N6F11 is a novel ferroptosis inducer that selectively triggers the ubiquitination degradation of GPX4 by binding to the specific structural domain of TRIM25, a ubiquitinated E3 ligase, which is expressed in tumor cells, leading to ferroptosis in cancer cells.
| Molecular Weight | 311.19 |
| Formula | C13H8Cl2N2OS |
| CAS Number | 851398-76-0 |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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| GPX4-IN-3
GPX4-IN-3 is a potent glutathione peroxidase 4 (GPX4) inhibitor that selectively induces ferroptosis.1 μM of GPX4-IN-3 inhibited 71.7% of GPX4 activity. |
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MMRi62 is a ferroptosis inducer targeting MDM2-MDM4 (negative regulator of the oncogene p53), which induces ferroptosis accompanied by an increase in reactive oxygen species (ROS) and lysosomal degradation of ferritin heavy chain (FTH1).MMRi62 displays p53-independent apoptosis activity and induces autophagy in pancreatic ductal adenocarcinoma (PDAC) cells. MMRi62 shows p53-independent pro-apoptosis activity and induces autophagy in pancreatic ductal adenocarcinoma (PDAC) cells.) In addition, MMRi62 caused proteasomal degradation of mutant p53 and was active in vivo in an in situ xenograft PDAC mouse model characterized by high-frequency mutations in KRAS and TP53. |
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