ERK
The mitogen-activated protein kinase (MAPK) pathway (also known as the RAS-RAF-MEK-ERK pathway) is a central signaling cascade activated by receptor tyrosine kinases (RTKs) upon binding by extracellular mitogenic ligands. RAS is a small GTP-binding protein that is activated by tyrosine kinase receptors and transmits the signal from the cell membrane to the nucleus. At the plasmamembrane, RAS activates the RAF kinase (MAPKKK), which in turn activates the MEK kinase (MAPKK), which consecutively stimulates the ERK (extracellular signal-regulated kinase; MAPK) through serial phosphorylation. The prototypical ERK 1/2 isoforms (here named ERK in its singular noun) are responsive to stimulation to growth factors and have apparent redundant functions. Once activated, ERK translocates to the nucleus and phosphorylates multiple substrates, including transcription factors, such as CREB and Elk1. The activation and repression of nuclear targets result in the induction of growth and proliferation and in the prevention of cell death. Moreover, ERK phosphorylates intracellular substrates in the cytoplasm, among which cytoskeletal and adherens junction proteins as well as apoptotic and cell cycle regulators stand out.
References
1.Gallo S,et al. Int J Mol Sci. 2019;20(9):2164.
References
1.Gallo S,et al. Int J Mol Sci. 2019;20(9):2164.
MAPK/ERK Signaling
ERK
-
Gardenin A
产品货号 : M37771
cas no: 21187-73-5
Gardenin A 是一种口服有效的、合成的 PMF 类似物,对神经突生长和神经元分化具有神经营养作用。Gardenin A 通过激活 PC12 细胞中的 MAPK/ERK、PKC 和 PKA 信号通路促进神经细胞的发生,但不激活 TrkA、CREB 信号通路。Gardenin A也有镇静、抗焦虑、抗抑郁和抗惊厥作用。 -
mSIRK
产品货号 : M37262
cas no: 593267-11-9
mSIRK (G-Protein βγ Binding Peptide) 是一种细胞渗透性 ERK1/2 的激活剂,EC50 为 2.5-5 μM 。mSIRK 会破坏 α 和 βγ 亚基之间的相互作用并促进 α 亚基解离,而不刺激核苷酸交换。 -
ERK5-IN-5
产品货号 : M37092
cas no: 2318792-30-0
ERK5-IN-5 (compound 4a) 是一种具有抗癌活性的 ERK5 激酶抑制剂。ERK5-IN-5 对 A549 细胞表现出良好的抗增殖活性,IC50 值为 6.23 μg/mL。 -
ERK5-IN-6
产品货号 : M37089
cas no: 2734916-64-2
ERK5-IN-6 (compound 5J)是一种具有抗癌活性的 ERK5 激酶抑制剂。ERK5-IN-6 对 A549 细胞表现出良好的抗增殖活性,IC50 值为 4.56 μg/mL。 -
Patritumab
产品货号 : M36726
cas no: 1262787-83-6
Patritumab (Human Anti-ERBB3 Recombinant Antibody) 是针对 ERBB3 的中和性单克隆抗体。Patritumab与 Cetuximab (HY-P9905) 具有协同作用,可有效抑制 EGFR,HER2,HER3,ERK 和 AKT 的磷酸化。Patritumab 也能诱导细胞凋亡 (apoptosis),也抑制胰腺、非小细胞肺癌和结直肠癌异种移植物肿瘤的生长。