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E3 ligase Ligand 4

Cat. No. M9834
E3 ligase Ligand 4 Structure
Synonym:

Thalidomide 4-fluoride

Size Price Availability Quantity
10mg USD 49  USD49 In stock
50mg USD 79  USD79 In stock
100mg USD 108  USD108 In stock
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Quality Control & Documentation
Biological Activity

E3 ligase Ligand 4 (Thalidomide 4-fluoride) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein, it can connect to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.

Chemical Information
Molecular Weight 276.22
Formula C13H9FN2O4
CAS Number 835616-60-9
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Mikołaj Słabicki, et al. Small-molecule-induced polymerization triggers degradation of BCL6

[2] Tasuku Ishida, et al. E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones

[3] Takumi Ito, et al. Molecular mechanisms of thalidomide and its derivatives

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

[5] Jinfang Zhang, et al. Cyclin D-CDK4 kinase destabilizes PD-L1 via cullin 3-SPOP to control cancer immune surveillance

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Keywords: E3 ligase Ligand 4, Thalidomide 4-fluoride supplier, Ligand for E3 Ligase, inhibitors, activators


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