MEK

MEK is a member of the MAPK signaling cascade that is activated in melanoma. When MEK is inhibited, cell proliferation is blocked and apoptosis (controlled cell death) is induced.

Cat No.	product name
T2125	TrametinibHOT	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 MEK...
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	CI1040HOT	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 98059HOT	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 catalyt...
T6039	TAK285	TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aur...
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	SCH772984HOT	SCH 772984 is a potent inhibitor of ERK1/ERK2 (IC50: 4/1 nM) and has only weak inhibitory for other 300 tested kinases.
T6077	ZM 447439	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 ...
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-b...
T6189	PD0325901HOT	PD0325901 is a specific and non-ATP-competitive MEK inhibitor (IC50: 0.33 nM).
T6218	SelumetinibHOT	Selumetinib (AZD6244) is an effective, specific inhibitor of MEK1 and ERK1/2 phosphorylation (IC50: 14/10 nM).
T6223	U0126-EtOHHOT	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,...
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/...
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.
T6971	RO5126766	RO5126766 (CH5126766) is a dual RAF/MEK inhibitor with IC50 of 8.2 nM, 19 nM, 56 nM, and 160 nM for BRAF V600E, BRAF, CRAF, and MEK1, respectively. 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...
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 me...
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 e...
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 P...
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 is a major bioactive compounds isolated from Psoralea corylifolia L. it may be useful as a therapeutic drug for bone resorption-associated disease...
T5S0689	Demethylwedelolactone	Demethylwedelolactone is a natural product isolated from Eclipta alba, has trypsin inhibitory effect an IC50 of 3.0 μM. it exerts anti-invasive growth effect ...
T7190	Actein	Actein has a stimulatory effect on osteoblastic bone formation or has potential activity against osteoporosis, it also can prevent oxidative damage to osteoblas...
TN3397	Alpinumisoflavone	Alpinumisoflavone has atheroprotective effects, may result from their ability to upregulate mechanisms promoting HDL-cholesterol and bile acid formation, it is ...
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 i...
TN3711	Corylifol C	Corylifol C and, to a lesser extent, xanthoangelol are potent protein kinase inhibitors (inhibitory concentration 50% values for epidermal growth factor recepto...
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 mit...
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, resu...
T21295	BIX 02189	BIX02189 is a potent and selective inhibitor of MEK5 and ERK5(IC50 : 1.5 nM and 59 nM).
T2836	Isorhamnetin	Isorhamnetin is the methylated metabolite of quercetin. Quercetin is an important dietary flavonoid with in vitro antioxidant activity. Isorhamnetin prevents en...
TMS2181	trans-Zeatin	Trans-Zeatina is the member of the plant growth hormone family known as cytokinins, which regulate cell division, development, and nutrient processing.