fer kinase

Cenisertib is A potent ATP-competitive multi-kinase inhibitor, showing inhibitory effects on the activity of Aurora-kinase-A B, ABL1, AKT, STAT5, FLT3, as well as kinase inhibitors of FER and its homolog. Cenisertib inhibits the growth of tumor mast cells (MCS) by inhibiting the activity of several different molecular targets. Cenisertib also inhibits tumor growth in pancreatic, breast, colon, ovarian and lung cancer and leukemia in xenograft models.

Ro3280 (Ro5203280) is an effective, specific inhibitor of PLK1(IC50=3, Kd=0.09 nM).

NG 25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1 (IC50s = 21.7 and 149 nM, respectively).1It also inhibits the Src family kinases Src and LYN (IC50s = 113 and 12.9 nM, respectively) and Abl family kinases (IC50s = 75.2 nM), as well as CSK, FER, and p38α (IC50s = 56.4, 82.3, and 102 nM, respectively). NG 25 (100 nM) prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively, in Gen2.2 cells in a concentration-dependent manner.2NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration-dependent manner.3It also reduces tumor growth and increases the number of TUNEL-positive tumor cells in a CT26KRASG12Dmouse orthotopic model of colorectal cancer. 1.Tan, L., Nomanbhoy, T., Gurbani, D., et al.Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2)J. Med. Chem.58(1)183-196(2015) 2.Pauls, E., Shpiro, N., Peggie, M., et al.Essential role for IKKβ in production of type 1 interferons by plasmacytoid dendritic cellsJ. Biol. Chem. 287(23)19216-19228(2012) 3.Ma, Q., Gu, L., Liao, S., et al.NG25, a novel inhibitor of TAK1, suppresses KRAS-mutant colorectal cancer growth in vitro and in vivoApoptosis24(1-2)83-94(2019)

TL13-22 is a potent inhibitor of Anaplastic Lymphoma Kinase (ALK) with an IC₅₀ value of 0.54 nM and does not lead to degradation of ALK proteins.TL13-22 is often used as a negative control for TL13-12 (induces ALK protein degradation) as a negative control.TL13-22 also induces degradation of other kinases, including Aurora A, FER, PTK2, and RPS6KA1.

E260 (Fer and FerT inhibitor) is a Fer FerT kinase inhibitor

NG25 trihydrochloride is a type II kinase inhibitor that inhibits MAP4K2 and TAK1. It also inhibits the Src family kinases Src and LYN and Abl family kinases as well as CSK, FER, and p38α. NG 25 prevents TNF-α-induced IKKα β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively. NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration-dependent manner. It also reduces tumor growth and increases the number of TUNEL-positive tumor cells in a CT26KRASG12D mouse orthotopic model of colorectal cancer.

DB1113 (Example 24) is a bifunctional compound designed for the targeted degradation of various kinases, including ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2, and ULK1. This capability positions DB1113 as a valuable tool for research into diseases or disorders associated with aberrant kinase activity [1].

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].