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MAPK MEK

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.
Trametinib HOT
T2125CAS 871700-17-3
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...
Pelitinib
T2327CAS 257933-82-7
Pelitinib (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
BIX02189
T2416CAS 1094614-85-3
BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM.
CI1040 HOT
T2443CAS 212631-79-3
CI-1040 (PD184352) is an ATP non-competitive MEK1/2 inhibitor (IC50: 17 nM).
Binimetinib
T2508CAS 606143-89-9
Binimetinib (MEK162, ARRY-162, ARRY-438162) is an orally available inhibitor of MEK1/2 (IC50: 12 nM) in a cell-free assay.
BMS 599626
T2610CAS 714971-09-2
BMS-599626 has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.
PD 98059 HOT
T2623CAS 167869-21-8
PD98059 is a non-ATP competitive MEK inhibitor (IC50: 2/50 μM for MEK1/MEK2).
SL327
T2708CAS 305350-87-2
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.
Honokiol
T3001CAS 35354-74-6
Honokiol is the active principle of magnolia extract. It inhibits the activation of Akt and enhances the phosphorylation of ERK1/ERK2.
Cobimetinib
T3623CAS 934660-93-2
Cobimetinib is a selective inhibitor of mitogen-activated protein kinase kinase (MEK) (IC50: 0.9 nM). Cobimetinib specifically binds to and inhibits the catalyt...
TAK285
T6039CAS 871026-44-7
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...
URMC099
T6057CAS 1229582-33-5
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...
SCH772984 HOT
T6066CAS 942183-80-4
SCH 772984 is a potent inhibitor of ERK1/ERK2 (IC50: 4/1 nM) and has only weak inhibitory for other 300 tested kinases.
ZM 447439
T6077CAS 331771-20-1
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 ...
AZD8330
T6083CAS 869357-68-6
AZD8330 is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.
Pimasertib
T6131CAS 1236699-92-5
Pimasertib is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.
PD318088
T6152CAS 391210-00-7
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...
PD0325901 HOT
T6189CAS 391210-10-9
PD0325901 is a specific and non-ATP-competitive MEK inhibitor (IC50: 0.33 nM).
Selumetinib HOT
T6218CAS 606143-52-6
Selumetinib (AZD6244) is an effective, specific inhibitor of MEK1 and ERK1/2 phosphorylation (IC50: 14/10 nM).
U0126-EtOH HOT
T6223CAS 1173097-76-1
U0126-EtOH is a non-ATP competitive specific inhibitor of MEK1/2 (IC50: 0.07/0.06 μM).
BIX02188
T6324CAS 1094614-84-2
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,...
BMS536924
T6419CAS 468740-43-4
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/...
Refametinib
T6636CAS 923032-37-5
Refametinib (RDEA119, Bay 86-9766) is an effective, ATP non-competitive and specific inhibitor of MEK1/2 (IC50: 19/47 nM).
TAK733
T6692CAS 1035555-63-5
MEK Inhibitor TAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.
BI847325
T6785CAS 1207293-36-4
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.
GDC0623
T6843CAS 1168091-68-6
GDC-0623 is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.
RO5126766
T6971CAS 946128-88-7
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.
Epiberberine
T5S2361CAS 6873-09-2
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...
RO4987655
T5412CAS 874101-00-5
RO4987655 is an orally active and highly selective MEK inhibitor (IC50: 5.2 nM for MEK1/MEK2).
Trametinib DMSO solvate
T5857CAS 1187431-43-1
Trametinib DMSO solvate is a Highly Potent and Selective MEK Inhibitor that specifically inhibits MEK1/2(IC50 :2 nM)
GW284543
T7610CAS 790186-68-4
GW284543 is a selective inhibitor of MEK5 .
GW 284543 hydrochloride
T7742CAS 179246-08-3
GW 284543 hydrochloride is a selective inhibitor of MEK5 .
Hederacolchiside A1
T2P2806CAS 106577-39-3
Hederacolchiside A1 shows anti-leishmanial activity, it exhibits a strong antiproliferative activity on all stages of development of the parasite by altering me...
Bufarenogin
TN1459CAS 17008-65-0
Bufarenogin has inhibitory activity on human kidney Na(+)/K(+)-ATPase, it has cytotoxicity against HepG2 and MCF-7 human cancer cells.
Cajanin
TN1462CAS 32884-36-9
Cajanin has potential hypolipidemic effects,possibly via up-regulating the ABCA1 protein expression,subsequently resulting in increased macrophage cholesterol e...
Kaempferol 3-neohesperidoside
TN1819CAS 32602-81-6
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...
Rhamnocitrin
TN2151CAS 569-92-6
Rhamnocitrin can enhance the immune function, improve the formation of spleen cells of mice serum hemolysin of chicken red blood cell immune.
MS432
T13782CAS T13782
MS432 is a highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2.
EBI-1051
T15193CAS 1801896-05-8
EBI-1051 is a highly potent and orally efficacious inhibitor of MEK (IC50: 3.9 nM).
MEK-IN-1
T10675CAS 870600-45-6
MEK-IN-1 is a MEK inhibitor from patent WO2008076415A1.
Pavinetant
T16114CAS 941690-55-7
Pavinetant is an antagonist of the neurokinin-3 receptor (NK3R).
MEK inhibitor
T11993CAS 334951-92-7
MEK inhibitor is a potent MEK inhibitor with antitumor potency.
Bavachalcone
T3S0137CAS 28448-85-3
Bavachalcone is a major bioactive compounds isolated from Psoralea corylifolia L. it may be useful as a therapeutic drug for bone resorption-associated disease...
Demethylwedelolactone
T5S0689CAS 6468-55-9
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 ...
Actein
T7190CAS 18642-44-9
Actein has a stimulatory effect on osteoblastic bone formation or has potential activity against osteoporosis, it also can prevent oxidative damage to osteoblas...
Alpinumisoflavone
TN3397CAS 34086-50-5
Alpinumisoflavone has atheroprotective effects, may result from their ability to upregulate mechanisms promoting HDL-cholesterol and bile acid formation, it is ...
Boehmenan
TN3525CAS 57296-22-7
(±)-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...
Corylifol C
TN3711CAS 775351-91-2
Corylifol C and, to a lesser extent, xanthoangelol are potent protein kinase inhibitors (inhibitory concentration 50% values for epidermal growth factor recepto...
Griffipavixanthone
TN4166CAS 219649-95-3
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...
Uncarinic acid E
TN5201CAS 277751-61-8
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...
BIX 02189
T21295CAS 1265916-41-3
BIX02189 is a potent and selective inhibitor of MEK5 and ERK5(IC50 : 1.5 nM and 59 nM).
Isorhamnetin
T2836CAS 480-19-3
Isorhamnetin is the methylated metabolite of quercetin. Quercetin is an important dietary flavonoid with in vitro antioxidant activity. Isorhamnetin prevents en...
trans-Zeatin
TMS2181CAS 1637-39-4
Trans-Zeatina is the member of the plant growth hormone family known as cytokinins, which regulate cell division, development, and nutrient processing.