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MLCK inhibitor peptide 18

MLCK抑制肽18
Catalog No.
B5211
肌球蛋白轻链激酶的竞争性抑制剂
组合的产品项目
规格价格库存 数量
1mg
¥ 572.00
现货
5mg
¥ 2,004.00
现货
10mg
¥ 3,665.00
现货

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背景

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.

化学属性

Physical AppearanceA crystalline solid
StorageDesiccate at -20°C
M.Wt1324.64
Cas No.224579-74-2
FormulaC60H105N23O11
Solubility≥58.5 mg/mL in DMSO; ≥45.3 mg/mL in EtOH; ≥49.4 mg/mL in H2O
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-
SDFDownload SDF
Canonical SMILESNCCCC[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
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试验操作

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.

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