GPX4-IN-3 (26a) 是有效的谷胱甘肽过氧化物酶4(GPX4)抑制剂，可选择性诱导铁死亡 (Ferroptosis)。GPX4-IN-3 (26a) 在1 μM 的浓度可抑制GPX4 71.7% 活性。

GPX4-IN-3 (26a) is a potent glutathione peroxidase 4 (GPX4) inhibitor as a selective ferroptosis inducer. GPX4-IN-3 (26a) exhibits 71.7% inhibition for GPX4 with 1 μM [1].

GPX4-IN-3 (26a) exhibits IC 50 values of 0.78 μM, 6.9 μM, 0.15 μM and 4.73 μM in 4T1, MCF-7, HT1080 and HT1080 (with Fer-1) cells, respectively [1]. GPX4-IN-3 (26a) exhibits outstanding GPX4 inhibitory activity with a percent inhibition up to 71.7% at 1.0 μM compared to 45.9% of RSL-3 [1]. GPX4-IN-3 (26a) could significantly induce lipid peroxide (LPO) increase and effectively induce ferroptosis with satisfactory selectivity [1]. GPX4-IN-3 (26a) is more likely to induce ferroptosis through the accumulation of intracellular peroxides via inhibiting GPX4 activity [1]. GPX4-IN-3 (26a) significantly increased the level of ROS in 4T1 cells, which could also be reversed by Ferrostatin-1 (fer-1) [1].

GPX4-IN-3 (26a) exertes antitumor activity and good biological safety in vivo [1]. Animal Model: Mouse 4T1 xenograft model [1]. Dosage: 15 and 30 mg/kg. Administration: Intravenous injection, every two days for a total of five times. Result: Significantly suppress tumor growth with a tumor growth inhibition (TGI) value of 33.2 and 55.1% at 15 and 30 mg/kg, respectively.

C29H24ClN3O3S

530.04

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years