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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.
| Molecular Weight | 530.61 |
| CAS Number | 1225383-33-4 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage | 2-8°C, sealed |
| 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.
[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
| Related Ligand for E3 Ligase Products |
|---|
| HaloPROTAC3
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
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
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
CC-90009 is a novel cereblon (CRBN) E3 ligase modulator and specifically targets GSPT1 (G1 to S phase transition 1) for proteasomal degradation. |
| VH032
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. |
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