lck inhibitor 2

TG 100572 is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively).

TG 100801 Hydrochloride is a prodrug to treat age-related macular degeneration. TG 100572 is a inhibitor of multi-targeted kinase(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src,

A-770041 is an orally active and selective Lck inhibitor that inhibits concanavalin A-stimulated IL-2 production in whole blood and prevents cardiac allograft rejection. A-770041 reduces pulmonary fibrosis by inhibiting TGF-β production in regulatory T cells.

AZ-23 is an inhibitor of ATP-competitive and Trk kinase A B C. For TrkA, TrkB, FGFR1, Flt3, Ret, MuSk, Lck, the IC50s values are 2 nM, 8 nM, 24 nM, 52 nM, 55 nM, 84 nM, 99 nM, respectively.

RK-24466 (KIN 001-51) is a selective and potent Lck inhibitor, targeting Lck (64-509) and LckCD isoforms with IC50 values of less than 1 nM and 2 nM, respectively.

WH-4-023 (Dual LCK SRC inhibitor) is a potent and orally active Lck Src inhibitor. It also potently inhibits SIK.

ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A B than MEK1, Src, Lck and has little effect against CDK1 2 4, Plk1, Chk1, etc.

ITK inhibitor 6 is a selective and potent ITK inhibitor that acts on ITK (IC50: 4 nM), BTK (IC50: 133 nM), JAK3 (IC50: 320 nM), EGFR (IC50: 2360 nM), LCK (IC50: 155 nM). ITK inhibitor 6 inhibited the phosphorylation of PLCγ1 and ERK1 2 and showed anti-proliferative effect.

BMS-536924 (BMS 536924) is an ATP-competitive IGF-1R IR inhibitor with IC50 of 100 nM 73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1 2.

Lck inhibitor II is a cell-permeable, ATP binding site-targeting, tri-substituted pyrimidine that acts as a highly potent Lck (lymphocyte specific kinase) inhibitor

AMG-47a is a potent inhibitor of Lck and T cell proliferation. AMG-47a could promote the degradation of the KRAS oncoprotein. AMG-47a selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells.

RK-20448 is an ATP-competitive inhibitor of Lck, Src, KDR VEGF2R, and Tie-2. It also inhibits BLK, Csk, Fyn, and Lyn. RK-20448 is the cis isomer of A-419259

Lck Inhibitor III, a potent inhibitor of Lck, exhibits an IC50 value of 867 nM. Additionally, this compound effectively inhibits IL-2 synthesis in Jurkat cells, demonstrating an IC50 of 1.270 μM.

HPK1-IN-2 dihydrochloride, a potent and orally active inhibitor of hematopoietic progenitor kinase-1 (HPK1) with an IC 50 of less than 0.05 µM, demonstrates significant antitumor activity. It additionally exhibits inhibition of Lck kinase activity, with an IC 50 ranging from 0.05 to less than 0.5 µM, and Flt3 kinase activity, with an IC 50 of less than 0.05 µM [1].

Lck-IN-2 (compound 12a), an inhibitor of Lymphocyte-specific protein tyrosine kinase (Lck), demonstrates an IC50 of 10.6 nM. It displays efficacy in colon cancer cells, exhibiting GI50 values ranging from 0.24-1.26 μM. Furthermore, Lck-IN-2 induces apoptotic effects in Colo201 cells [1].