PF-3644022
Cat. No.：YN350049
CAS No. ：1276121-88-0
| 产品名称: | PF-3644022 |
| CAS No.: | 1276121-88-0 |
| Chemical Name: | (10R)-9,10,11,12-tetrahydro-10-methyl-3-(6-methyl-3-pyridinyl)-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one |
| Synonyms: | PF 3644022;PF3644022 |
| 分子量: | 374.46 |
| 分子式: | C₂₁H₁₈N₄OS |
| SMILES: | O=C1C2=C(NC[C@@H](C)N1)C3=C(C=CC4=NC(C5=CN=C(C)C=C5)=CC=C34)S2 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | PF-3644022 是一种有效的，选择性的，口服活性的，具有 ATP 竞争性的MAPKAPK2 (MK2)抑制剂，IC50为 5.2 nM，Ki为 3 nM。PF-3644022 还抑制 MK3 和 p38 调节/激活激酶 (PRAK)，IC50分别为 53 nM 和 5.0 nM。PF-3644022 有效抑制 TNFα 的产生并具有抗炎作用。 |
| IC50和靶点: | |
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Mourey, R.J., Burnette, B.L., Brustkern, S.J., et al.A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor α production and has oral anti-inflammatory efficacy in acute and chronic models of inflammationJ. Pharmacol. Exp. Ther.333(3),797-807(2010)
Yu, L., Song, H., Fang, X., et al.Role of MK2 signaling pathway mediating microglia/macrophages polarization in chronic compression injury of cervical spinal cordAnn. Palliat. Med.10(2),1304-1312(2021)
Berggren, K.L., Cruz, S.R., Hixon, M.D., et al.MAPKAPK2 (MK2) inhibition mediates radiation-induced inflammatory cytokine production and tumor growth in head and neck squamous cell carcinomaOncogene38(48),7329-7341(2019)
