lck in 1

Lck-IN-1 is a potent inhibitor of lymphocyte protein tyrosine kinase (Lck) [1].

OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel growth (angiogenesis) in tumors.

HPK1-IN-2 (Thieno[2,3-b]pyridin-6(7H)-one, 4-amino-5-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-HPK1-IN-2) is a potent and orally active inhibitor of hematopoietic progenitor kinase-1 (HPK1; IC50<0.05 μΜ). It also inhibits Lck (0.05 μΜinase activities with antitumor activity.

GSK2646264 (Compound 44) is a highly effective and specific inhibitor of spleen tyrosine kinase (SYK) with a pIC50 of 7.1. It also inhibits multiple kinases, including LCK (pIC50 5.4), LRRK2 (pIC50 5.4), GSK3β (pIC50 5.3), JAK2 (pIC50 5), VEGFR2 (pIC50 4.5), Aurora B (pIC50 <4.6), and Aurora A (pIC50 <4.3). Notably, GSK2646264 demonstrates skin penetrability, reaching both the epidermis and dermis [1].

AMG-25 (c-Kit-IN-5-1) is a selective and potent c-Kit inhibitor that inhibits c-Kit, KDR, p38, Lck, and Src, and can be used in the study of mast cell-associated fibrosis.

DB0614 (Example 21) is a bifunctional compound designed for the targeted degradation of kinases, effectively breaking down AAK1, AURKA, BMP2K, CAMKK1, CDK16, CML, CDK6, EIF2AK2, FER, GAK, LCK, LIMK2, MAP3KH, MAPK8, MAPK9, NEK9, PLK4, PTK2B, SIK2, STK17A, STK17B, ULK1, ULK3, and WEE1. This compound has potential applications in research on diseases or disorders caused by aberrant kinase activity [1].

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.

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].

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].

2,3,4,6,8-Pentahydroxy-1-methylxanthone, a xanthone derivative of Wardomyces anomalus, exhibits significant antioxidant activities and functions as an inhibitor of the p56 lck tyrosine kinase, with potential applications in the treatment of cardiovascular disease [1].

HPK1-IN-55 (compound 19) is a selective and orally active inhibitor of hematopoietic progenitor kinase 1 (HPK1) with an IC50 of less than 0.51 nM. It exhibits exceptional kinase selectivity, being over 637 times more selective for HPK1 compared to GCK kinase and over 1022 times compared to LCK. HPK1-IN-55 possesses anti-cancer properties.