2. GPCR/G Protein PI3K/Akt/mTOR
  3. Adhesion G Protein-coupled Receptors (AGPCRs) PI3K
  4. (3aS,4R,9bR)-G-1

(3aS,4R,9bR)-G-1 is a highly selective G protein-coupled receptor GPR30 (GPER) agonist with a Ki value of approximately 7 nM. (3aS,4R,9bR)-G-1 activates rapid signaling pathways such as intracellular calcium mobilization and PI3K signaling through GPR30, promoting uterine epithelial cell proliferation and exerting antidepressant effects. (3aS,4R,9bR)-G-1 is promising for research of breast cancer and depression.

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(3aS,4R,9bR)-G-1

(3aS,4R,9bR)-G-1 Chemical Structure

CAS No. : 925419-53-0

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Other Forms of (3aS,4R,9bR)-G-1:

(3aS,4R,9bR)-G-1 Related Antibodies

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Description

(3aS,4R,9bR)-G-1 is a highly selective G protein-coupled receptor GPR30 (GPER) agonist with a Ki value of approximately 7 nM. (3aS,4R,9bR)-G-1 activates rapid signaling pathways such as intracellular calcium mobilization and PI3K signaling through GPR30, promoting uterine epithelial cell proliferation and exerting antidepressant effects. (3aS,4R,9bR)-G-1 is promising for research of breast cancer and depression[1].

Cellular Effect
Cell Line Type Value Description References
COS-7 EC50
2 nM
Compound: 1, G-1
Agonist activity at GFP-tagged GPR30 expressed in COS7 cells assessed as half life for increase in intracellular calcium level by spectrofluorimetry
Agonist activity at GFP-tagged GPR30 expressed in COS7 cells assessed as half life for increase in intracellular calcium level by spectrofluorimetry
[PMID: 16520733]
HTLA IC50
2.49412 μM
Compound: EUB0000831a
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
10.6019/CHEMBL5442687
MCF7 IC50
1.6 nM
Compound: 1, G-1
Inhibition of chemoattractant-induced cell migration of human MCF7 cells after 48 hrs by transwell migration assay
Inhibition of chemoattractant-induced cell migration of human MCF7 cells after 48 hrs by transwell migration assay
[PMID: 16520733]
SK-BR-3 IC50
0.7 nM
Compound: 1, G-1
Inhibition of chemoattractant-induced cell migration of human SK-BR-3 cells after 48 hrs by transwell migration assay
Inhibition of chemoattractant-induced cell migration of human SK-BR-3 cells after 48 hrs by transwell migration assay
[PMID: 16520733]
Vero C1008 IC50
>2.0 × 105M
Compound: COVC-3893226076
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
10.6019/CHEMBL4651402
Molecular Weight

412.28

Formula

C21H18BrNO3
CAS No.
SMILES

CC(C1=CC2=C(N[C@@H](C3=C(Br)C=C(OCO4)C4=C3)[C@]5([H])[C@@]2([H])C=CC5)C=C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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(3aS,4R,9bR)-G-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(3aS,4R,9bR)-G-1925419-53-0Adhesion G Protein-coupled Receptors (AGPCRs)PI3KPhosphoinositide 3-kinaseGPERintracellular calcium mobilizationbreast cancerdepressionInhibitorinhibitorinhibit

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