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首页-小分子抑制剂&激动剂-Others-Other Targets-IGGi-11me
IGGi-11me

Chemical Structure : IGGi-11me

CAS No.:

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IGGi-11me

货号: PC-20014Not For Human Use, Lab Use Only.

IGGi-11me is a specific, cell-active small molecule inhibitor of GIV-dependent G-protein cell signaling, binds to G-protein α-subunits, specifically disrupts their engagement with GIV/Girdin.

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

    生物&药学活性

    IGGi-11me is a specific, cell-active small molecule inhibitor of GIV-dependent G-protein cell signaling, binds to G-protein α-subunits, specifically disrupts their engagement with GIV/Girdin.
    IGGi-11me was converted to IGGi-11 (Cat# PC-20013) by esterases present in the cytosol of MDA-MB-231 cells.
    IGGi-11me specifically inhibits GIV-dependent cancer cell signaling reduced the phosphorylation of Akt at S473 (pAkt) upon EGF stimulation in MDA-MB-231 (IC50=16 uM) and HeLa cells, but not in GIV-depleted cells.
    IGGi-11me does not affect GIV-independent G-protein cell signaling.
    IGGi-11me specifically inhibits GIV-dependent tumor cell migration, IGGi-11me was approximately four times more potent inhibiting the migration of MDA-MB-231 cells (GIVHigh) than of MCF-7 cells (GIVLow).
    IGGi-11me inhibits growth of MDA-MB-231 breast cancer invasive cells, but not of non-transformed MCF-10A cells.
    IGGi-11me inhibits MDA-MB-231 cell tumor growth and metastatic invasion in NCr nu/nu athymic nude mice.

    物理化学性质&存储条件

    分子量 552.66
    分子式 C25H32N2O8S2
    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

    dimethyl 4,4'-((9H-fluorene-2,7-disulfonyl)bis(methylazanediyl))dibutyrate

    参考文献

    1. Jingyi Zhao, et al. Small-molecule targeting of GPCR-independent non-canonical G protein signaling inhibits cancer progression. bioRxiv. 2023 Feb 19;2023.02.18.529092.

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