2. MAPK/ERK Pathway Immunology/Inflammation
  3. MAP4K Interleukin Related
  4. HPK1-IN-68

HPK1-IN-68 (Compound 39) 是一种 HPK1 抑制剂，其 IC50 为 2.8 nM。HPK1-IN-68 可阻断 HPK1 信号传导，抑制 HPK1 介导的 SLP76 磷酸化，促进 IL-2 细胞因子的产生。HPK1-IN-68 可拮抗 PGE2 介导的免疫抑制作用。HPK1-IN-68 可增强 CD3+/CD8+ T 细胞向肿瘤组织的浸润。HPK1-IN-68 在小鼠结肠癌模型中具有 T 细胞依赖性的抗肿瘤功效。HPK1-IN-68 与 anti-PD-1 联合使用时，表现出显著的协同抗肿瘤作用。HPK1-IN-68 可用于结肠癌的相关研究。

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HPK1-IN-68

HPK1-IN-68 Chemical Structure

CAS No. : 3078477-58-1

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HPK1-IN-68 相关抗体

Top Publications Citing Use of Products

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MAP4K2/GCK MAP4K3/GLK MAP4K4/HGK MAP4K5/KHS1 MAP4K6/MINK1 MAP4K7/TNIK MAP4K1/HPK1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HPK1-IN-68 (Compound 39) is a HPK1 inhibitor with an IC50 of 2.8 nM. HPK1-IN-68 blocks HPK1 signaling, inhibits HPK1-mediated phosphorylation of SLP76, and promotes the production of the IL-2 cytokine. HPK1-IN-68 antagonizes the immunosuppressive effect mediated by PGE2. HPK1-IN-68 enhances the infiltration of CD3+/CD8+ T cells into tumor tissues. HPK1-IN-68 exerts T cell-dependent antitumor efficacy in a mouse colon cancer model. HPK1-IN-68 exhibits significant synergistic antitumor effects when used in combination with anti-PD-1. HPK1-IN-68 is applicable to research related to colon cancer[1].

IC50 & Target[1]

HPK1

2.8 nM (IC50)

IL-2

 

体外研究
(In Vitro)

HPK1-IN-68 (预平衡 10 min, 1 h) 可强效抑制重组 HPK1 激酶活性，其 IC50 为 2.8 nM[1]。
HPK1-IN-68 (0-1000 nM; 2 h) 可在 Jurkat T 细胞中抑制 HPK1 介导的 SLP76 磷酸化，其 IC50 为 30.4 nM[1]。
HPK1-IN-68 (0.01 nM-1 μM; 48 h) 可在亚微摩尔浓度下增强经 CD3/CD28 刺激的 Jurkat T 细胞中 IL-2 细胞因子的产生[1]。
HPK1-IN-68 在肝微粒体中具有中等代谢稳定性，半衰期为 26.1 min[1]。

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

HPK1-IN-68 相关抗体:

ELISA Assay[1]

Cell Line: Jurkat T cells
Concentration: 0.01 nM-1 μM
Incubation Time: 48 h
Result: Increased IL-2 production relative to vehicle control at concentrations from 0.01 nM to 100 nM.
Reduced IL-2 production at the highest tested concentration (1 μM).
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Vdss AUC0-t AUC0-∞ CL MRT0-∞ Tmax Cmax CL/F Vz/F Bioavailability
Mice[1] 1 mg/kg i.v. 4.8 ± 1.1 h 16.8 ± 4.0 L/kg 260.5 ± 20.9 ng·h/mL 271.3 ± 21.9 ng·h/mL 61.7 ± 5.1 mL/h/kg 4.6 ± 1.1 h / / / / /
Mice[1] 10 mg/kg p.o. 4.2 ± 0.6 h / 743.4 ± 224.1 ng·h/mL 755.8 ± 223.7 ng·h/mL / 4.5 ± 0.2 h 1.7 ± 0.6 h 140.1 ± 42.3 ng/mL 235.7 ± 77.9 mL/min/kg 89.3 ± 42.5 L/kg 28.5 ± 8.6 %
体内研究
(In Vivo)

HPK1-IN-68 (10 mg/kg；腹腔注射；每日 2 次；17 天) 在小鼠 CT26 结肠癌模型中，单试剂处理和抗 PD-1 抗体联合使用都可发挥抗肿瘤作用[1]。

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

Animal Model: Balb/c (female, 4-5 weeks old, 18-22 g, subcutaneously injected with 5×105 CT26 tumor cells)[1]
Dosage: 10 mg/kg (monotherapy; combination with anti-PD-1)
Administration: i.p.; bid; 17 days (monotherapy); i.p.; bid (combination with anti-PD-1, anti-PD-1 administered on days 0, 3, 7, and 10 at 5 mg/kg i.p.)
Result: Achieved 48% tumor growth inhibition (TGI) as monotherapy.
Achieved 59% TGI with combination index (CI) < 1 and synergy score (SS) > 0 when combined with anti-PD-1 antibody, confirming synergistic activity.
Was well-tolerated, with no significant body weight loss observed.
Increased infiltration of CD3+/CD8+ T cells into tumor tissues, and this effect was amplified when combined with anti-PD-1 antibody.
分子量

453.51

Formula

C23H28FN7O2
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

HPK1-IN-68 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:

HPK1-IN-683078477-58-1MAP4KInterleukin RelatedMAPK Kinase Kinase KinaseILCD3+/CD8+ T cellsERKHPK1prostaglandin E2IL-2T-cell receptor pathwaycolon canceranti-PD-1SLP76NF-κBInhibitorinhibitorinhibit

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目录号：
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