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Results for "

mek1/2

" in TargetMol Product Catalog
  • Inhibitors & Agonists
    54
    TargetMol | Inhibitors_Agonists
  • Peptide Products
    1
    TargetMol | Peptide_Products
  • PROTAC Products
    5
    TargetMol | PROTAC
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    5
    TargetMol | Natural_Products
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    2
    TargetMol | Recombinant_Protein
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    TargetMol | Isotope_Products
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    TargetMol | Antibody_Products
MEK1/2-IN-3
T205362
MEK1 2-IN-3 (Compound M15) is an inhibitor of MEK1, with an IC50 value of 10.29 nM. It effectively suppresses tumor cell proliferation and migration, induces apoptosis, and exhibits good liver microsomal stability. MEK1 2-IN-3 is applicable in the study of solid tumors.
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MEK1/2-IN-2
T63547
MEK1 2-IN-2 is a potent, ATP-competitive MEK1 2 inhibitor that exhibits equal inhibitory effects on both wild-type MEK1 2 and a range of MEK1 2 mutant cells.
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10-14 weeks
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Trametinib (DMSO solvate)
Trametinib DMSO solvate, Trametinib dimethyl sulfoxide, JTP-74057 (DMSO solvate), GSK-1120212 (DMSO solvate)
T58571187431-43-1
Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate)) is a highly potent and selective MEK inhibitor that specifically inhibits MEK1 2 (IC50: 2 nM).
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PD98059
PD 98059
T2623167869-21-8
PD98059 is an MEK inhibitor that inhibits MEK1 and MEK2 (IC50=2 50 μM) and is non-ATP-competitive. PD98059 is also antagonistic as a ligand for AHR. PD98059 inhibits autophagy.
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TargetMol | Inhibitor Hot
EF24
EF-24, EF 24, 3,5-Bis[(2-fluorophenyl)Methylene]-4-piperidinone
T27242342808-40-6In house
EF24 (3,5-Bis[(2-fluorophenyl)Methylene]-4-piperidinone) treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK. EF24 shows potent anti-tumor activity in oral squamous cell carcinoma (OSCC) via deactivation of the MAPK ERK signaling pathway.
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Refametinib
BAY 86-97661, BAY 869766, RDEA119
T6636923032-37-5In house
Refametinib (RDEA119) (RDEA119, Bay 86-9766) is an effective, ATP non-competitive and specific inhibitor of MEK1 2 (IC50: 19 47 nM).
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CI-1040
PD 184352
T2443212631-79-3
CI-1040 (PD 184352) (PD184352) is an ATP non-competitive MEK1 2 inhibitor (IC50: 17 nM).
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Binimetinib
ARRY-438162, ARRY-162, MEK162
T2508606143-89-9
Binimetinib (ARRY-162) is a MEK1 2 inhibitor (IC50=12 nM) with selective and oral activity. Binimetinib has antitumor activity for the treatment of metastatic melanoma that cannot be resected or has a BRAF V600E or V600K mutation.
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SL327
SL 327, SL-327
T2708305350-87-2
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.
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TargetMol | Inhibitor Sale
AZD8330
ARRY-424704, ARRY-704
T6083869357-68-6
AZD8330 (ARRY-704) is a novel, selective, non-ATP competitive MEK 1 2 inhibitor with IC50 of 7 nM. Phase 1.
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selumetinib
AZD6244, ARRY-142886
T6218606143-52-6
Selumetinib (AZD6244) is a MEK1 2 inhibitor that inhibits MEK1 (IC50=14 nM) with potent selectivity and is non-ATP-competitive. Selumetinib has antitumor activity and is used for the treatment of neurofibromatosis type 1 (NF1).
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U0126-EtOH
U0126 Ethanol, U0126
T62231173097-76-1
U0126-EtOH (U0126 Ethanol) is a non-ATP competitive specific inhibitor of MEK1 2 (IC50: 0.07 0.06 μM).
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GW 5074
GW5074, Raf1 Kinase Inhibitor I
T6525220904-83-6
GW 5074 (Raf1 Kinase Inhibitor I)(IC50=9 nM) is an effective and specific c-Raf inhibitor. It has no effect on the activities of JNK1 2 3, MEK1, MKK6 7, CDK1 2, c-Src, p38 MAP, VEGFR2 or c-Fms.
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TAK-285
TAK285, TAK 285
T6039871026-44-7
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, Aurora B, Lck, CSK etc. Phase 1.
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4-6 weeks
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TargetMol | Inhibitor Sale
5Z-7-Oxozeaenol
FR148083, L783279, LL-Z 1640-2
T14055253863-19-3
5Z-7-Oxozeaenol (FR148083) is a potent, irreversible and selective inhibitor of transforming growth factor (TGF)-β-activated kinase 1 with IC50 of 8.1 nM for TAK1 and low activity against MEK1 with IC50 of 411 nM, it is also an inhibitor of VEGF-R2 with IC50 of 52 nM.
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Agerafenib hydrochloride
RXDX-105 hydrochloride, CEP-32496 (hydrochloride)
T149281227678-26-3
Agerafenib hydrochloride, a highly potent inhibitor of BRAFV600E (Kd: 14 nM), demonstrates significant efficacy.
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8-10 weeks
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(S,R,S)-AHPC-Me-C10-Br
T186682836297-55-1
(S,R,S)-AHPC-Me-C10-Br is a chemically synthesized conjugate and ligand-linker for E3 ligase, consisting of MS432 for MEK1 2 inhibitors and a VHL E3 ligase linker.
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MEK/RAF-IN-1
T200267
MEK RAF-IN-1 (Compound 16b) serves as an inhibitor targeting both MEK and RAF, demonstrating potent efficacy with IC 50 values reported at 28 nM for MEK1, and 3 nM for both BRAF and BRAFV600E. This compound exhibits significant antitumor capabilities, effectively curbing cell proliferation in vitro in MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Furthermore, MEK RAF-IN-1 significantly restricts tumor growth in xenograft mouse models employed in the study of colorectal cancer.
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MEK ligand-2
T201410212631-56-6
MEK ligand-2, a ligand for the target protein for PROTAC (Ligand for Target Protein for PROTAC), functions as an inhibitor for both MEK1 and MEK2. This compound plays a crucial role in MS934, which is a VHL-recruiting MEK1 2 PROTAC degrader.
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(S,R,S)-AHPC-Me-12-((4-Bromobutyl)amino)dodecanamide
T201787
(S,R,S)-AHPC-Me-12-((4-Bromobutyl)amino)dodecanamide comprises a VHL ligand for recruiting E3 ubiquitin ligases and a PROTAC linker. This compound is used in synthesizing PROTACs such as MS934. MS934 represents a novel and improved VHL-recruiting MEK1 2 PROTAC degrader.
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agerafenib
RXDX-105, CEP-32496, CEP32496, CEP 32496
T20701188910-76-0
Agerafenib (CEP32496) is a highly potent inhibitor of BRAF.
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PD184161
T21635212631-67-9
PD184161 is a novel, orally-active MEK inhibitor. PD184161 inhibited MEK activity (IC50 = 10-100 nM) in a time- and concentration-dependent manner[1].
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TargetMol | Inhibitor Sale
TCS PIM-1 1
SC 204330
T2253491871-58-0
TCS PIM-1 1 (SC 204330)(sc-204330) is an effective and specific ATP-competitive Pim-1 kinase inhibitor (IC50: 50 nM), exhibiting good specificity over MEK1 MEK2 and Pim-2 (IC50s > 20,000 nM).
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RGB-286638 free base
T2378784210-88-4
RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM 2 nM 3 nM 4 nM 5 nM for cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2 cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6.
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