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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Plasminogen Activator Inhibitor-1 (PAI-1)-WX-340
WX-340

Chemical Structure : WX-340

CAS No.:

WX-340 (WX340, Cyclo21,29 [D-Cys21 Cys29]-uPA21-30)

货号: PC-49100Not For Human Use, Lab Use Only.

WX-340 is a highly specific and selective, peptidic cyclic competitive inhibitor of urokinase-type plasminogen activator (uPA) with Ki of 12 and 170 nM for human and mouse uPA, respectively, inhibits 10 Units of human uPA with IC50 of 90 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    WX-340 is a highly specific and selective, peptidic cyclic competitive inhibitor of urokinase-type plasminogen activator (uPA) with Ki of 12 and 170 nM for human and mouse uPA, respectively, inhibits 10 Units of human uPA with IC50 of 90 nM.
    WX-340 blocks uPA‐PAI‐1 heteromerization, significantly increases the proliferation of 4T1 cells.
    WX‐340 significantly reduces neutrophil trafficking to the neoplasms already on the level of intravascular adherence in the tumor microvaculature.
    WX-340 reduces cell adhesion and invasiveness in a dose-dependent manner in anaplastic thyroid carcinoma (ATC) derived cell lines, CAL-62 and BHT-101, WX-340 increases uPA receptor (uPAR) protein levels without affecting its plasma membrane concentration.
    WX-340 (10 mg/kg, i.p.) prolonged (p<0.05) survival of animal modesl of amyotrophic lateral sclerosis (ALS), as well as improving rotarod performance.

    物理化学性质&存储条件

    分子量 1275.465
    分子式 C58H78N14O15S2
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    ((4R,7R,10S,13S,16S,19S,22S,25S,28S)-28-amino-10,25-bis(2-amino-2-oxoethyl)-22-(4-aminobutyl)-16-benzyl-7-((S)-sec-butyl)-19-(4-chlorobenzyl)-13-(hydroxymethyl)-6,9,12,15,18,21,24,27-octaoxo-1,2-dithia-5,8,11,14,17,20,23,26-octaazacyclononacosane-4-carbonyl)-L-tryptophan

    参考文献

    1. Glas M, et al. Exp Neurol. 2007 Oct;207(2):350-6.

    2. Serratì S, et al. Arthritis Rheum. 2011 Sep;63(9):2584-94.

    3. Bernd Uhl, et al. EMBO Mol Med. 2021 Jun 7;13(6):e13110.

    4. Baldini E, et al. Int J Mol Sci. 2022 Mar 28;23(7):3724.

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