K67 is a specific inhibitor against the interaction between KEAP1 (Kelch-like ECH-associated protein 1) DC (double glycine repeat and C-terminal region) domain and S349-phosphorylated (human Ser349, mouse Ser351) KIR (Keap1-interacting region) of p62/SQSTM1, thereby preventing phospho-p62 from blocking KEAP1-DC and NRF2 (nuclear factor erythroid 2-related factor 2) DLGex motif association. K67 effectively inhibits the proliferation of HCC (hepatocellular carcinoma) cultures (by 59% of Huh7 cells post 72 h 50 μM K67 treatment) with high cellular p62 S351-phosphorylation by restoring KEAP1-driven NRF2 ubiquitination and degradation.
Molecular Weight | 582.69 |
Formula | C29H30N2O7S2 |
CAS Number | 2046250-48-8 |
Solubility (25°C) | DMSO: 10 mg/mL |
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.
[3] I Fried, et al. Merkel cell carcinoma
[5] R Mushin. The occurrence of enteropathogenic Escherichia coli 0128: K67 (B12)
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