Kelch-like ECH-associated protein 1 (KEAP1) is a cytoplasm and nucleus protein that contains one BACK (BTB/Kelch associated) domain, one BTB (POZ) domain, and six Kelch repeats. KEAP1 is a key regulator of the NRF2 transcription factor, which transactivates the antioxidant response element (ARE) and upregulates numerous proteins involved in antioxidant defense. KEAP1 targets NRF2 for ubiquitination and proteolytic degradation and as such is responsible for the rapid turnover of NRF2. KEAP1 retains NFE2L2/NRF2 in the cytosol. KEAP1 functions as a substrate adapter protein for the E3 ubiquitin ligase complex formed by CUL3 and RBX1.
The recombinant human KEAP1/GST chimera consists of 860 amino acids and has a calculated molecular mass of 97.37 kDa. The recombinant protein migrates as an approximately 109 kDa band in SDS-PAGE under reducing conditions.
A DNA sequence encoding the human KEAP1 (NP_036421.2) (Gln2-Cys624) was expressed with the N-terminal polyhistidine-tagged GST tag at the N-terminus.
Lyophilized from sterile 20mM Tris, 500mM NaCl, 10% glycerol, pH 7.4.
Storage | Stable for up to twelve months from date of receipt at -20℃ to -80℃ |
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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