(R,R)-VVD-118313

Modify Date: 2025-11-28 00:28:12

(R,R)-VVD-118313 Structure
(R,R)-VVD-118313 structure
Common Name (R,R)-VVD-118313
CAS Number 2875046-31-2 Molecular Weight 429.36
Density N/A Boiling Point N/A
Molecular Formula C19H22Cl2N2O3S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of (R,R)-VVD-118313


(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].

 Names

Name (R,R)-VVD-118313

 (R,R)-VVD-118313 Biological Activity

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
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.  

 Chemical & Physical Properties

Molecular Formula C19H22Cl2N2O3S
Molecular Weight 429.36
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