Lck degrader-1

Lck degrader-1 (compound 17) promotes the formation of a ternary complex between LCK and CRBN-DDB1, with an EC₅₀ of 77.1 nM^[1].
Lck degrader-1 induces CK1α degradation in CK1α-HiBiT HEK293 cells, with a DC₅₀ of 17.8 nM after 24 h of treatment; under the same conditions, its DC₅₀ against GSPT1 is > 10000 nM, indicating weak degradation activity against GSPT1^[1].
Lck degrader-1 reduces cell viability after 72 h of treatment in Dasatinib (HY-10181)-resistant KOPT-K1 cells harboring the LCK T316I gatekeeper mutation, with an LC₅₀ of 63.0 nM^[1].
Lck degrader-1 (1000 nM; 24 h) induces significantly weaker LCK degradation in LCK G415N KOPT-K1 cells than in cells expressing wild-type LCK, indicating that the G415-containing helical G-loop degron plays an important role in its mediated LCK degradation^[1].
Lck degrader-1 (1000 nM; 24 h) retains significant LCK degradation activity in KOPT-K1 cells harboring the LCK T316I mutation, whereas LCK degradation by the Dasatinib-based PROTAC SJ11646 is significantly impaired^[1].
Lck degrader-1 (1000 nM; 24 h) significantly reduces the protein level of CK1α in KOPT-K1 cells^[1].
Lck degrader-1 induces dose-dependent degradation of LCK in KOPT-K1 LCK-HiBiT cells, with a DC₅₀ of 103.4 nM at 4 h and 6.2 nM at 24 h^[1].
Lck degrader-1 reduces the viability of KOPT-K1 cells after 72 h of treatment, with an LC₅₀ value of 32.9 nM^[1].
Lck degrader-1 (1000 nM; 24 h) reduces LCK protein levels in these PDX-derived cells^[1].
Lck degrader-1 (72 h) exhibits dose-dependent cytotoxicity to varying degrees in a panel of T-ALL cell lines including CCRF-CEM, Jurkat, ALL-SIL, DND-41, Loucy, SUP-T1, KOPT-K1 and HSB-2, where different cell lines represent molecular subtypes such as NKX2-5, TAL1, TLX1, TLX3, ETP-like/HOXA9 and T-other^[1].

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