Home Cart Sign in  
Chemical Structure| 881639-98-1 Chemical Structure| 881639-98-1

Structure of G-1
CAS No.: 881639-98-1

Chemical Structure| 881639-98-1

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

G-1 is a nonsteroidal, high-affinity, selective agonist of GPR30 that binds with a Ki value of 11 nM.

Synonyms: LNS 8801

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Product Citations

Oladimeji Aladelokun ; Lingeng Lu ; Jie Zheng ; Hong Yan ; Abhishek Jain ; Joanna Gibson , et al.

Abstract: Background: Sex-related diferences in colorectal (CRC) incidence and mortality are well-documented. However, the impact of sex on metabolic pathways that drive cancer growth is not well understood. High expression of asparagine synthetase (ASNS) is associated with inferior survival for female CRC patients only. Here, we used a CRISPR/Cas9 technology to generate HCT116 ASNS−/− and HCT 116 ASNS+/+ cancer cell lines. We examine the efects of ASNS deletion on tumor growth and the subsequent rewiring of metabolic pathways in male and female Rag2/IL2RG mice. Results: ASNS loss reduces cancer burden in male and female tumor-bearing mice (40% reduction, q < 0.05), triggers metabolic reprogramming including gluconeogenesis, but confers a survival improvement (30 days median survival, q < 0.05) in female tumor-bearing mice alone. Transcriptomic analyses revealed upregulation of G-protein coupled estrogen receptor (GPER1) in tumors from male and female mice with HCT116 ASNS−/− xenograft. Estradiol activates GPER1 in vitro in the presence of ASNS and suppresses tumor growth. Conclusions: Our study indicates that inferior survival for female CRC patients with high ASNS may be due to metabolic reprogramming that sustains tumor growth. These fndings have translational relevance as ASNS/GPER1 signaling could be a future therapeutic target to improve the survival of female CRC patients.

Keywords: Metabolism ; Colorectal cancer ; ASNS ; GPER1 ; Sex diferences

Purchased from AmBeed:

Alternative Products

Product Details of G-1

CAS No. :881639-98-1
Formula : C21H18BrNO3
M.W : 412.28
SMILES Code : 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
Synonyms :
LNS 8801
MDL No. :MFCD16618392

Safety of G-1

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H302-H319-H332-H372-H400
Precautionary Statements:P260-P264-P270-P273-P280-P301+P312+P330-P304+P312-P305+P351+P338-P314-P337+P313-P391-P501
Class:9
UN#:3077
Packing Group:

Related Pathways of G-1

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
IEC-6 cells 10^-7 mol/L 48 hours or 96 hours To investigate the protective effect of G-1 on 5-FU-induced DNA damage, results showed that G-1 inhibited DNA damage by restoring ERK1/2 activity. Cell Death Dis. 2021 Oct 30;12(11):1034.
A2780 cells 0.5 μM and 1.0 μM 24 hours To evaluate the effect of Shikonin on apoptosis of A2780 cells, results showed that Shikonin significantly increased the apoptosis rate and upregulated Bax protein expression while downregulating Bcl-2 protein expression. Evid Based Complement Alternat Med. 2022 Oct 5;2022:6517732
SKOV3 cells 5 μM and 10 μM 24 hours To evaluate the effect of Shikonin on apoptosis of SKOV3 cells, results showed that Shikonin significantly increased the apoptosis rate and upregulated Bax protein expression while downregulating Bcl-2 protein expression. Evid Based Complement Alternat Med. 2022 Oct 5;2022:6517732
J774A.1 cells 0, 10, 20, 50 μM 1 hour Established an NLRP3 inflammasome activation model to evaluate the effect of DHEA on NLRP3 activation, showing DHEA decreased NLRP3, pro-IL-1β, and pro-caspase-1 protein levels in a dose-dependent manner Cell Death Dis. 2022 Apr 19;13(4):372
J774A.1 cells 50 μM 1 or 4 hours Analyzed the effects of DHEA on inflammatory signals and NLRP3 components expression in LPS-stimulated macrophages, showing DHEA significantly inhibited p-ERK expression level Cell Death Dis. 2022 Apr 19;13(4):372
J774A.1 cells 10-50 μM 12 hours Assessed the effect of DHEA on the viability of J774A.1 cells, showing no cytotoxicity at 50 μM concentration Cell Death Dis. 2022 Apr 19;13(4):372
primary murine retinal microglia 0.1μM 48 hours GPER activation reduced autophagy and increased the viability of hyperoxia-treated primary murine retinal microglia. Aging (Albany NY). 2020 Sep 13;12(17):17367-17379
MCF-7 cells 0.05 μM to 5.0 μM two weeks G-1 inhibited MCF-7 spheroid growth in a time- and concentration-dependent manner, suggesting that G protein-coupled estrogen receptor (GPER) plays a critical role in MCF-7 spheroid growth. J Cancer Ther. 2022 Mar;13(3):117-130

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Single prolonged stress (SPS) model Intraperitoneal injection 5 μg/kg 14 consecutive days G1 improved PTSD-like behaviors in SPS mice by increasing hippocampal GPER1 expression and promoting BDNF/TrkB signaling to repair synaptic and mitochondrial functional impairments CNS Neurosci Ther. 2024 Jul;30(7):e14855

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.43mL

0.49mL

0.24mL

12.13mL

2.43mL

1.21mL

24.26mL

4.85mL

2.43mL

References

 

Historical Records

Categories