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VVD-118313

CAS No. :

MCE 站：VVD-118313

产品活性：VVD-118313 (compound 5a) 是一个有效的选择性 JAK1 抑制剂。VVD-118313 靶向异构体限制性变构半胱氨酸 (C817)，阻断 JAK1 依赖的反式磷酸化和细胞因子信号。VVD-118313可用于癌症的研究。

研究领域：Epigenetics  |  Stem Cell/Wnt  |  JAK/STAT Signaling  |  Immunology/Inflammation

作用靶点：JAK  |  STAT  |  IFNAR  |  Interleukin Related

In Vitro: VVD-118313 (compound 5a; 0.01-10μM; 3 h; primary human PBMCs) inhibits JAK1 by engagement of C817 ａnd JAK2 by engagement of C838. VVD-118313 inhibits cysteine reactivity in a dose-dependent manner.
VVD-118313 (2 M, 2h) blocks IFNα-simulated STAT1 ａnd IL-6-stimulated STAT3 phosphorylation in WT- or C810A-JAK1-expressing 22Rv1 cells. VVD-118313 also blocks the constitutive phosphorylation of WT- ａnd C810A-JAK1.
VVD-118313 (0.01-10μM) selectively inhibits JAK1 signaling in primary human immune cells. VVD-118313 inhibits JAK1-dependent IFNα-pSTAT1, IL-6-pSTAT3, ａnd IL-2-pSTAT5 pathways in human PBMCs in a dose-dependent manner.
VVD-118313 (0.1-0.4 μM; 24h) inhibits T-cell activation induction. VVD-118313 inhibits the activation of human T cells co-stimulated with αCD3/αCD28 by a reduction in the proportion of CD25⁺ T cells. VVD-118313 blocks the secretion of the Th1-polarizing cytokine IFNγ ａnd increases the production of IL-2.
VVD-118313 (0.1-0.5μM; 2h) inhibits on the production of pro-inflammatory cytokines ａnd chemokines. VVD-118313 suppresses the induction of several pro-inflammatory chemokines, including CCL2/MCP-1, CXCL10/IP-10, ａnd CCL4/MIP-1β.

In Vivo: VVD-118313 (compound 5a; 25-50 mg/kg; i.h.; once; TYK2 knockout mice) inhibits JAK1 signaling in mice.

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