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首页-小分子抑制剂&激动剂-Others-Small GTPase-PREX-in1
PREX-in1

Chemical Structure : PREX-in1

CAS No.: 674801-27-5

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PREX-in1 (P-Rex inhibitor 1)

货号: PC-20881Not For Human Use, Lab Use Only.

PREX-in1 is a specific small-molecule inhibitor of P-Rex1 and P-Rex2 Rac-GEF activity with IC50 of 4.5 uM (P-Rex1 DHPH Rac-GEF activity) in liposome-based GEF assay, inhibits P-Rex1 and P-Rex2 through their catalytic DH domain.

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

    生物&药学活性

    PREX-in1 is a specific small-molecule inhibitor of P-Rex1 and P-Rex2 Rac-GEF activity with IC50 of 4.5 uM (P-Rex1 DHPH Rac-GEF activity) in liposome-based GEF assay, inhibits P-Rex1 and P-Rex2 through their catalytic DH domain.
    PREX-in1 is selective for P-Rex1 and P-Rex2 over a panel of other Rho-GEFs.
    PREX-in1 (10 uM) inhibits PIP3-stimulated Rac-GEF activity of full-length P-Rex1 and P-Rex2 in liposome-based in vitro GEF activity assay.
    PREX-in1 also inhibits P-Rex1 in the mant-GTP assay (IC50=10 uM), but not EHop-016.
    PREX-in1 inhibits P-Rex Rac-GEFs, but not a selection of other Rho-GEFs.
    PREX-in1 (10 uM) affects the cell cycle in a similar manner to NSC23766, induces cell death in HEK-293 cells.
    PREX-in1 (1 uM) inhibits the P-Rex1-dependent spreading of endothelial cells in response to PDGF stimulation.
    PREX-in1 (1 uM) inhibits the P-Rex1 dependent production of ROS in mouse neutrophils stimulated with the chemoattractant fMLP.

    物理化学性质&存储条件

    分子量 444.88
    分子式 C24H17ClN4O3
    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

    6-amino-4-(5-(4-chlorophenyl)furan-2-yl)-3-(4-methoxyphenyl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile

    参考文献

    1. C D Lawson, et al. Small GTPases. 2022 Jan;13(1):307-326.

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