CDK8-IN-15,2988020-03-5

CDK8-IN-15 产品活性：CDK8-IN-15 (Compound 46) 是一种强有效的 CDK8 抑制剂，IC50 值为 57 nM。它能增强 CDK8 的热稳定性并同时抑制 NF-κB ，也能选择性抑制 CDK 家族 和 酪氨酸。此外，也能对体外 TNF-α 导致的牛皮癣起积极作用并增强 Foxp3 和 IL-10 的表达来减弱炎症反应，有望用于牛皮癣疾病的研究。 产品来源： www.medchemexpress.cn/cdk8-in-15.html 研究领域：Cell Cycle/DNA Damage 作用靶点：CDK In Vitro: CDK8-IN-15 exhibits the highest activity against CDK8 with an IC50 value of 57.3 nM and exerts a positive effect on the TNF-α-induced psoriasis model of HaCat cells with an IC50 value of 4.6 μM . CDK8-IN-15 (5 μM, 4 h) inhibits CDK8 enzyme activity and enhances the thermal stability of endogenous and exogenous CDK8 in HEK293T-CDK8 cells. CDK8-IN-15 (0,1,2,4 μM, 75h) significantly reduces the levels of CXCL1, CXCL2, IL-8 in HEK293 cells . In Vivo: CDK8-IN-15 (2 MG/KG, iv and 10 MG/KG , p.o.) shows high permeability and no obvious inhibition of the five cytochrome p450 isoenzymes . CDK8-IN-15 (1000 MG/KG, i.g. ) doesn’t cause a significant tissue damage . CDK8-IN-15 (5/10/20 MG/KG,i.g.) might enhance IL-10 production and Foxp3 expression by targeting CDK8, thereby alleviating psoriasis . 相关产品：Palbociclib | Abemaciclib | Ro-3306 | Ribociclib | Dinaciclib | GSK3326595 | Flavopiridol | (R)-Roscovitine | THZ1 | AZD4573 | THZ531 | SR-4835 | Kenpaullone | SY-5609 | Wogonin | GSK 3 Inhibitor IX | SNS-032 | Toyocamycin | NVP-2 | OTS964 hydrochloride | 5,6-Dichlorobenzimidazole riboside | Cirtuvivint | Simurosertib | PF-07220060 | AT7519 | Amantadine | JNJ-7706621 品牌介绍: MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；设有专业的实验中心和严格的质控、验证体系；提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；产品的生物活性多经各国客户实验验证；Nature, Cell, Science 等多种TOP期刊及制药专利收录了MCE客户的科研成果；专业团队跟踪前沿的制药及生命科学研究进展，为您提供全球前沿的活性化合物；与世界各大制药公司及知名科研机构建立了长期的合作。