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

Chemical Structure : IGGi-11

CAS No.: 303059-39-4

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IGGi-11

货号: PC-20013Not For Human Use, Lab Use Only.

IGGi-11 is a first-in-class small molecule inhibitor of non-canonical activation of heterotrimeric G-protein signaling, binds to G-protein α-subunits (Gαi, Gαi3 ITC Kd=4 uM), 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-11 is a first-in-class small molecule inhibitor of GIV-dependent G-protein cell signaling, binds to G-protein α-subunits (Gαi, Gαi3 ITC Kd=4 uM), specifically disrupts their engagement with GIV/Girdin.
    IGGi-11 did not interfere with canonical G-protein signaling mechanisms triggered by GPCRs.
    IGGi-11 also blocked GIV binding to Gαi3 in FP assays with an inhibition constant (Ki) of ~14 μM, and similar activity for the other two Gα proteins of Gi family: Gαi1 and Gαi2.
    IGGi-11 also inhibited the ability of GIV to promote the steady-state GTPase activity of Gαi3, which reports increased nucleotide exchange in vitro. IGGi-11 does not affect GIV-independent aspects of G-protein regulation and function.
    GIV/Girdin has emerged as a prototypical non-GPCR activator of G proteins that promotes cancer metastasis.
    IGGi-11 has low membrane permeability because IGGi-11 contains two negatively charged carboxylate groups, and pro-drug IGGi-11me could be used for cellular function assays.

    物理化学性质&存储条件

    分子量 524.60
    分子式 C23H28N2O8S2
    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

    4,4'-((9H-fluorene-2,7-disulfonyl)bis(methylazanediyl))dibutyric acid

    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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