Lck Selective Inhibitors
|Catalog No.||Product Name||Information||Selective / Pan||IC50 / Ki|
RK-24466 (KIN 001-51, Lck inhibitor C 8863, C8863) is a potent and selective inhibitor of Lck that inhibits two constructs of the human lck kinase, lck (64-509) and lckcd with IC50 of < 0.001 μM and 0.002 μM, respectively.
|Selective||Lckcd, IC50: 0.002 μM; Lck (64-509), IC50: 0.001 μM|
WH-4-023 (KIN001-112, KIN112, Dual LCK/SRC inhibitor) is a potent and orally active Lck/Src inhibitor with IC50s of 2 nM and 6 nM in cell-free assays, respectively. Exhibits >300-fold selectivity against p38α and KDR. Also potently inhibits SIK (IC50 values are 10, 22 and 60 nM for SIK 1, 2 and 3 respectively) and displays selectivity over a range of closely related kinases.
|Selective||Lck, IC50: 2 nM|
CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
|Selective||LCK, IC50: 0.02 μM|
|S6567||Src Inhibitor 1||
Src Inhibitor 1 is a potent competitive inhibitor of both Src and Lck (IC50 = 44 and 88 nM, respectively), as well as Csk and Yes.
|Selective||Lck, IC50: 88 nM|
AMG-47a is a potent, nonselective inhibitor of Lck kinase with IC50 of 3.4 uM and it also inhibits T cell proliferation. AMG-47a exhibit anti-inflammatory activity (ED50) of 11 mg/kg in the anti-CD3-induced production of interleukin-2 (IL-2) in mice.
|Selective||LCK, IC50: 3.4 μM|
PP2 (AG 1879, AGL 1879), a Src family kinase inhibitor, potently inhibits Lck/Fyn with IC50 of 4 nM/5 nM in cell-free assays, ~100-fold less potent to EGFR, inactive for ZAP-70, JAK2 and PKA.
|Pan||LCK, IC50: 4 nM|
Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3.
|Pan||LCK, IC50: <4 nM|
PP1 (AGL 1872, EI 275) is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.
|Pan||LCK, IC50: 5 nM|
ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2.
|Pan||LCK, IC50: 43.7 nM|
|S8032||PRT062607 (P505-15) HCl||
PRT062607 (P505-15, BIIB057, PRT-2607) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70.
|Pan||LCK, IC50: 249 nM|
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