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.
|Solubility (25°C)||DMSO 90 mg/mL|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
 Yasmina Filali-Mouncef, et al. The ménage à trois of autophagy, lipid droplets and liver disease
 Yifan Chen, et al. Phosphorylation regulates cullin-based ubiquitination in tumorigenesis
 Dhanusha A Nalawansha, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine
 Ye Xu, et al. Emerging views of mitophagy in immunity and autoimmune diseases
 Jun Araya, et al. PRKN-regulated mitophagy and cellular senescence during COPD pathogenesis
|Related Ligand for E3 Ligase Products|
HaloPROTAC3 is a conjugate of ligands for E3 and 16-atom-length linker, and it is also a highly potent and efficacious degrader of GFP-HaloTag7 fusion proteins with a DC50 of 19 nM.
Golcadomide (CC-99282) is a potent and orally active CRBN E3 ligase modulator (CELMoD).CC-99282 co-induces effective and targeted degradation of Ikaros and Aiolos with CRBN.CC-99282 can be used in studies of non-Hodgkin's lymphoma.
ZXH-1-161 is a potent cereblon (CRBN) regulator with an IC50 of 39 μM in wild-type MM1.S cells. ZXH-1-161 has selective degradation activity against GSPT1. ZXH-1-161 can be used in the study of multiple myeloma.
CC-90009 is a novel cereblon (CRBN) E3 ligase modulator and specifically targets GSPT1 (G1 to S phase transition 1) for proteasomal degradation.
VH032 is a VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. VH032 is a VHL/HIF-1α interaction inhibitor with a Kd value of 185 nM.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.