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GSK046

CAS No. : 2474876-09-8

MCE 国际站：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).

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