MEK

<p>Lidocaine, an amide local anesthetic, reduces pain and inflammation by dampening ICAM-1, cytokines, and neutrophil influx.</p>

<p>Lidocaine HCl: local anesthetic, antiarrhythmic, stronger &amp; longer-lasting than procaine but shorter than bupivacaine/prilocaine.</p>

<p>Lidocaine Hydrochloride hydrate is an amide local anesthetic, has anti-inflammatory property.</p>

<p>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.</p>

<p>MEK/PI3K-IN-1 (6r) is a dual MEK/PI3K inhibitor; IC50: 124 nM (MEK1), 130 nM (PI3Kα), 236 nM (PI3Kδ). It reduces pAKT, pERK1/2, and hinders tumor growth.</p>

<p>BAY-6035 is an inhibitor of SET and MYND domain-containing protein 3 (SMYD3). BAY-6035 has more than 100-fold selectivity over other histone methyltransferases.</p>

<p>A unique collection of 365 compounds targeting MAPK signaling for drug discovery in MAPK related diseases;</p>

<p>A unique collection of 263 kinase inhibitors/regulators for specific targeting of kinases, ready for high-throughput screening and high-content screening.</p>

<p>MEK/PI3K-IN-2 is a potent dual inhibitor (MEK1 IC50: 352 nM, PI3Kα: 107 nM, PI3Kδ: 137 nM) that reduces pAKT, pERK1/2, and hinders tumor cell growth.</p>

<p>NST-628 is a pan-RAF-MEK molecular glue that prevents RAF from phosphorylating and activating MEK. NST-628 inhibits the RAF-MEK signaling complex.</p>

<p>Inactive analog of U0126(MEK-1/2 inhibitor), used as a negative control</p>

<p>Debromohymenialdisine is a natural product for research related to life sciences. The catalog number is T35596 and the CAS number is 75593-17-8.</p>

<p>Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib which is a selective MEK inhibitor.</p>

<p>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.</p>

<p>MEK4 inhibitor-1 targets MEK4 enzyme in pancreatic cancer, IC50=61 nM.</p>

<p>DS03090629, an orally active MEK inhibitor, functions by competitively inhibiting MEK activity in the presence of ATP. This compound demonstrates strong binding affinity to both MEK and phosphorylated MEK, with dissociation constants (Kd) of 0.11 and 0.15 nM, respectively. It has shown efficacy in suppressing the proliferation of melanoma cell lines that overexpress BRAF mutations, achieving IC50 values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 is thus considered promising for anti-melanoma therapies.</p>

<p>PD 198306: a MEK inhibitor with antihyperalgesic properties, reduces Streptozocin-boosted active ERK1.</p>

<p>Midkine is a heparin-binding growth factor, originally reported as the product of a retinoic acid-responsive gene during embryogenesis, but currently viewed as</p>

<p>Midkine is a heparin-binding growth factor, originally reported as the product of a retinoic acid-responsive gene during embryogenesis, but currently viewed as</p>

<p>Anti-Midkine Antibody (5T766) is an antibody targeting Midkine. Anti-Midkine Antibody (5T766) can be used in ELISA, IHC.</p>

<p>Midkine is a heparin-binding growth factor, originally reported as the product of a retinoic acid-responsive gene during embryogenesis, but currently viewed as</p>

<p>Pimasertib (AS703026) is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.</p>

<p>Zapnometinib (ATR-002) is a MEK inhibitor.</p>

<p>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.</p>

<p>Anemarsaponin B has anti-inflammatory effect in LPS-treated RAW 264.7macrophages, the effect is associated with the inhibition of NF-κB transcriptional activity</p>

<p>BIX02189 is a potent and selective inhibitor of MEK5 and ERK5(IC50 : 1.5 nM and 59 nM).</p>

<p>PD98059 is an MEK inhibitor that inhibits MEK1 and MEK2 (IC50=2/50 μM) and is non-ATP-competitive.</p>

<p>CI-1040 (PD 184352) (PD184352) is an ATP non-competitive MEK1/2 inhibitor (IC50: 17 nM).</p>

<p>Refametinib (RDEA119) (RDEA119, Bay 86-9766) is an effective, ATP non-competitive and specific inhibitor of MEK1/2 (IC50: 19/47 nM).</p>

<p>RGB-286638 free base inhibits CDKs (1-5 nM), weaker on CDK7/6.</p>

<p>Selumetinib (AZD6244) is a selectivity and non-ATP-competitive MEK1/2 inhibitor. Selumetinib has antitumor activity. Cost-effective and quality-assured.</p>

<p>TAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.</p>

<p>APS-2-79: KSR-dependent MEK inhibitor, blocks ATP biotin at KSR2, IC50 of 120 nM, disrupts Ras-MAPK signaling.</p>

<p>Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate)) is a Highly Potent and Selective MEK Inhibitor that specifically inhibits MEK1/2(IC50 :2 nM)</p>

<p>Binimetinib (ARRY-162) is a MEK1/2 inhibitor (IC50=12 nM) with selective and oral activity. Binimetinib has antitumor activity. Cost-effective and quality-assured.</p>

<p>GW 284543 hydrochloride is a selective inhibitor of MEK5 .</p>

<p>Mirdametinib (PD325901) is an MEK inhibitor (IC50=0.33 nM) with selective, non-ATP-competitive, and oral activity.</p>

<p>GDC-0623 (RG 7421) is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.</p>

<p>AZD8330 (ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.</p>

<p>Sodium aurothiomalate (Miochrysin) inhibits PKC-ι, TrxR; used as an anti-rheumatic and has anti-tumor properties.</p>

<p>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.</p>

<p>PD184161 is a novel, orally-active MEK inhibitor. PD184161 inhibited MEK activity (IC50 = 10-100 nM) in a time- and concentration-dependent manner[1].</p>

<p>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.</p>

<p>U0126-etoh (U0126 Ethanol) is a non-ATP competitive inhibitor of MEK1 (IC50=72 nM) and MEK2 (IC50=58 nM) with selectivity, inhibit autophagy. Low-Cost!</p>

<p>trans-Zeatin ((E)-Zeatin) is the member of the plant growth hormone family known as cytokinins, which regulate cell division, development, and nutrient</p>

<p>Cobimetinib (GDC-0973) is a MEK1 inhibitor with selective and oral activity. Cobimetinib exhibits antitumor activity. Cost-effective and quality-assured.</p>

<p>U0126, an effective and selective non-competitive inhibitor of MAP kinase, inhibits MEK-1 and MEK-2 with IC50 values of 0.07 and 0.06 μM respectively.</p>

<p>APS-2-79 hydrochloride (APS-2-79 HCl) is a MAPK antagonist that modulating KSR-dependent MAPK signalling by antagonizing RAF heterodimerization.</p>

<p>Isorhamnetin (3-methylquercetin) is the methylated metabolite of quercetin.</p>

<p>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-</p>

<p>Trametinib (GSK1120212), an ATP-noncompetitive MEK 1/2 inhibitor (IC50: 0.7/0.9 nM), weakly inhibits &gt;180 kinases.</p>

<p>RO4987655 (RG7167) is an orally active and highly selective MEK inhibitor (IC50: 5.2 nM for MEK1/MEK2).</p>

<p>GW284543 (UNC10225170) is a selective inhibitor of MEK5 .</p>

<p>Trametiglue, a potent Trametinib derivative, selectively targets KSR-MEK and RAF-MEK through unique binding.</p>

<p>Avutometinib potassium, a MEKi, blocks Delta and Omicron infection in airway cells, potentially lessening disease severity.</p>

<p>MEK1 inhibitor</p>

<p>MEK inhibitor is a MEK receptor and cell cycle protein/CDK complex inhibitor with antitumor activity that can be used to study tumor cell proliferation.</p>

<p>JTP-70902 is a protein kinase inhibitor with antineoplastic activity.</p>

<p>MEK-IN-1 is a MEK inhibitor.</p>

<p>MEK-IN-4 is a MEK inhibitor that can be used to study inflammatory diseases and cancer.</p>

<p>(R)-PD 0325901CL, a PD 0325901CL isomer, is a MEK inhibitor used in cancer research, effective against cancer cells in vitro and in vivo.</p>

<p>Cobimetinib racemate (Cobimetinib (racemate)) (GDC-0973 racemate) is a selective inhibitor of MEK.Cobimetinib racemate is also known as a mitogen-activated</p>

<p>MEK-IN-6 hydrate (compound 69), a MEK inhibitor, exhibits an IC50 value of 2 nM in A375 cells [1].</p>

<p>MS934, a novel VHL-recruiting MEK 1/2 degrader, exhibits potent anti-proliferative effects on HT-29 cell growth, achieving a GI50 of 0.023 μM.</p>

<p>GSK1790627, the N-deacetylated metabolite of Trametinib, represents an orally active MEK inhibitor that promotes autophagy and triggers apoptosis [1].</p>

<p>Nedometinib (NFX-179) is a MEK1 inhibitor with anticancer and antitumor activities, which can be used to study malignant tumors.</p>

<p>MEK1/2-IN-2 is a potent, ATP-competitive MEK1/2 inhibitor that exhibits equal inhibitory effects on wild-type MEK1/2 and a group of MEK1/2 mutant cells.</p>

<p>Refametinib R enantiomer (RDEA119 R enantiomer) is an MEK inhibitor with an EC50 of 2.0-15 nM.Refametinib (R enantiomer) has anticancer activity and can be used</p>

<p>EBI-1051 is a highly potent and orally efficacious inhibitor of MEK (IC50: 3.9 nM).</p>

<p>G-479, a potent MEK inhibitor and improved analogue of GDC-0623, has distributed polarity enhancing bioactivity.</p>

<p>Luvometinib is an inhibitor of the mitogen-activated protein kinase (MEK) with antitumor activity.</p>

<p>MEK4 Inhibitor-2, a novel MEK4 inhibitor, demonstrates efficacy against pancreatic adenocarcinoma, exhibiting an IC50 value of 83 nM.</p>