GPR30 inhibitor G1 chemical structure
Chemical structureResearch use only
CAT. NO. DC11705Featured

GPR30 inhibitor G1

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Product overview

Description & Application

A potent and selective GPER/GPR30 agonist with Ki of 11 nM, EC50 of 2 nM; displays no activity at ERα and ERβ at concentrations up to 10 uM; increases cytosolic Ca2+ and inhibits migration of SKBr3 cells and MCF-7 cells in response to chemoattractants with IC50 of 0.7 and 1.6 nM respectively; induces cell cycle arrest, DNA damage and cell death by the activation of the intrinsic apoptotic mechanism in H295R cells.

ParameterValue
Chemical NameG-1
CAS No.881639-98-1
SynonymsG-1;(±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone;1-[4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]ethanone;rel-1-[(3aR,4S,9bS)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]ethanone (ACI);G 1;G 1 (Anti-tumor agent);G1
FormulaC21H18BrNO3
M.Wt412.276525020599
SMILESBrC1C=C2OCOC2=CC=1[C@@H]1NC2C=CC(=CC=2[C@@H]2C=CC[C@H]12)C(=O)C
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

A potent and selective GPER/GPR30 agonist with Ki of 11 nM, EC50 of 2 nM; displays no activity at ERα and ERβ at concentrations up to 10 uM; increases cytosolic Ca2+ and inhibits migration of SKBr3 cells and MCF-7 cells in response to chemoattractants with IC50 of 0.7 and 1.6 nM respectively; induces cell cycle arrest, DNA damage and cell death by the activation of the intrinsic apoptotic mechanism in H295R cells.

In Vitro

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In Vivo

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References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

Product documentation

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Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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