GA-017
目录号: PL13227 纯度: ≥98%
CAS No. :2351906-74-4
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中文名称
GA-017
英文名称
GA-017
英文别名
1-[1-(2,4-Dihydroxy-3-methylphenyl)propylideneamino]-3-[(3-hydroxyphenyl)methyl]urea;Hydrazinecarboxamide, 2-[1-(2,4-dihydroxy-3-methylphenyl)propylidene]-N-[(3-hydroxyphenyl)methyl]-;GA-017
Cas No.
2351906-74-4
分子式
C18H21N3O4
分子量
343.38
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
GA-017是一种强效的选择性 LATS1 和 LATS2 (大型肿瘤抑制激酶 1/2) 抑制剂,其 IC50 值分别为 4.10 和 3.92 nM。GA-017 是一种细胞增殖激活剂。GA-017 促进 YAP/TAZ 激活和核转位。GA-017 在 3D 培养条件下促进细胞生长。GA-017 增强小鼠肠道类器官离体的形成。
生物活性
GA-017 is a potent and selective LATS1 and LATS2 (large tumor suppressor kinase 1/2) inhibitor, with IC 50 values of 4.10 and 3.92 nM, respectively. GA-017 is an activator of cell proliferation. GA-017 promotes YAP/TAZ activation and nuclear translocation. GA-017 promotes cell growth under 3D culture conditions. GA-017 enhances the ex vivo formation of mouse intestinal organoids.
性状
Solid
IC50 & Target[1][2]
IC50: 3.92 ± 0.42 nM (LATS2), 4.10 ± 0.79 nM (LATS1)
体外研究(In Vitro)
GA-017 suppresses the cell death of HUVECs and promotes their cell growth.
GA-017 facilitates SKOV3 cell growth, with an EC50 of 3.51 ± 0.26 μM.
GA-017 competitively inhibited LATS1 and 2 against ATP, with Ki (inhibition constant) values of 0.58 ± 0.11 and 0.25 ± 0.03 nM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Aihara A, et al. Small molecule LATS kinase inhibitors block the Hippo signaling pathway and promote cell growth under 3D culture conditions. J Biol Chem. 2022 Apr;298(4):101779.
溶解度数据
In Vitro: DMSO : 20.83 mg/mL (60.66 mM; ultrasonic and warming and heat to 80°C)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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