2875046-31-2

2875046-31-2 structure

Name: (R,R)-VVD-118313
Chemical Name: (R,R)-VVD-118313
CAS Number: 2875046-31-2
Molecular Formula: C₁₉H₂₂Cl₂N₂O₃S
Molecular Weight: 429.36
Catalog: Signaling Pathways Epigenetics JAK
Create Date: 2023-04-10 16:55:47
Modify Date: 2024-02-24 19:20:27
(R,R)-VVD-118313 is the isomer of VVD-118313 (HY-151385). VVD-118313 is a selective JAK1 inhibitor and blocks JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer[1].

Name	(R,R)-VVD-118313

Description	(R,R)-VVD-118313 is the isomer of VVD-118313 (HY-151385). VVD-118313 is a selective JAK1 inhibitor and blocks JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer[1].
Related Catalog	Signaling Pathways >> Stem Cell/Wnt >> STAT Research Areas >> Cancer Signaling Pathways >> JAK/STAT Signaling >> JAK Signaling Pathways >> Immunology/Inflammation >> IFNAR Signaling Pathways >> Epigenetics >> JAK Signaling Pathways >> Stem Cell/Wnt >> JAK Signaling Pathways >> JAK/STAT Signaling >> STAT Signaling Pathways >> Immunology/Inflammation >> Interleukin Related
Target	JAK1
In Vitro	VVD-118313 (化合物 5a；0.01-10μM；3 小时；原代人 PBMC) 靶向 C817 以抑制 JAK1，并靶向 C838 以抑制 JAK2。VVD-118313 以剂量依赖性方式抑制半胱氨酸反应性[1]。 VVD-118313 (2 µM, 2 h) 在表达 WT 或 C810A-JAK1 的 22Rv1 细胞中阻断 IFNα 模拟的 STAT1 和 IL-6 刺激的 STAT3 磷酸化。VVD-118313 还阻断野生型 JAK1 和 C810A-JAK1 的组成型磷酸化[1]。 VVD-118313 (0.01-10 μM) 选择性抑制原代人免疫细胞中的 JAK1 信号传导。VVD-118313 以剂量依赖性方式抑制人 PBMC 中 JAK1 依赖性 IFNα-pSTAT1、IL-6-pSTAT3 和 IL-2-pSTAT5 通路[1]。 VVD-118313 (0.1-0.4 μM; 24 h) 抑制 T 细胞活化诱导。VVD-118313 通过降低 CD25+ T 细胞的比例来抑制与 αCD3/αCD28 共刺激的人 T 细胞的活化。VVD-118313 阻断 Th1 极化细胞因子 IFNγ 的分泌并增加 IL-2 的产生[1]。 VVD-118313 (0.1-0.5 μM; 2 h) 抑制促炎细胞因子和趋化因子的产生。VVD-118313 抑制多种促炎趋化因子的诱导，包括 CCL2/MCP-1、CXCL10/IP-10 和 CCL4/MIP-1β[1]。 Western Blot Analysis[1] Cell Line: 22Rv1 cells Concentration: 0.01, 0.1, and 1 μM Incubation Time: 2 hours Result: Showed labeling of recombinant WT-JAK1 and C810A-JAK1, but not C817A-JAK1. Inhibited WT- and C810A-JAK1 phosphorylation with even greater potency than STAT1/STAT3 phosphorylation.
In Vivo	VVD-118313 (化合物 5a；25-50 mg/kg；皮下注射；单剂量) 抑制 TYK2 敲除小鼠中的 JAK1 信号传导[1]。
References	[1]. Kavanagh ME, et, al. Selective inhibitors of JAK1 targeting an isoform-restricted allosteric cysteine. Nat Chem Biol. 2022 Sep 12.

Molecular Formula	C₁₉H₂₂Cl₂N₂O₃S
Molecular Weight	429.36

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