2. Apoptosis Stem Cell/Wnt MAPK/ERK Pathway
  3. Apoptosis YAP ERK
  4. GQ127

GQ127 is an orally active Gαq/11 inhibitor with an IC50 of 22.6 μM. GQ127 binds directly to Gαq/11 protein and inhibits its activity. GQ127 induces Apoptosis, suppresses viability, migration and invasion of uveal melanoma cells. GQ127 increases the phosphorylation level of YAP and decreases the phosphorylation level of ERK. GQ127 inhibits the growth of uveal melanoma xenografts in mouse models. GQ127 can be used for research related to uveal melanoma.

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GQ127

GQ127 Chemical Structure

CAS No. : 2625582-70-7

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GQ127 Related Antibodies

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Description

GQ127 is an orally active Gαq/11 inhibitor with an IC50 of 22.6 μM. GQ127 binds directly to Gαq/11 protein and inhibits its activity. GQ127 induces Apoptosis, suppresses viability, migration and invasion of uveal melanoma cells. GQ127 increases the phosphorylation level of YAP and decreases the phosphorylation level of ERK. GQ127 inhibits the growth of uveal melanoma xenografts in mouse models. GQ127 can be used for research related to uveal melanoma[1].

In Vitro

GQ127 (10 μM) potently inhibits Gαq/11-mediated IP1 accumulation in CHO-M1 cells, with an IC50 of 22.6 μM[1].
GQ127 potently inhibits the proliferation of UM 92.1 cells (IC50 = 10.1 μM) and MP41 cells (IC50 = 24.8 μM) in a time- and dose-dependent manner[1].
GQ127 (1.25-20 μM; 24 h) exhibits low cytotoxicity against CHO-M1 cells, with no reduction in cell viability observed after 24 h of treatment at concentrations below 20 μM[1].
GQ127 (5-30 μM; 48 h) induces apoptosis in UM 92.1 and MP41 cells in a dose-dependent manner[1].
GQ127 (5-30 μM; 48 h) significantly inhibits the migration of UM 92.1 and MP41 cells after treatment at concentrations of 15 μM and higher for 48 h[1].
GQ127 (5-30 μM; 48 h) inhibits Gαq/11-mediated tumorigenesis in UM 92.1 and MP41 cells by increasing the phosphorylation level of YAP and decreasing the phosphorylation level of ERK[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GQ127 Related Antibodies

Apoptosis Analysis[1]

Cell Line: uveal melanoma (UM) 92.1 cells, uveal melanoma (UM) MP41 cells
Concentration: 5 μM, 15 μM (92.1 cells); 15 μM, 30 μM (MP41 cells)
Incubation Time: 48 h
Result: Induced apoptosis of 92.1 cells at rates of 9.48% (5 μM) and 20.1% (15 μM).
Induced apoptosis of MP41 cells at rates of 9.74% (15 μM) and 24.1% (30 μM).
Exhibited a dose-dependent apoptotic effect.

Western Blot Analysis[1]

Cell Line: uveal melanoma (UM) 92.1 cells, uveal melanoma (UM) MP41 cells
Concentration: 5 μM, 15 μM (92.1 cells); 15 μM, 30 μM (MP41 cells)
Incubation Time: 48 h
Result: Enhanced the phosphorylation level of YAP in both 92.1 and MP41 cells at 15 μM and 30 μM.
Inhibited the phosphorylation level of ERK in both 92.1 and MP41 cells at 15 μM and 30 μM.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t MRT0-t Vss CL F
Mice[1] 10 mg/kg i.v. 1.17 h 0.08 h 2608 ng/mL 2136 ng·h/mL 0.93 h 4.53 L/kg 77.9 mL/min/kg /
Mice[1] 30 mg/kg p.o. 1.41 h 0.42 h 2888 ng/mL 5936 ng·h/mL 1.88 h / / 92.6 %
In Vivo

GQ127 (10-30 mg/kg; i.p.; daily; 21 days) exhibits robust dose-dependent antitumor activity in MP41 uveal melanoma xenografts, with a 99.0% TGI at 30 mg/kg and a 65.4% TGI at 10 mg/kg, while showing no severe systemic toxicity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude (nu/nu) (male and female, 6−8 weeks old, 20−25 g, subcutaneous MP41 uveal melanoma patient-derived xenograft model)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: i.p.; daily; 21 days
Result: Achieved a tumor growth inhibition (TGI) of 99.0% at 30 mg/kg.
Achieved a TGI of 65.4% at 10 mg/kg.
Caused no significant changes in mouse body weight during treatment.
Induced no obvious morphological changes in heart, liver, spleen, lung, or kidney tissues via H&E staining.
Promoted phosphorylation of YAP and inhibited phosphorylation of ERK in tumor tissues at both doses.
Molecular Weight

408.58

Formula

C25H36N4O
CAS No.
SMILES

CC[C@@H](C)[C@H](N)C(N1CCN2C([C@@H]1CC3CCCCC3)=NC(C4=CC=CC=C4)=C2)=O
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GQ127 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:

GQ1272625582-70-7GQ 127GQ-127ApoptosisYAPERKYes-associated proteinExtracellular signal regulated kinasesUM 92.1 cellsHEK293-AT1R cellsapoptosisMP41 cellsCHO-M1 cellsmouse modelsGαq/11 proteinsuveal melanoma cellsInhibitorinhibitorinhibit

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