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Table 1 Inducers of ferroptosis

From: Induction and application of ferroptosis in cancer therapy

Target Compound/Drug Mechanism Tumour type Refs
Class I FINs
 SLC7A11 Erastin Inhibit SLC7A11 and prevent cystine import, combine with VDAC2/3 Glioma, lung cancer, fibrosarcoma, melanoma, breast cancer, cervical cancer, RCC [7, 29, 30]
Piperazine erastin (PE) Inhibit SLC7A11 and prevent cystine import Fibrosarcoma [33]
Imidazole ketone erastin (28) Inhibit SLC7A11 and prevent cystine import DLBCL [20]
Sulfasalazine Inhibit SLC7A11 Breastcancer, glioblastoma, fibrosarcoma, NSCLC, prostate cancer [7, 97]
Sorafenib Inhibit SLC7A11 AML, HCC, neuroblastoma, NSCLC, RCC [65]
Glutamate Inhibit SLC7A11 - [7, 17]
 GCL Buthionine sulfoximine (113) Inhibit the GCL and reduce GSH synthesis Melanoma, neuroblastoma [33, 70, 115]
 GSH Cyst(e)inase Degrade cysteine and cystine, reduce GSH levels Prostate cancer, chronic lymphocytic leukemia and pancreatic cancer [107, 116]
Cisplatin Combine with GSH to inactivate GPX4 Ovarian cancer, pancreatic cancer, NSCLC, urothelial cancer [94, 117,118,119]
Class II and III FINs
 GPX4 RSL3 Inhibit GPX4 directly Fibrosarcoma, NSCLC, pancreatic cancer,
leukemia
[19, 33, 120]
FIN56 Combine and activate SQS to reduce CoQ10 Fibrosarcoma [77, 111]
ML162(DPI7), DPI12, ML210(DPI10), DPI13 Inhibit GPX4 covalently - [33]
Altretamine Inhibit GPX4 Lymphoma, sarcoma, ovarian cancer [77]
FINO2 Oxidize Fe2+ and PUFAs, promote the accumulation of ROS; indirectly inactivate GPX4; Fibrosarcoma [33, 55]
Class IV FINs
 Iron Heme Up-regulate HMOX1 expression and increase LIP Glioblastoma, leukemia [34, 38]
Withaferin A Up-regulate HMOX1 expression and increase LIP at middle dose and inactivate GPX4 at high doses Breast cancer, Neuroblastoma [82, 121]
BAY 11–7085 Up-regulate HMOX1 expression and increase LIP CRC, cervical cancer [83]
Artesunate Oxidize Fe2+, promote the accumulation of ROS, induce ferritinophagy Pancreatic cancer [122,123,124,125,126]
Dihydroartemisinin Oxidize Fe2+, promote the accumulation of ROS, induce ferritinophagy and inhibit ferritin synthesis Ovarian cancer
Siramesine, lapatinib Decrease SLC40A1, increase transferrin and LIP Breast cancer [113]
Neratinib Decrease SLC40A1, increase transferrin and LIP Breast cancer, CRC [127]
Salinomycin Decrease SLC40A1, increase transferrin and LIP Various solid tumour types [128]
Others
 ROS BAY 87–2243 Combine with mitochondrial respiratory chain complex I NSCLC [83]
 FSP1 iFSP1 Inhibit the reduction of CoQ10 by FSP1 Fibrosarcoma, NSCLC [109, 110]
 HMGCR Statins Combine as lipid- lowering agent, in oncology phase I trials; CoQ10 deletion Breast cancer, AML, HCC, MM, Fibrosarcoma, NSCLC [111, 127, 129]
 Nrf2 Trigonelline, brusatol Nrf2 inhibition HCC, NSCLC [34, 130]
  1. AML acute myeloid leukaemia, CRC colorectal cancer, GSH glutathione; HCC hepatocellular carcinoma, MM multiple myeloma, NA not available, NSCLC non- small- cell lung cancer, RCC renal cell carcinoma, DLBCL diffuse large B cell lymphoma