MEK1/2
MEK1/2, also known as MAPKK (mitogen-activated protein kinase kinase), is a kinase enzyme which phosphorylates MAPK (mitogen-activated protein kinase).
Products for MEK1/2
- Cat.No. Product Name Information
- GC12851 10Z-Hymenialdisine Pan kinase inhibitor
- GC15240 APS-2-79 APS-2-79 is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATPbiotin binding to KSR2 within the KSR2-MEK1 complexe with an IC50 of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling.
- GN10063 Arctigenin
- GC17030 AZD6244(Selumetinib) A highly selective inhibitor of MEK1/2
- GC14643 AZD8330 MEK 1/2 inhibitor
- GC33305 Balamapimod (MKI 833) Balamapimod (MKI 833) (MKI 833) is a reversible Ras/Raf/MEK inhibitor with potential anti-tumor activity.
- GC17828 BI-847325 dual inhibitor of MEK and Aurora kinases
- GC15693 BIX 02188 MEK5 inhibitor,potent and selective
- GC12220 BIX 02189 Selective MEK5 inhibitor
- GC35684 CHMFL-EGFR-202 CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ?10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines.
- GC10033 Cobimetinib A potent, orally available MEK1 inhibitor
- GC14337 Cobimetinib (R-enantiomer)
- GC17426 Cobimetinib (racemate)
- GC35719 Cobimetinib hemifumarate Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC50 value against MEK1 is 4.2 nM.
- GC14247 GDC-0623 MEK1 inhibitor, potent and ATP-uncompetitive
- GC12006 GDC-0994 GDC-0994 (GDC-0994) is an orally active ERK kinase inhibitor with an IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.
- GC36199 GW284543 GW284543 (UNC10225170) is a selective MEK5 inhibitor. GW284543 reduces pERK5, and decreases endogenous MYC protein.
- GC43885 Hypothemycin A resorcylic acid lactone polyketide
- GN10023 Isorhamnetin
- GC17608 Lidocaine Anasthetic and class Ib antiarrhythmic agent
- GC33831 Lidocaine hydrochloride (Lignocaine hydrochloride) Lidocaine hydrochloride (Lignocaine hydrochloride) (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence.
- GC64904 MAP855 MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2.
- GC11277 MEK inhibitor
- GC33388 MEK-IN-1 MEK-IN-1 is a MEK inhibitor extracted from patent WO2008076415A1.
- GC12843 MEK162 (ARRY-162, ARRY-438162) MEK162 (ARRY-162, ARRY-438162) (MEK162) is an oral and selective MEK1/2 inhibitor. MEK162 (ARRY-162, ARRY-438162) (MEK162) inhibits MEK with an IC50 of 12 nM.
- GC64292 MS432 MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively.
- GC15646 PD 184161 MEK1/2 inhibitor
- GC17964 PD 198306 MEK1/2 inhibitor
- GC17485 PD 334581 MEK1 inhibitor
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GC10397
PD0325901
A MEK inhibitor that sustains stem cell renewal
- GC63554 PD0325901-O-C2-dioxolane PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader.
- GC12989 PD184352 (CI-1040) PD184352 (CI-1040) (PD 184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.
- GC10110 PD318088 Allosteric MEK1/2 inhibitor, non-ATP competitive
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GC12819
PD98059
PD98059 is a potent and selective MEK inhibitor with an IC50 of 2 μM.
- GC18050 Pimasertib (AS-703026) Pimasertib (AS-703026) (AS703026) is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor.
- GC14732 PLX-4720 An orally-available inhibitor of the B-raf mutant B-RafV600E
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GC16872
Refametinib
MEK 1/ MEK 2 inhibitor
- GC37516 Refametinib R enantiomer Refametinib R enantiomer is a MEK inhibitor extracted from patent WO2007014011A2, compound 1022, has an EC50 of 2.0-15 nM.
- GC37522 RGB-286638 A multi-kinase inhibitor
- GC37523 RGB-286638 free base A multi-kinase inhibitor
- GC12141 RO4987655 MEK inhibitor
- GC12406 RO5126766(CH5126766) RO5126766(CH5126766) (CH5126766) is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAFV600E, CRAF, MEK, and BRAF (IC50: 8.2, 56, 160 nM, and 190 nM, respectively).
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GC16001
SCH772984
A selective inhibitor of ERK1/2
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GC14647
SCH772984 HCl
ERK1/2 inhibitor
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GC15044
SCH772984 TFA
ERK1/2 inhibitor
- GC38653 Selumetinib sulfate Selumetinib (AZD6244) is selective, non-ATP-competitive oral?MEK1/2?inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
- GC15359 SL-327 Selective MEK1/2 inhibitor
- GC10209 TAK-733 MEK allosteric site inhibitor
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GC41573
Theaflavin 3,3'-digallate
Theaflavin-3,3'-digallate (TFDG) is a major polyphenol found in black tea with diverse biological activities.
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GC70053
Trametiglue
Trametiglue is a derivative of Trametinib that binds to KSR-MEK and RAF-MEK with unprecedented potency and selectivity through a unique interface interaction.
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GC13508
Trametinib (GSK1120212)
An inhibitor of MEK1 and MEK2
- GC15260 Trametinib DMSO solvate
- GC30162 trans-Zeatin A cytokinin plant growth regulator
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GC45099
U-0126
A MEK inhibitor
- GC15061 U0124 Inactive analog of U0126(MEK-1/2 inhibitor), used as a negative control
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GC12807
U0126-EtOH
U0126-EtOH-EtOH (U0126 has potent inhibition on MEK1 and MEK2 with IC50s of 72 nM and 58 nM, respectively
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GC13412
Vemurafenib (PLX4032, RG7204)
An inhibitor of mutant V600E and wild type B-Raf
- GC63264 Zapnometinib Zapnometinib (PD0184264), an active metabolite of CI-1040, is a MEK inhibitor, with an IC50 of 5.7 nM.