non-atp competitive inhibitor

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6 15 2 3 3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7 0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis.

PD98059 is an MEK inhibitor that inhibits MEK1 and MEK2 (IC50=2 50 μM) and is non-ATP-competitive. PD98059 is also antagonistic as a ligand for AHR. PD98059 inhibits autophagy.

Mirdametinib (PD325901) is an MEK inhibitor (IC50=0.33 nM) with selective, non-ATP-competitive, and oral activity. Mirdametinib exhibits antitumor activity by inhibiting p-ERK1 2 expression and inducing apoptosis.

MK-8033 hydrochloride is an effective and orally active dual inhibitor of ATP competitive c-Met Ron, with 1 nM for c-Met and 7nM for Ron IC50. MK-8033 hydrochloride has a high affinity for activated kinase conformation, and is suitable for the study of breast cancer, bladder cancer, and non-small cell lung cancer (NSCLC).

Refametinib (RDEA119) (RDEA119, Bay 86-9766) is an effective, ATP non-competitive and specific inhibitor of MEK1 2 (IC50: 19 47 nM).

Tideglusib (NP031112), a non-ATP competitive inhibitor of glycogen synthase kinase 3 (GSK-3), is with anti-inflammatory and neuroprotective activities.

Tepotinib (EMD-1214063) is a c-MET tyrosine kinase inhibitor (IC50=3 nM) that is selective, orally active, and ATP-competitive. Tepotinib has antitumor effect and is used in the treatment of non-small cell lung cancer.

U0126-EtOH (U0126 Ethanol) is a non-ATP competitive specific inhibitor of MEK1 2 (IC50: 0.07 0.06 μM).

Alectinib (RG-7853) is an ALK inhibitor (IC50=1.9 nM, Kd=2.4 nM) that is selective, orally active, and ATP-competitive. Alectinib has antitumor activity and is used in the treatment of non-small cell lung cancer.

Chelerythrine Chloride is a cell-permeable inhibitor of protein kinase C, competitive with respect to the phosphate acceptor and non-competitive with respect to ATP.

Butyrolactone I (Olomoucin) is an ATP-competitive inhibitor of CDK and cdc2 kinase family. Butyrolactone I shows antitumor effects in non-small cell lung, small cell lung, and prostate cancer cell lines.

CI-1040 (PD 184352) (PD184352) is an ATP non-competitive MEK1 2 inhibitor (IC50: 17 nM).

Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578 nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride has anti-tumor effects.

AZD8330 (ARRY-704) is a novel, selective, non-ATP competitive MEK 1 2 inhibitor with IC50 of 7 nM. Phase 1.

Selumetinib (AZD6244) is a MEK1 2 inhibitor that inhibits MEK1 (IC50=14 nM) with potent selectivity and is non-ATP-competitive. Selumetinib has antitumor activity and is used for the treatment of neurofibromatosis type 1 (NF1).

GSK4418959 (IDE275) is an orally active, non-covalent, reversible, and selective WRN helicase inhibitor. GSK4418959 inhibits ATPase and DNA unwinding functions in an ATP-competitive manner. GSK4418959 can be used to study MSI-H related research.

GSK3-IN-3 is a mitochondrial autophagy (mitophagy) inducer and GSK-3 inhibitor (IC50: 3.01 μM) that induces parkin-dependent mitochondrial autophagy. GSK3-IN-3 is non-ATP and non-substrate competitive and neuroprotective against 6-OHDA.

Rigosertib sodium (ON-01910), a non-ATP-competitive inhibitor of PLK1(IC50=9 nM), exhibits 30-fold higher specificity activity over Plk2 and no effect on Plk3.

GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl.

GNF-5 is a specific non-ATP competitive inhibitor of Bcr-Abl (IC50: 0.22±0.1 uM, Wild-type Abl). It is an analog of GNF-2 with improved pharmacokinetic properties.

SP-146 is a selective, potent and non-ATP-competitive Aurora B inhibitor(IC50 : 0.316 nM).

Poloxin is a non-ATP competitive Polo-like Kinase 1 inhibitor targeting the polo-box domain (IC50: appr 4.8 μM).

Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibit