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

GQ127 是一种具有口服活性的 Gαq/11 抑制剂，IC50 为 22.6 μM。GQ127 直接结合 Gαq/11 蛋白，抑制其活性。GQ127 可诱导葡萄膜黑色素瘤细胞凋亡 (Apoptosis)，抑制其活力、迁移及侵袭能力。GQ127 可提高 YAP 磷酸化水平并降低 ERK 磷酸化水平。GQ127 抑制小鼠模型中葡萄膜黑色素瘤异种移植物的生长。GQ127 可用于葡萄膜黑色素瘤的相关研究。

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GQ127

GQ127 Chemical Structure

CAS No. : 2625582-70-7

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GQ127 相关抗体

Top Publications Citing Use of Products

查看 YAP 亚型特异性产品:

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YAP/TAZ YAP/TAZ-TEAD TEAD YAP1

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ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

GQ127 (10 μM) 可强效抑制 CHO-M1 细胞中 Gαq/11 介导的 IP1 积累，其 IC50 为 22.6 μM[1]。
GQ127 可以时间和剂量依赖的方式强效抑制 UM 92.1 细胞 (IC50 = 10.1 μM) 和 MP41 细胞 (IC50 = 24.8 μM) 的增殖[1]。
GQ127 (1.25-20 μM; 24 h) 对 CHO-M1 细胞表现出低细胞毒性，在 20 μM 以下浓度作用 24 h 后细胞活力未出现下降[1]。
GQ127 (5-30 μM; 48 h) 可呈剂量依赖性诱导 UM 92.1 和 MP41 细胞发生凋亡[1]。
GQ127 (5-30 μM; 48 h) 可在 15 μM 及更高浓度处理 48 h 后显著抑制 UM 92.1 和 MP41 细胞的迁移[1]。
GQ127 (5-30 μM; 48 h) 可通过提高 YAP 磷酸化水平并降低 ERK 磷酸化水平，抑制 UM 92.1 和 MP41 细胞中 Gαq/11 介导的肿瘤发生[1]。

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

GQ127 相关抗体:

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.
药代动力学
(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 %
体内研究
(In Vivo)

GQ127 (腹腔注射；每日一次；连续 21 天，剂量 10-30 mg/kg) 在 MP41 葡萄膜黑色素瘤异种移植模型中表现出显著的剂量依赖性抗肿瘤活性，30 mg/kg 剂量下的 TGI 为 99.0%，10 mg/kg 剂量下的 TGI 为 65.4%，且未表现出严重的全身毒性[1]。

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.
分子量

408.58

Formula

C25H36N4O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

GQ127 相关分类

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  • 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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