PF-06651600产品描述：PF-06651600 is a potent JAK3-selective inhibitor with an IC₅₀ of 33.1 nM.IC50 & Target: IC50: 33.1 nM (JAK3)^[1]In Vitro: PF-06651600 is a potent JAK3-selective inhibitor which can inhibit the JAK3 kinase activity with an IC₅₀ of 33.1 nM but without activity (IC₅₀>10?000 nM) against JAK1, JAK2, and TYK2. PF-06651600 inhibits the phosphorylation of STAT5 elicited by IL-2, IL-4, IL-7, and IL-15 with IC₅₀ values of 244, 340, 407, and 266 nM, respectively. PF-06651600 also inhibits the phosphorylation of STAT3 elicited by IL-21 with an IC₅₀ of 355 nM. Functional assessment in T-cell differentiation assays demonstrate that PF-06651600 suppresses Th1 and Th17 differentiation as measured by IFNγ, after 5 days under Th1 conditions, and IL-17 production, after 6 days under Th17 conditions, with IC₅₀ values of 30 nM and 167 nM, respectively. PF-06651600 also suppresses Th1 and Th17 function as measured by the inhibition of IFNγ production (IC₅₀=48 nM) and IL-17 production (IC₅₀=269 nM) in cells that have been previously differentiated and rested before being treated with PF-06651600^[1].In Vivo: In the rat adjuvant-induced arthritis (AIA) model, PF-06651600 reduces paw swelling with an unbound EC₅₀ of 169 nM. Similarly, PF-06651600 significantly reduces disease severity in the experimental autoimmune encephalomyelitis (EAE) mouse model when dosed either therapeutically at 30 or 100 mg/kg or prophylactically at 20 and 60 mg/kg. The efficacy of PF-06651600 in these two rodent models of inflammatory and autoimmune diseases illustrates that JAK3-selective inhibition can be sufficient to have disease modifying effects in human diseases^[1].
产品链接：www.medchemexpress.com/PF-06651600.html

研究领域：Epigenetics

靶点：JAK

相关产品：Baricitinib  |  Pacritinib  |  Upadacitinib  |  CYT387  |  AZD-1480  |  WP1066  |  TG-101348  |  AT9283  |  Cerdulatinib  |  GLPG0634  |  Itacitinib  |  Decernotinib  |  LY2784544  |  CHZ868  |  SB1317  |  



公司介绍：MedChemExpress(MCE)专注于各种抑制剂、激动剂、API及化合物库，总部位于美国新泽西，分别在瑞典和上海设有欧洲区子公司和亚洲区总代理，营销网点遍及全球20多个国家地区。MCE经过多年努力已成为全球生物活性小分子领域的一流供应商， 产品涵盖癌症、神经科学、抗感染、表观遗传学等20个热门研究领域，PI3K、MAPK等近千个细分靶点，超过4000个活性小分子化合物现货，以及GPCR、API、离子通道等超过20种不同类型的化合物库，同时提供从毫克到千克的专业定制合成服务。
MCE 对每批产品都进行严格的LCMS和NMR检验，其产品已被全球近万名客户广泛使用并发表大量文章、；
MCE 定期增加各领域热门抑制剂、激动剂，不断扩增已有化合物库，以满足*新的科研需求；
数千种产品在上海有充足备货，24-48小时内送达客户；
大量产品提供免费试用装；已为全球多个知名企业、院校构建各种定制型化合物库。

更新时间：2024/1/2 10:10:55