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E3 ligase Ligand 8

Cat. No. M14866
E3 ligase Ligand 8 Structure
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Biological Activity

E3 ligase Ligand 8 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 8 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.

Chemical Information
Molecular Weight 530.61
CAS Number 1225383-33-4
Solubility (25°C) DMSO 90 mg/mL
Storage 2-8°C, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Yasmina Filali-Mouncef, et al. The ménage à trois of autophagy, lipid droplets and liver disease

[2] Yifan Chen, et al. Phosphorylation regulates cullin-based ubiquitination in tumorigenesis

[3] Dhanusha A Nalawansha, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine

[4] Ye Xu, et al. Emerging views of mitophagy in immunity and autoimmune diseases

[5] Jun Araya, et al. PRKN-regulated mitophagy and cellular senescence during COPD pathogenesis

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