1. Metabolic Enzyme/Protease Immunology/Inflammation Stem Cell/Wnt Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  2. Phosphatase IFNAR JAK STAT
  3. PTPN2-IN-2

PTPN2-IN-2 是一种强效且口服有效的 PTPN2 抑制剂 (IC50 = 7.05 nM),可增强 IFN-γ 信号通路。PTPN2-IN-2 对 PTP1B 的抑制作用 IC50 为 9.88 nM。在 B16-OVA 小鼠模型中,PTPN2-IN-2 可抑制肿瘤生长,并促进肿瘤免疫细胞的活化和浸润。PTPN2-IN-2 可用于黑色素瘤的研究。

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PTPN2-IN-2

PTPN2-IN-2 Chemical Structure

CAS No. : 3093350-44-5

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生物活性

PTPN2-IN-2 is a potent and orally active PTPN2 inhibitor (IC50 = 7.05 nM) that enhances the IFN-γ signaling pathway. PTPN2-IN-2 inhibits PTP1B with an IC50 of 9.88 nM. PTPN2-IN-2 inhibits tumor growth, promotes the activation and infiltration of tumor immune cells in a B16-OVA mouse model. PTPN2-IN-2 can be used for the research of melanoma[1].

IC50 & Target[1]

PTPN2

7.05 nM (IC50)

PTP1B

9.88 nM (IC50)

体外研究
(In Vitro)

PTPN2-IN-2 (compound K-38) (0-100 µM; 24 小时) 可增强 Jurkat 和 B16 细胞中的 IFN-γ/JAK/STAT1 信号通路,表现为 IFN-γ 刺激后 STAT1 磷酸化增加[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Jurkat and B16 cells
Concentration: 0; 1; 10; 50; 100 µM
Incubation Time: 24 h
Result: Induced an increase in STAT1 phosphorylation.
体内研究
(In Vivo)

PTPN2-IN-2 (50-150 mg/kg;口服;每日一次;持续 24 天) 在 B16-OVA 小鼠模型中通过调节 IFN-γ 信号转导来抑制肿瘤生长[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female C57BL/6J mice subcutaneously implanted with B16-OVA cells[1]
Dosage: 50; 100; 150 mg/kg
Administration: p.o.; once daily for 24 days
Result: Significantly inhibited the volume, proliferation rate and tumor weight of melanoma in mice.
Significantly enhanced the inhibitory activity of PD-1 on tumor growth.
Had no significant effect on the body weight.
Markly increased CD8+ T and CD45+ leukocyte infiltration in B16-OVA tumors.
Increased IFN-γ levels in tumor tissues.
Upreugalted PD-L1 and p-STAT1 levels.
分子量

451.47

Formula

C19H22FN5O5S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
PTPN2-IN-2
目录号:
HY-179380
需求量: