KT-474, also known as KT-I-417 and SAR444656, is an orally bioavailable degrader of IRAK4. KT-474 is a heterobifunctional small-molecule degrader of IRAK4 composed of ligands to the E3 ligase cereblon (CRBN) and IRAK4 joined by a chemical linker. KT-474 forms a ternary complex with CRBN and IRAK4, leading to the ubiquitination and proteasomal degradation of IRAK4. KT-474 potently degraded IRAK4 in lymphocytes and monocytes with the half-maximal degradation concentration in the 1–2 nM range and a maximum degradation of 100%. KT-474 exhibited more potent and stronger downregulation of both R848 (TLR7/8)-induced and lipopolysaccharide (LPS: TLR4)-induced IL-6 and IL-8 production by PBMCs. KT-474 also blocked TLR9-mediated NF-κB activation by CpG-B in B cells, whereas PF-06550833 had no effect
MedKoo Cat#: 130269
Name: KT-474
CAS#: 2432994-31-3
Chemical Formula: C44H49F2N11O6
Exact Mass: 865.3835
Molecular Weight: 865.94
Elemental Analysis: C, 61.03; H, 5.70; F, 4.39; N, 17.79; O, 11.09
The following data is based on the product molecular weight 865.94 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
