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| Catalog No. | Inhibitor Name | MEK | MEK1 | MEK1/2 | MEK2 | MEK5 | Other |
|---|---|---|---|---|---|---|---|
| A10257 | Selumetinib | *** | |||||
| A10256 | PD0325901 | **** | |||||
| A11029 | Trametinib | **** | **** | ||||
| A10957 | U0126-EtOH | * | ** | MKK6/p38 MAPK,MKK3/p38 MAPK | |||
| A10212 | PD184352 | ** | ** | ||||
| A10705 | PD98059 | * | |||||
| A10151 | BIX 02189 | **** | ERK5,TGFβR1 | ||||
| A10089 | Pimasertib | * | |||||
| A10150 | BIX 02188 | *** | ERK5,TGFβR1 | ||||
| A11040 | TAK-733 | **** | |||||
| A10115 | AZD8330 | ERK phosphorylation | |||||
| A11493 | Binimetinib | *** | *** | ||||
| A14137 | SL-327 | * | * | AP-1,MKK3/p38 MAPK | |||
| A11264 | Refametinib | ** | ** | ||||
| A12974 | GDC-0623 | **** | |||||
| A15762 | BI-847325 | ** | *** | Aurora B,Aurora C,Aurora A | |||
| A11441 | Cobimetinib | *** | |||||
| A10704 | PD318088 | ||||||
| A10453 | Honokiol | Akt-phosphorylation | |||||
| A11247 | RO4927350 | ||||||
| A13272 | RO4987655 | **** | |||||
| A14019 | RO5126766 (CH5126766) | * | BRAF, CRAF |
Notes:
1.Hover mouse over "" to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of "" is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
38 Item(s)
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PD 198306
Catalog No. A16032 MEK inhibitorPD 198306 is a potent, selective and non-ATP competitive MAPK/ERK-kinase (MEK) inhibitor. Learn More -
SL-327
Catalog No. A14137 MKK/MEK inhibitorSL-327 is a selective inhibitor of MEK1 and MEK2 (IC50 values are 0.18 and 0.22 μM respectively); blocks hippocampal LTP in vitro. Brain penetrant in vivo, blocking fear conditioning and learning in rats, and producing neuroprotection in mice, following systemic administration. Learn More -
Refametinib
Catalog No. A11264 MEK inhibitorRefametinib is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively. Learn More -
Cobimetinib (racemate)
Catalog No. A15050 MEK inhibitorCobimetinib is a potent, highly selective inhibitor of MEK1/2. Learn More -
Cobimetinib (R-enantiomer)
Catalog No. A15051 MEK inhibitorCobimetinib R-enantiomer is the R-enantiomer of Cobimetinib, which is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase(MEK1/2). Learn More -
MEK inhibitor
Catalog No. A15157 -
BI-847325
Catalog No. A15762 MEK/Aurora InhibitorBI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1. Learn More -
G-479
Catalog No. A14380 MEK inhibitorG-479 is an potent MEK inhibitor. G-479 with polarity distributed throughout the molecule was shown improved bioactivity over GDC-0623 in many aspects. Learn More -
GDC-0623
Catalog No. A12974 MEK1 inhibitorGDC-0623 is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1. Learn More -
AZD6244 (Selumetinib)
Catalog No. A10257 MEK inhibitorAZD6244 (Selumetinib) also known as Selumetinib, ARRY142886, AZD-6244 & ARRY-142886 is MEK 1/2 inhibitor with GI50 values ranging from 14 to 50 nm. Learn More -
PD 334581
Catalog No. A16044 MEK1 inhibitorPD 334581 is used in biological studies to evaluate halogen bonding as a novel interaction for rational drug design. It is also an inhibitor of MEK1. Learn More -
EPZ031686
Catalog No. A16375 SMYD3/ MEKK2 inhibitorEPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a Ki=1.2 and 1.1 nM respectively. Learn More -
GW284543
Catalog No. A18808 MEK5 inhibitorGW284543, also known as UNC10225170;, is a potent and selective MEK5 inhibitor with the potential for cancer treatment. Learn More -
EBI-1051
Catalog No. A13176 MEK inhibitorEBI-1051 is a highly potent and orally efficacious MEK inhibitor with an IC50 of 3.9 nM. Learn More -
Cobimetinib hemifumarate
Catalog No. A18033 MEK1 inhibitorCobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC50 value against MEK1 is 4.2 nM. Learn More -
Trametinib (DMSO solvate)
Catalog No. A21450 MEK inhibitorTrametinib DMSO solvate (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is a potent MEK inhibitor that specifically inhibits MEK1/2, with an IC50 value of about 2 nM. Learn More -
BIX02189
Catalog No. A21729 MEK5 inhibitorBIX02189 is a potent and selective MEK5 inhibitor with an IC50 of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC50 of 59 nM. Learn More -
PD184161
Catalog No. A22601 -
PD0325901
Catalog No. A10256 MEK inhibitorPD0325901 is MEK inhibitor and non-competitive with ATP, Kiapp of 1 nM against activated MEK1 and MEK2. Learn More -
PD98059
Catalog No. A10705 MEK InhibitorPD98059 is an equipotent antagonist of the aryl hydrocarbon receptor and inhibitor of mitogen-activated protein kinase kinase. Learn More -
Refametinib (RDEA-119, BAY 86-9766)
Catalog No. A12866 MEK1/2 inhibitorRefametinib, also known as RDEA119, BAY 86-9766, is an orally bioavailable selective MEK inhibitor with potential antineoplastic activity. Learn More -
U0126-EtOH
Catalog No. A10957 MEK inhibitorU0126-EtOH is an inhibitor of both MEK1 and MEK2 with an IC50 of 72 nM and 58 nM respectively. Learn More -
MEK162 (ARRY-438162, Binimetinib)
Catalog No. A11493 MEK1/2 inhibitorMEK162 (ARRY-438162) is a potent, selective, ATP uncompetitive inhibitor of MEK1/2. Learn More -
GDC-0973 (Cobimetinib)
Catalog No. A11441 MEK1 inhibitorCobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Learn More -
Honokiol
Catalog No. A10453 Antiangiogenic and Antitumor AgentHonokiol is a lignan present in the cones, bark, and leaves of Magnolia grandiflora that has shown pro-apoptotic effects in melanoma, sarcoma, myeloma, leukemia, bladder, lung, prostate, oral squamous cell carcinoma and colon cancer cell lines. Learn More -
GSK1120212 (JTP-74057, Trametinib)
Catalog No. A11029 MEK InhibitorGSK1120212 (JTP-74057) strongly prevented the activities of MEK1 and MEK2 kinases rather than activities of other 98 kinases. Learn More -
BIX 02189
Catalog No. A10151 MEK inhibitorBIX 02189 is a selective dual MEK5 and ERK5 (or BMK1) kinase inhibitor, with IC50 values of 1.5, 59, 580 and >6200 nM for MEK5, ERK5, TGFbR1 and other closely related kinases respectively. Learn More -
PD318088
Catalog No. A10704 -
PD184352 (CI-1040)
Catalog No. A10212 MEK1/2 inhibitorPD184352 (CI-1040) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM in cell-based assays, 100-fold more selective for MEK1/2 than MEK5. Phase 2. Learn More -
AS703026 (Pimasertib)
Catalog No. A10089 MEK1/2 inhibitorAS703026 is a novel, selective, orally bioavailable MEK1/2 inhibitor that inhibits growth and survival of MM cells and cytokine-induced osteoclast differentiation. Learn More -
TAK-733
Catalog No. A11040 MEK InhibitorTAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity. Learn More -
AZD8330
Catalog No. A10115 MEK InhibitorAZD8330 is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1. Learn More -
RO5126766 (CH5126766)
Catalog No. A14019 Raf/MEK dual inhibitorRO5126766, also known as CH5126766, is a protein kinase inhibitor specific for the Raf and MEK mitogen-activated protein kinases (MAPKs) with potential anti-neoplastic activity. Learn More -
BIX02188
Catalog No. A10150 -
RO4927350
Catalog No. A11247 MEK1/2 inhibitorRO4927350 a potent and highly selective non-ATP-competitive MEK1/2 inhibitor. Learn More -
Balamapimod (MKI-833)
Catalog No. A13119 Ras/Raf/MEK inhibitorBalamapimod, also known as MKI-822, is a Ras/Raf/MEK inhibitor. Learn More -
RO4987655
Catalog No. A13272 MEK1 inhibitorRO4987655 is an orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), with potential antineoplastic activity. Learn More -
Hypothemycin
Catalog No. A13750 Hypothemycin is a resorcylic acid lactone polyketide. It was found to inhibit the proliferation of mouse and human T cells stimulated with anti-CD3 mAb + PMA and of human PBMC stimulated with anti-CD3 mAb alone. Learn More
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