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K-252c

现货
Catalog No.
A8344
蛋白激酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 3,300.00
现货
1mg
¥ 1,040.00
现货
5mg
¥ 4,000.00
现货
25mg
¥ 10,000.00
现货

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Background

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt311.34
Cas No.85753-43-1
FormulaC20H13N3O
SynonymsStaurosporinone
Solubility≥15.55mg/mL in DMSO
Chemical Name6,7,12,13-tetrahydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-5-one
SDFDownload SDF
Canonical SMILESO=C1C2=C(C3=CC=CC=C3N4)C4=C(NC5=CC=CC=C65)C6=C2CN1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

生物活性

描述 K-252c是蛋白激酶C(PKC)的细胞渗透性抑制剂,IC50值为2.45 μM。
靶点 PKC PKA        
IC50 2.45 μM 25.7 μM        

质量控制

化学结构

K-252c