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Referencia número: HY-182405

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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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No. CAS: 2625582-70-7
Fòrmula: C₂₅H₃₆N₄O
Peso molecular:408.58

Almacenamiento:

Please store the product under the recommended conditions in the Certificate of Analysis.

GQ127 Chemical Structure

No. CAS: 2625582-70-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
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Actividad biológica

Descripciòn

Ver todos los productos específicos de isoformas YAP :

Ver todos los productos específicos de isoformas ERK :

Cellular Effect

Cell Line	Type	Value	Description	References
MP41	IC₅₀	24.8 μM Compound: GQ127	Antiproliferative activity against human MP41 cells assessed as inhibition of cell growth after 72 hrs by CCK8 assay Antiproliferative activity against human MP41 cells assessed as inhibition of cell growth after 72 hrs by CCK8 assay	[PMID: 33715360]

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.

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	T_1/2	T_max	C_max	AUC_0-t	MRT_0-t	V_ss	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.

Chemical Information

No. CAS 2625582-70-7
Peso molecular 408.58
Fòrmula C₂₅H₃₆N₄O
SMILES

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

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Ge Y, et al. Design, Synthesis, and Evaluation of Small Molecule Gαq/11 Protein Inhibitors for the Treatment of Uveal Melanoma. J Med Chem. 2021;64(6):3131-3152. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Actividad biológica
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GQ127

Ver todos los productos específicos de isoformas YAP

Ver todos los productos específicos de isoformas ERK

Actividad biológica

Chemical Information

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Referencias

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GQ127 Related Classifications

HY-182405 Related Classifications