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MEK
T2125 Trametinib Trametinib is an ATP-noncompetitive inhibitor of MEK 1/2 (IC50s: 0.7/0.9 nM). It shows low inhibition for more than 180 kinases, including B-Raf, c-Raf, and MEK5.
T2327 Pelitinib Pelitinib (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
T2416 BIX02189 BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM.
T2443 CI1040 CI-1040 (PD184352) is an ATP non-competitive MEK1/2 inhibitor (IC50: 17 nM).
T2508 Binimetinib Binimetinib (MEK162, ARRY-162, ARRY-438162) is an orally available inhibitor of MEK1/2 (IC50: 12 nM) in a cell-free assay.
T2610 BMS 599626 BMS-599626 has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.
T2623 PD 98059 PD98059 is a non-ATP competitive MEK inhibitor (IC50: 2/50 μM for MEK1/MEK2).
T2708 SL327 SL327 is a selective inhibitor for MEK1/2 with IC50 of 0.18 μM/0.22 μM; able to transport through the blood-brain barrier.
T3001 Honokiol Honokiol is the active principle of magnolia extract. It inhibits the activation of Akt and enhances the phosphorylation of ERK1/ERK2.
T3623 Cobimetinib Cobimetinib is a selective inhibitor of mitogen-activated protein kinase kinase (MEK) (IC50: 0.9 nM). Cobimetinib specifically binds to and inhibits the catalytic activity of MEK1,
T6057 URMC099 URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM).
T6066 SCH772984 SCH 772984 is a potent inhibitor of ERK1/ERK2 (IC50: 4/1 nM) and has only weak inhibitory for other 300 tested kinases.
T6083 AZD8330 AZD8330 is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.
T6131 Pimasertib Pimasertib is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.
T6152 PD318088 PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binding simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.
T6189 PD0325901 PD0325901 is a specific and non-ATP-competitive MEK inhibitor (IC50: 0.33 nM).
T6218 Selumetinib Selumetinib (AZD6244) is an effective, specific inhibitor of MEK1 and ERK1/2 phosphorylation (IC50: 14/10 nM).
T6223 U0126-EtOH U0126-EtOH is a non-ATP competitive specific inhibitor of MEK1/2 (IC50: 0.07/0.06 μM).
T6324 BIX02188 BIX02188 is a specific MEK5 inhibitor (IC50: 4.3 nM), also inhibits ERK5 catalytic activity (IC50: 810 nM), and does not inhibit closely related kinases MEK1/2, JNK2, and ERK2.
T6419 BMS536924 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.
T6636 Refametinib Refametinib (RDEA119, Bay 86-9766) is an effective, ATP non-competitive and specific inhibitor of MEK1/2 (IC50: 19/47 nM).
T6692 TAK733 MEK Inhibitor TAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.
T6785 BI847325 BI-847325 is a selective dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively.
T6843 GDC0623 GDC-0623 is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.
T5S2361 Epiberberine 1. Epiberberine may be caused drug interactions based on CYP2D6 enzyme. 2. Epiberberine has anti-adipogenic effect is mediated by downregulation of the Raf/MEK1/ERK1/2 and AMPKα/
T5412 RO4987655 RO4987655 is an orally active and highly selective MEK inhibitor (IC50: 5.2 nM for MEK1/MEK2).
T5857 Trametinib DMSO solvate Trametinib DMSO solvate is a Highly Potent and Selective MEK Inhibitor that specifically inhibits MEK1/2(IC50 :2 nM)
T7610 GW284543 GW284543 is a selective inhibitor of MEK5 .
T7742 GW 284543 hydrochloride GW 284543 hydrochloride is a selective inhibitor of MEK5 .
T2P2806 Hederacolchiside A1 Hederacolchiside A1 shows anti-leishmanial activity, it exhibits a strong antiproliferative activity on all stages of development of the parasite by altering membrane integrity and
TN1459 Bufarenogin Bufarenogin has inhibitory activity on human kidney Na(+)/K(+)-ATPase, it has cytotoxicity against HepG2 and MCF-7 human cancer cells.
TN1462 Cajanin Cajanin has potential hypolipidemic effects,possibly via up-regulating the ABCA1 protein expression,subsequently resulting in increased macrophage cholesterol efflux and RCT, it ca
TN1819 Kaempferol 3-neohesperidoside Kaempferol 3-neohesperidoside has insulin-like properties in terms of glucose lowering, it stimulates glucose uptake in the rat soleus muscle via the PI3K and PKC pathways and, at
TN2151 Rhamnocitrin Rhamnocitrin can enhance the immune function, improve the formation of spleen cells of mice serum hemolysin of chicken red blood cell immune.
T13782 MS432 MS432 is a highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2.
T15193 EBI-1051 EBI-1051 is a highly potent and orally efficacious inhibitor of MEK (IC50: 3.9 nM).
T10675 MEK-IN-1 MEK-IN-1 is a MEK inhibitor from patent WO2008076415A1.
T16114 Pavinetant Pavinetant is an antagonist of the neurokinin-3 receptor (NK3R).
T11993 MEK inhibitor MEK inhibitor is a potent MEK inhibitor with antitumor potency.
T3S0137 Bavachalcone Bavachalcone has antibiotic or anticancer activities, it may be useful as a therapeutic drug for bone resorption-associated diseases.Bavachalcone can protect the endothelial functi
T5S0689 Demethylwedelolactone Demethylwedelolactone has trypsin inhibitory effect, it exerts anti-invasive growth effect on breast cancer cells.
T7190 Actein Actein has a stimulatory effect on osteoblastic bone formation or has potential activity against osteoporosis, it also can prevent oxidative damage to osteoblasts in osteoporotic p
TN3397 Alpinumisoflavone Alpinumisoflavone has atheroprotective effects, may result from their ability to upregulate mechanisms promoting HDL-cholesterol and bile acid formation, it is endowed with estroge
TN3525 Boehmenan (±)-Boehmenan shows potent protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity in vitro with the IC(50) values of 43.5 uM, it inhibits PTP1B activity in a competitive mann
TN3711 Corylifol C Corylifol C and, to a lesser extent, xanthoangelol are potent protein kinase inhibitors (inhibitory concentration 50% values for epidermal growth factor receptor (EGFR): 1.1 and 4.
TN4166 Griffipavixanthone Griffipavixanthone inhibits the growth of human Non-small-cell lung cancer H520 cells in dose- and time-dependent manners, it induces cell apoptosis through mitochondrial apoptotic
TN5201 Uncarinic acid E Uncarinic acid E has anti-cancer activity, it induces apoptosis in HepG2 cells via accumulation of p53, alters the Bax/Bcl-2 ratio, and activates caspases, resulting in cytochrome
T21295 BIX 02189 BIX02189 is a potent and selective inhibitor of MEK5 and ERK5(IC50 : 1.5 nM and 59 nM).
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