Name: PROTAC HPK1 Degrader-5
Brand: TargetMol
SKU: T212062
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

10 mg

待询

50 mg

待询

产品介绍

生物活性

产品描述	PROTACHPK1 Degrader-5 is a potent, orally active HPK1 PROTAC degrader with a DC50 of 5.0 nM and a Dmax of at least 99%. It significantly inhibits HPK1 by degrading it, reducing SLP76 phosphorylation, and enhancing ERK pathway activation, which in turn stimulates the release of IL-2 and IFN-γ. This compound effectively counteracts immune suppression induced by PGE2, NECA, or TGF-β. Alone, PROTACHPK1 Degrader-5 is capable of suppressing tumor growth in MC38 syngeneic mouse models. It is used in research for immunotherapy applications in cancers such as colorectal cancer.
体外活性	PROTAC HPK1 Degrader-5 (Compound 10m) (30 nM, 24 h) 导致 Jurkat 细胞中 HPK1 的降解，并需要 UPS、CRBN、HPK1 和 CRBN 的协同。PROTAC HPK1 Degrader-5 (10 nM) 在剂量依赖的情况下显著抑制 Jurkat 细胞及抗 CD3/CD28 抗体刺激的 PBMC 中 SLP76 的磷酸化，同时强化远端下游 ERK 的激活，与 HPK1 降解相一致。
体内活性	PROTAC HPK1 Degrader-5 (Compound 10m) 在剂量为 0.5-3 mg/kg 的情况下，每隔一天口服一次，持续 14 天，有效抑制 MC38 同基因肿瘤小鼠模型中的肿瘤生长，与 PD-1 阻断剂联合使用时，抗肿瘤效果更显著。