ML385 ML385 is a novel and specific NRF2 inhibitor with an IC50 of 1.9 μM. It inhibits the downstream target gene expression of NRF2. NRF2 regulates the activity of several ferroptosis and lipid peroxidation-related proteins. In vitro
ML385 shows anti-tumor activity in NSCLC (subcutaneous and orthotopic NSCLC models) both as a single agent and in combination with carboplatin. The PK profile tested in CD-1 mice shows that ML385 has a half-life (t1/2 = 2.82 h) after IP injection (30 mg/kg). ML385 could alleviate the pancreatic injury.
In vivo
Cell Data
cell lines：Rat leukemic cell lines RCL/0, RO/1 and K7 and human myelomonocytic leukemic U937
1.Fan Wenbo, Zhou Jianwu. (2023) Icariside II Suppresses Ferroptosis to Protect Against MPP+-Induced Parkinson's Disease through Keap1/Nrf2/GPX4 Signaling. CHINESE JOURNAL OF PHYSIOLOGY, 66 (6):(437). [PMID:38149556]
2.Bing-hao Lin, Run-xun Ma, Jing-tao Wu, Shi-qi Du, Yi-yun Lv, Hao-nan Yu, Wei Zhang, Shu-ming Mao, Guang-yao Liu, Yi-tian Bu, Zi-hao Chen, Chen Jin, Zong-yi Wu, Lei Yang. (2023) Cinnamaldehyde Alleviates Bone Loss by Targeting Oxidative Stress and Mitochondrial Damage via the Nrf2/HO-1 Pathway in BMSCs and Ovariectomized Mice. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, 71 (45):(17362–17378). [PMID:37917162]
3.Yue Tang, Yueyue Kang, Xinru Zhang, Caiyi Cheng. (2023) Mesenchymal stem cell exosomes as nanotherapeutics for dry age-related macular degeneration. JOURNAL OF CONTROLLED RELEASE, 357 (356). [PMID:37028452]
4.Hengju Ge, Jiaxin Li, Yang Xu, Jiahong Xie, Naymul Karim, Fujie Yan, Jianling Mo, Wei Chen. (2023) Ameliorative effect of Fructus Gardeniae against lipotoxicity associated hepatocytes injury through activating Nrf2 signaling pathway. Food Bioscience, 53 (102596). [PMID:]
1.Fan Wenbo, Zhou Jianwu. (2023) Icariside II Suppresses Ferroptosis to Protect Against MPP+-Induced Parkinson's Disease through Keap1/Nrf2/GPX4 Signaling. CHINESE JOURNAL OF PHYSIOLOGY, 66 (6):(437). [PMID:38149556]
2.Bing-hao Lin, Run-xun Ma, Jing-tao Wu, Shi-qi Du, Yi-yun Lv, Hao-nan Yu, Wei Zhang, Shu-ming Mao, Guang-yao Liu, Yi-tian Bu, Zi-hao Chen, Chen Jin, Zong-yi Wu, Lei Yang. (2023) Cinnamaldehyde Alleviates Bone Loss by Targeting Oxidative Stress and Mitochondrial Damage via the Nrf2/HO-1 Pathway in BMSCs and Ovariectomized Mice. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, 71 (45):(17362–17378). [PMID:37917162]
3.Yue Tang, Yueyue Kang, Xinru Zhang, Caiyi Cheng. (2023) Mesenchymal stem cell exosomes as nanotherapeutics for dry age-related macular degeneration. JOURNAL OF CONTROLLED RELEASE, 357 (356). [PMID:37028452]
4.Hengju Ge, Jiaxin Li, Yang Xu, Jiahong Xie, Naymul Karim, Fujie Yan, Jianling Mo, Wei Chen. (2023) Ameliorative effect of Fructus Gardeniae against lipotoxicity associated hepatocytes injury through activating Nrf2 signaling pathway. Food Bioscience, 53 (102596). [PMID:]
