C (PKC) and protein kinase A (PKA) with IC50 value of 2.45 μM and 25.7 μM, respectively. This component was inhibits β-lactamase, malate dehydrogenase and chymotrypsin with IC50 values of 8, 8 and 10 μM respectively [1].

Protein kinase is known as kinase enzymes that modify other proteins by chemically adding phosphate groups to them (phosphorylation). Phosphorylation can result in a functional change of the target protein (substrate) by changing enzyme activity, cellular location, or association with other proteins in the cells. PKA and PKC are important family member of AGC kinases.

K-252a was previously shown to block nerve growth factor (NGF)-induced neurite outgrowth and the changes in protein phosphorylation elicited by NGF in PC12h cells [2].

The effect of K-252c was also investigated on the severe combined immunodeficient (SCID) mouse-human skin model of psoriasis. It was shown that psoriasis significantly improved after 2 weeks treatment of K-252c [3].

References:
1.  Fabre S, Prudhomme M, Rapp M. Protein kinase C inhibitors; structure-activity relationships in K252c-related compounds. Bioorg Med Chem 1993,1:193-196.
2.  Hashimoto S. K-252a, a potent protein kinase inhibitor, blocks nerve growth factor-induced neurite outgrowth and changes in the phosphorylation of proteins in PC12h cells. J Cell Biol 1988,107:1531-1539.
3.  Raychaudhuri SP, Sanyal M, Weltman H, Kundu-Raychaudhuri S. K252a, a high-affinity nerve growth factor receptor blocker, improves psoriasis: an in vivo study using the severe combined immunodeficient mouse-human skin model. J Invest Dermatol 2004,122:812-819.