2. Immunology/Inflammation Stem Cell/Wnt JAK/STAT Signaling
  3. Transmembrane Glycoprotein STAT
  4. TPST2-IN-1

TPST2-IN-1 是一种高效且选择性的 TPST2 抑制剂，其 IC50 为 946 nM，Ka 为 19.4 μM。TPST2-IN-1 通过抑制 TPST2 活性，增加 Stat1 的磷酸化水平，并上调 IFNγ 反应基因 CXCL10 的表达。TPST2-IN-1 具有抗肿瘤活性，并能增强 T 细胞介导的抗肿瘤免疫，其特征是效应 CD8+ T 细胞浸润增加。TPST2-IN-1 可用于癌症研究，如结肠癌。

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TPST2-IN-1

TPST2-IN-1 Chemical Structure

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TPST2-IN-1 相关抗体

Top Publications Citing Use of Products

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STAT3 STAT5 STAT6 STAT1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TPST2-IN-1 is a potent and selective TPST2 inhibitor with an IC50 of 946 nM and a Ka of 19.4 μM. TPST2-IN-1 increases the phosphorylation of Stat1 and upregulates the IFNγ-responsive gene CXCL10 by inhibiting TPST2 activity.TPST2-IN-1 exhibits anti-tumor activity and enhances T cell-mediated antitumor immunity characterized by increased infiltration of effector CD8+ T cells. TPST2-IN-1 can be used for the research of cancer, such as colon cancer[1].

IC50 & Target[1]

STAT1

 

体外研究
(In Vitro)

TPST2-IN-1 (Compound 77c) (0.5-1 μM, 24-48 h) 增强 MC38 细胞中 IFNγ 诱导的 Cxcl10 基因表达，促进 Stat1 磷酸化，同时降低 HEK293 细胞中 IFNγ 受体 1 (IFNGR1) 的酪氨酸硫酸化水平[1]。
TPST2-IN-1 (2 μM, 1 h) 在过表达 Flag-TPST2 的 MDA-MB-231 细胞中增强 TPST2 的热稳定性[1]。

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

TPST2-IN-1 相关抗体:

Western Blot Analysis[1]

Cell Line: MC38 cells
Concentration: 0.5 μM
Incubation Time: 24 h
Result: Increased phosphorylation of Stat1.
体内研究
(In Vivo)

TPST2-IN-1 (Compound 77c) (50 mg/kg；腹腔注射；每日；1 天) 抑制 C57BL/6 小鼠皮下 MC38 结肠癌模型中的肿瘤生长并增强 T 细胞浸润[1]。

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

Animal Model: C57BL/6 mice with subcutaneous implantation of MC38 colon carcinoma cells (male, 6-8 weeks old, 18-20 g)[1]
Dosage: 50 mg/kg
Administration: Intraperitoneally injection;once a day
Result: Inhibited tumor growth.
\r\nIncreased the infiltration of effector CD8+ T cells, memory CD8+ T cells and NK cells in the spleen and tumor tissues.
\r\nEnhanced systemic immune activation.
\r\n
分子量

612.69

Formula

C31H34F2N4O5S
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

TPST2-IN-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

TPST2-IN-1Transmembrane GlycoproteinSTATimmunosuppression CD8 T cells interferon γ (IFNγ) receptor MC38 antitumor immunity tumor microenvironment anti-PD-1Inhibitorinhibitorinhibit

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目录号：
HY-179288
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