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Chemical Structure : IGGi-11
Catalog No.: 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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IGGi-11 is a first-in-class small molecule inhibitor of 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.
| M.Wt | 524.60 | |
| Formula | C23H28N2O8S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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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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