2. MAPK/ERK Pathway Cell Cycle/DNA Damage Immunology/Inflammation
  3. MAP4K HOXA Interleukin Related
  4. HPK1-IN-65

HPK1-IN-65 是一种选择性且具有口服活性的 HPK1 抑制剂 IC50 值小于 5 nM，并对 MAP4K 激酶家族成员 GLK 表现出 1257 倍的选择性。HPK1-IN-65 抑制 pSLP76 磷酸化的 IC50 为 92.3 nM。HPK1-IN-65 刺激 IL-2 生成的 EC50 为 398 nM。HPK1-IN-65 以剂量依赖的方式抑制 TCR 诱导的 SLP76 Ser376 位点的磷酸化。HPK1-IN-65 可进一步用于结肠癌研究。

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HPK1-IN-65

HPK1-IN-65 Chemical Structure

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HPK1-IN-65 相关抗体

Top Publications Citing Use of Products

查看 MAP4K 亚型特异性产品:

查看所有亚型
MAP4K2/GCK MAP4K3/GLK MAP4K4/HGK MAP4K5/KHS1 MAP4K6/MINK1 MAP4K7/TNIK MAP4K1/HPK1

查看 Interleukin Related 亚型特异性产品:

查看所有亚型
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HPK1-IN-65 is a selective and orally active HPK1 inhibitor with an IC50 value of < 5 nM. HPK1-IN-65 inhibits HPK1 kinase activity and displays 1257-fold selectivity over the MAP4K kinase family member GLK. HPK1-IN-65 exhibits an IC50 of 92.3 nM for inhibiting pSLP76 phosphorylation. HPK1-IN-65 demonstrates an EC50 of 398 nM for stimulating IL-2 production. HPK1-IN-65 inhibits TCR-induced phosphorylation of SLP76 at Ser376 in a dose-dependent manner. HPK1-IN-65 can be further utilized for colorectal cancer research[1].

IC50 & Target[1]

HPK1

<5 nM (IC50)

IL-2

398 nM (EC50)

体外研究
(In Vitro)

HPK1-IN-65 (compound 34) 在 Jurkat 细胞中以剂量依赖性方式降低 pSLP76 水平，其 IC50 值为 92.3 nM[1]。
HPK1-IN-65 可刺激 IL-2 生成，EC50 为 398 nM，并将激活效应最高提升 3.59 倍[1]。
HPK1-IN-65 对 Jurkat 细胞具有抗增殖作用[1]。
HPK1-IN-65 对 MAP4K2, MAP4K3, MAP4K4, MAP4K5, MAP4K6 具有选择性[1]。

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

HPK1-IN-65 相关抗体:
体内研究
(In Vivo)

HPK1-IN-65 (compound 34) (60 mg/kg，口服给药，每日一次共 14 天) 在 CT-26 同源肿瘤的雌性 BALB/c 小鼠 (6 weeks old) 模型中展现出强效的抗肿瘤作用[1]。

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

Animal Model: Colorectal carcinoma cell line CT-26 cells (2.5 × 105 cells, s.c.) induced female BALB/c mice (6- week-old)[1]
Dosage: 60 mg/kg
Administration: i.g., once daily for 14 consecutive days, Anti-PD-1 monoclonal antibody (HY-P99709) (i.p., 10 mg/kg, twice a week)
Result: Achieved a robust anti-tumor response with a TGI of 62.90%.
Caused no significant impact on animal body weight in either monotherapy or combination groups.
Delayed the tumor growth, with the tumor growth inhibi tion (TGI) reaching 41.73 % at 14 days post-treatment (without Anti-PD-1 monoclonal antibody).
分子量

528.99

Formula

C23H22ClFN8O2S
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-65 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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-65MAP4KHOXAInterleukin RelatedMAPK Kinase Kinase KinaseHomeobox AILHPK1 inhibitorMAP4K kinasetumor efficacySer376Inhibitorinhibitorinhibit

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目录号：
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