HJ-PI01

HJ-PI01 (10-Acetylphenoxazine) is an orally active Pim-2 inhibitor. HJ-PI01 induces apoptosis and autophagic cell death of cancer cells. HJ-PI01 inhibits tumor growth in MDA-MB-231 xenograft mice. HJ-PI01 can be used for cancer research[1].

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> Pim

HJ-PI01 (0-3200 nmol/L；48 小时) 剂量性依赖地抑制 MDA-MB-231 细胞生长，与氯丙嗪和 PI003 相比效果更为显著改善[1]。 HJ-PI01 (100-400 nmol/L；24 小时) 对正常非癌细胞显示弱毒性[1]。 HJ-PI01 (300 nmol/L；24 小时) 诱导 MDA-MB-231 细胞自噬性细胞死亡[1]。 HJ-PI01 (300 nmol/L；24 小时) 诱导 MDA-MB-231 细胞凋亡性死亡[1]。 HJ-PI01 (300 和 460 nmol/L；12-48 小时) 影响自噬和凋亡相关蛋白的表达水平[1]。 Western Blot Analysis[1] Cell Line: MDA-MB-231 cell line Concentration: 300 and 460 nmol/L Incubation Time: 12, 24, 36 and 48 hours Result: Time-dependently increased LC3-II and Beclin-1 and induced p62 degradation in MDA-MB-231 cells. Increased the level of Bax. Decreased the level of Bcl-2, and Pim-2 and Pim-2 phosphorylation. Activated caspase-9 and caspase-3.

HJ-PI01 (40 mg/kg；口服，每日 1 次，持续 10 天) 抑制 MDA-MB-231 异种移植小鼠肿瘤生长[1]。 Animal Model: BALB/c female nude mice with MDA-MB-231 cells injection[1] Dosage: 40 mg/kg Administration: Oral administration; 40 mg/kg, once daily for 10 days Result: Significantly inhibited tumor growth with an obvious decreasing of the body, liver, spleen and kidney weights of the mice.

[1]. Zhao YQ, et al. Characterization of HJ-PI01 as a novel Pim-2 inhibitor that induces apoptosis and autophagic cell death in triple-negative human breast cancer. Acta Pharmacol Sin. 2016 Sep;37(9):1237-50.