LC-04-045

LC-04-045 is a NEK7 (NIMA-related kinase 7) molecular glue degrader (MGD) . LC-04-045 demonstrates potent activity of NEK7 degradation with a DC50 (half-maximal degradation) of 7 nM and a Dmax (maximum degradation) of 90% in MOLT-4 cells. LC-04-045 displays high selectivity for NEK7 across the proteome. LC-04-045 degrades NEK7 mediated by the ubiquitin-proteasome system (UPS) and relies on the glycine 57 (G57) -containing degron motif in NEK7. LC-04-045 effectively inhibits secretion of IL-1β and IL-18 with IC50s of 33.03 nM and 32.99 nM, respectively. LC-04-045 is potential for inflammatory diseases research[1].

C32H28ClN5O3

566.05

O=C([C@@H](N(CC1=C2C=CC(C3=CN=C4CN(CC5=CC=CC=C5C6=CC=CC=C6Cl)CCN43)=C1)C2=O)CC7)NC7=O

Interleukin Related; NEKs

IL-1; IL-8; NEK7

99.56

DMSO : 100 mg/mL (ultrasonic)

-20°C, 3 years; 4°C, 2 years (Powder)

Room Temperature