CAS NO: | 224579-74-2 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Desiccate at -20°C |
M.Wt | 1324.64 |
Cas No. | 224579-74-2 |
Formula | C60H105N23O11 |
Solubility | Soluble to 1 mg/ml in sterile water |
Chemical Name | (S,Z)-6-amino-N-((S,Z)-1-(((S,Z)-1-(((S,Z)-1-(((S)-6-amino-1-hydroxy-1-iminohexan-2-yl)imino)-5-guanidino-1-hydroxypentan-2-yl)imino)-5-guanidino-1-hydroxypentan-2-yl)imino)-1-hydroxy-3-(4-hydroxyphenyl)propan-2-yl)-2-((Z)-((6S,7Z,9S,10Z,12S,13Z,15S)-1,6- |
Canonical SMILES | NCCCC[C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](N)([H])CCCNC(N)=N)([H])CCCCN)([H])CCCCN)([H])CC1=CC=C(O)C=C1)([H])CCCCN)([H])CC2=CC=C(O)C=C2)([H])CCCNC(N)=N)([H])CCCNC(N)=N)([H])C(O)=N |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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。溶液形式一般不宜长期储存,请尽快用完。 |
MLCK inhibitor peptide 18 is a cell-permeable inhibitor of MLCK (IC50 = 50 nM), with 4000-fold selectivity for MLCK over another closely related calmodulin (CaM)-regulated protein kinase, CaM-dependent kinase II (CaMPKII). MLCK inhibitor peptide 18 can cross cell membrane, and regulate paracellular permeability by reducing intracellular MLC phosphorylation, with the potential to restore barrier function in intestinal disease states. In addition, MLCK inhibitor peptide 18 can also inhibit chromosome-mediated cortical reorganization in mouse oocytes, as well as complement receptor-3 (CR3) mediated phagocytosis of C3bi-opsonized zymosan by mouse microglia.
References:
1. Lukas TJ, Mirzoeva S, Slomczynska U, et al. Identification of novel classes of protein kinase inhibitors using combinatorial peptide chemistry based on functional genomics knowledge. Journal of Medicinal Chemistry, 1999, 42(5): 910-919.
2. Zolotarevsky Y, Hecht G, Koutsouris A, et al. A membrane-permeant peptide that inhibits MLC kinase restores barrier function in in vitro models of intestinal disease. Gastroenterology, 2002, 123(1): 163-172.
3. Deng M, Williams CJ, Schultz RM. Role of MAP kinase and myosin light chain kinase in chromosome-induced development of mouse egg polarity. Developmental Biology, 2005, 278(2): 358-366.
4. Gitik M, Reichert F, Rotshenker S. Cytoskeleton plays a dual role of activation and inhibition in myelin and zymosan phagocytosis by microglia. The FASEB Journal, 2010, 24(7): 2211-2221.
Cell experiment:[2] | |
Cell lines | Escherichia coli-infected T84 monolayers, as well as TNF-α and IFN-γ stimulated Caco-2 monolayers |
Reaction Conditions | 330 μM MLCK inhibitor peptide 18 |
Applications | MLCK inhibitor peptide 18 prevented defects in transepithelial barrier resistance induced by bacteria or TNF-α plus IFN-γ. Moreover, MLCK inhibitor peptide 18 effectively reduced MLC phosphorylation triggered by TNF-α and IFN-γ. |
Note | The technical data provided above is for reference only. |
References: 1. Lukas TJ, Mirzoeva S, Slomczynska U, et al. Identification of novel classes of protein kinase inhibitors using combinatorial peptide chemistry based on functional genomics knowledge. Journal of Medicinal Chemistry, 1999, 42(5): 910-919. 2. Zolotarevsky Y, Hecht G, Koutsouris A, et al. A membrane-permeant peptide that inhibits MLC kinase restores barrier function in in vitro models of intestinal disease. Gastroenterology, 2002, 123(1): 163-172. 3. Deng M, Williams CJ, Schultz RM. Role of MAP kinase and myosin light chain kinase in chromosome-induced development of mouse egg polarity. Developmental Biology, 2005, 278(2): 358-366. 4. Gitik M, Reichert F, Rotshenker S. Cytoskeleton plays a dual role of activation and inhibition in myelin and zymosan phagocytosis by microglia. The FASEB Journal, 2010, 24(7): 2211-2221. |