MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

GSK046

CAS No. : 2474876-09-8

MCE 站：GSK046

产品活性：GSK046 (iBET-BD2) 是一种有效，选择性和具有口服活性的 BET 蛋白 BD2 溴结构域的抑制剂，IC₅₀ 值为 264 nM (BRD2 BD2)，98 nM (BRD3 BD2)，49 nM (BRD4 BD2) 和 214 nM (BRDT BD2)。GSK046 具有免疫调节活性。

研究领域：Epigenetics

作用靶点：Epigenetic Reader Domain

In Vitro: GSK046 (1000 nM; refresh every three days) reduces the recruitment of BET proteins to interferon (IFN) target genes following IFN-γ stimulation. GSK046 appears to more prominently affect the recruitment of BRD2 ａnd BRD3 compared to BRD4.
GSK046 (0.1-10 μM) displays a more selective phenotypic fingerprint, particularly inhibiting the production of key pro-inflammatory mediators including Th17 cytokines in the B ａnd T cell co-culture system.
GSK046 (0.01-10 μM; 72 hours) does not affect the proliferative activity of human primary CD4⁺ T cells but still inhibits the production of effector cytokines including IFNγ, IL-17A ａnd IL-22.
GSK046 (0.005-10 μM; 48 hours) impairs macrophage activation following PMA stimulation, without impacting cellular viability.

In Vivo: GSK046 (40 mg/kg/QD; s.c. for 14 days) has immunomodulatory activity.
GSK046 exhibits C_max (C57BL6 1589, C57B16 2993 ng/mL) ａnd terminal elimination half-lives (C57BL6 1.8, C57B16 1.9 h) following oral administration (C57BL6 10, C57B16 40 mg/kg).
GSK046 exhibits C_max (mouse 1589, rat 202 ng/mL) ａnd terminal elimination half-lives (mouse 1.8, rat 1.4 h) following oral administration (mouse 10, rat 10 mg/kg).

相关产品：Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Immunology/Inflammation Compound Library  |  Histone Modification Research Compound Library  |  Reprogramming Compound Library  |  Orally Active Compound Library  |  Anti-Blood Cancer Compound Library  |  A-485  |  Curcumin  |  Birabresib  |  C646  |  JQ-1 (carboxylic acid)  |  Anacardic Acid  |  I-BET151  |  SGC-CBP30  |  MG 149  |  KG-501  |  A-366  |  CPI-203  |  NSC 228155  |  PFI-1  |  GSK2801  |  ACBI1  |  IACS-9571 hydrochloride  |  MI-3  |  (+)-JQ1 PA  |  PF-CBP1 hydrochloride  |  SGC-iMLLT  |  Bromosporine  |  EML 425  |  HJB97  |  MS436  |  CeMMEC1  |  GSK1379725A  |  GSK6853  |  MS31 trihydrochloride  |  MS645

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*新*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 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。