MEK

Inhibitory Selectivity
Catalog No.Inhibitor Name MEKMEK1MEK1/2MEK2MEK5Other
A10257Selumetinib
***
A10256PD0325901
****
A11029Trametinib
****
****
A10957U0126-EtOH
*
**
MKK6/p38 MAPK,MKK3/p38 MAPK
A10212PD184352
**
**
A10705PD98059
*
A10151BIX 02189
****
ERK5,TGFβR1
A10089Pimasertib
*
A10150BIX 02188
***
ERK5,TGFβR1
A11040TAK-733
****
A10115AZD8330
ERK phosphorylation
A11493Binimetinib
***
***
A14137SL-327
*
*
AP-1,MKK3/p38 MAPK
A11264Refametinib
**
**
A12974GDC-0623
****
A15762BI-847325
**
***
Aurora B,Aurora C,Aurora A
A11441Cobimetinib
***
A10704PD318088
A10453Honokiol
Akt-phosphorylation
A11247RO4927350
A13272RO4987655
****
A14019RO5126766 (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.



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Catalog No. Product Name Application Product Information
A10453 SALE

Honokiol

Antiangiogenic and Antitumor Agent
Honokiol 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.
A16044

PD 334581

MEK1 inhibitor
PD 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.
A16032

PD 198306

MEK inhibitor
PD 198306 is a potent, selective and non-ATP competitive MAPK/ERK-kinase (MEK) inhibitor.
A12974

GDC-0623

MEK1 inhibitor
GDC-0623 is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.
A14380

G-479

MEK inhibitor
G-479 is an potent MEK inhibitor. G-479 with polarity distributed throughout the molecule was shown improved bioactivity over GDC-0623 in many aspects.
A15762

BI-847325

MEK/Aurora Inhibitor
BI-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.
A15157

MEK inhibitor

MEK inhibitor
MEK inhibitor is a potent MEK inhibitor, antitumor agent.
A15051

Cobimetinib (R-enantiomer)

MEK inhibitor
Cobimetinib R-enantiomer is the R-enantiomer of Cobimetinib, which is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase(MEK1/2).
A15050

Cobimetinib (racemate)

MEK inhibitor
Cobimetinib is a potent, highly selective inhibitor of MEK1/2.
A11264

Refametinib

MEK inhibitor
Refametinib is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.
A14137 SALE

SL-327

MKK/MEK inhibitor
SL-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.
A10150

BIX02188

MEK5 inhibitor
BIX02188 is a potent and selective inhibitor of MEK5.
A11441 SALE

GDC-0973 (Cobimetinib)

MEK1 inhibitor
Cobimetinib (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.
A11493 SALE

MEK162 (ARRY-438162, Binimetinib)

MEK1/2 inhibitor
MEK162 (ARRY-438162) is a potent, selective, ATP uncompetitive inhibitor of MEK1/2.
A11247

RO4927350

MEK1/2 inhibitor
RO4927350 a potent and highly selective non-ATP-competitive MEK1/2 inhibitor.
A12866

Refametinib (RDEA-119, BAY 86-9766)

MEK1/2 inhibitor
Refametinib, also known as RDEA119, BAY 86-9766, is an orally bioavailable selective MEK inhibitor with potential antineoplastic activity.
A13119

Balamapimod (MKI-833)

Ras/Raf/MEK inhibitor
Balamapimod, also known as MKI-822, is a Ras/Raf/MEK inhibitor.
A14019

RO5126766 (CH5126766)

Raf/MEK dual inhibitor
RO5126766, 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.
A13750

Hypothemycin

-
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.
A10704

PD318088

MEK Inhibitor
PD318088 is an inhibitor of MEK1 AND MEK2.
A10115

AZD8330

MEK Inhibitor
AZD8330 is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.
A11040 SALE

TAK-733

MEK Inhibitor
TAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.
A10256 SALE

PD0325901

MEK inhibitor
PD0325901 is MEK inhibitor and non-competitive with ATP, Kiapp of 1 nM against activated MEK1 and MEK2.
A10257

AZD6244 (Selumetinib)

MEK inhibitor
AZD6244 (Selumetinib) also known as Selumetinib, ARRY142886, AZD-6244 & ARRY-142886 is MEK 1/2 inhibitor with GI50 values ranging from 14 to 50 nm.
A10705

PD98059

MEK Inhibitor
PD98059 is an equipotent antagonist of the aryl hydrocarbon receptor and inhibitor of mitogen-activated protein kinase kinase.
A10212 SALE

PD184352 (CI-1040)

MEK1/2 inhibitor
PD184352 (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.
A10957 SALE

U0126-EtOH

MEK inhibitor
U0126-EtOH is an inhibitor of both MEK1 and MEK2 with an IC50 of 72 nM and 58 nM respectively.
A10089 SALE

AS703026 (Pimasertib)

MEK1/2 inhibitor
AS703026 is a novel, selective, orally bioavailable MEK1/2 inhibitor that inhibits growth and survival of MM cells and cytokine-induced osteoclast differentiation.
A11029 SALE

GSK1120212 (JTP-74057, Trametinib)

MEK Inhibitor
GSK1120212 (JTP-74057) strongly prevented the activities of MEK1 and MEK2 kinases rather than activities of other 98 kinases.
A10151 SALE

BIX 02189

MEK inhibitor
BIX 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.
A13272

RO4987655

MEK1 inhibitor
RO4987655 is an orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), with potential antineoplastic activity.

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