HPK1-IN-22

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HPK1-IN-22 

HPK1-IN-22 (compound ZYF0033) 是一种造血祖细胞激酶 1 (HPK1) 抑制剂，基于 MBP 蛋白的磷酸化抑制作用的 IC50 小于 10 nM。HPK1-IN-22 降低 SLP76 (丝氨酸 376) 的磷酸化。HPK1-IN-22 促进抗癌免疫反应。HPK1-IN-22 抑制 4T-1 同基因小鼠模型中的肿瘤生长并导致 DC、NK 细胞和 CD107a+CD8+ T 细胞的肿瘤内浸润增加，但导致 T 细胞、PD-1+CD8+ T 细胞、TIM-3+CD8+ T 细胞和 LAG3+CD8+ T 细胞的浸润减少。

HPK1-IN-22

HPK1-IN-22 Chemical Structure

CAS No. : 2380300-79-6

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生物活性

HPK1-IN-22 (compound ZYF0033) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 less than 10 nM based on the phosphorylation inhibition of MBP protein. HPK1-IN-22 decreases the phosphorylation of SLP76 (serine 376). HPK1-IN-22 promotes anticancer immune responses.HPK1-IN-22 inhibits tumor growth and caused increases intratumoral infiltration of DCs, NK cells, and CD107a+CD8+ T cells but decreased infiltration of regulatory T cells, PD-1+CD8+ T cells, TIM-3+CD8+ T cells, and LAG3+CD8+ T cells in the 4T-1 syngeneic mouse model[1].

IC50 & Target[1]

HPK1

<10 nM (IC50)

分子量

462.61

Formula

C26H30N4O2S
CAS 号

2380300-79-6
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.
参考文献

  • [1]. Jingwen Si, et al. Hematopoietic Progenitor Kinase1 (HPK1) Mediates T Cell Dysfunction and Is a Druggable Target for T Cell-Based Immunotherapies. Cancer Cell. 2020 Oct 12;38(4):551-566.e11.

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