MEK Inhibitor

Cobimetinib-¹³C₆ (GDC-0973-¹³C₆; XL518-¹³C₆) racemate is the deuterium labeled Cobimetinib (racemate) (HY-13078). Cobimetinib racemate (GDC-0973 racemate; XL518 racemate) is the racemate of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.

MEK ligand-2, a MEK1 and MEK2 inhibitor, is a ligand for target protein for PROTAC of MS934 (HY-153863). MS934 is a VHL-recruiting MEK 1/2 PROTAC degrader.

MEK4 IN-3 (Compound 39) is a selective MEK4 inhibitor with IC₅₀s of 78   and 2920 nM for MEK4 and RSK4, respectively. MEK4 IN-3 reduces toxicity in cells. MEK4 IN-3 can be used for liver failure, particularly nonalcoholic fatty liver disease (NAFLD) research.

Map2k2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Map2k2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

MAP2K2 Human Pre-designed siRNA Set A contains three designed siRNAs for MAP2K2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

MO-2097 is a RAF-1/HIF-1α inhibitor. MO-2097 induces RAF-1 destabilization, leading to a reduction in EMT-associated transcription factors and mesenchymal markers. MO-2097 inhibits HIF-1a protein expression mediated by hnRNPA2B1 under hypoxic and mimetic hypoxia. MO-2097 induces mitochondrial ROS, which leads to apoptosis in cells. MO-2097 effectively suppresses colorectal cancer metastasis by inhibiting the RAF/MEK/ERK signaling pathway. MO-2097 attenuates tumor growth in a xenograft HCT116 cell mouse model. MO-2097 can be used for the study of colorectal cancer.

BAY-866, a sulfamide campound, is an allosteric MEK1 inhibitor with an IC₅₀ of 14 nM. BAY-866 inhibits cell growth of A375 (BRAF) and HCT116 (K-Ras) with IC₅₀s of 13 nM and 277 nM, respectively. BAY-866 inhibits tumor growth in K-Ras-mutated A549 xenograft model.

VEGFR2/C-RAF kinase-IN-1 is a type II dual kinase inhibitor targeting VEGFR2 and C-RAF, with IC₅₀ values of 12.22 nM and 38.04 nM, respectively. VEGFR2/C-RAF kinase-IN-1 binds VEGFR2 and CRAF in a Type-II mode and inhibits the downstream Raf-MEK-ERK signaling cascade. VEGFR2/C-RAF kinase-IN-1 induces cell cycle arrest, apoptosis, and intracellular ROS accumulation in H1299 cells, while partially inhibiting P-gp efflux function. VEGFR2/C-RAF kinase-IN-1 can be used for cancer research, such as non-small cell lung cancer and liver cancer.

BRAFV600E/JNK-IN-1 (Compound 14c) is an inhibitor of JNK1, JNK2, JNK3 and BRAFV600E, with IC₅₀ values of 0.51 μM, 0.53 μM, 1.02 μM and 0.009 μM, respectively. BRAFV600E/JNK-IN-1 can inhibit the phosphorylation of MEK1/2 and ERK1/2. In addition, BRAFV600E/JNK-IN-1 can inhibit tumor cell proliferation, NO release and PGE2 production, and has anti-tumor and anti-inflammatory activities.

SL43 is an orally active and potent SOS1 inhibitor with a K_d of 0.16 μM. SL43 disrupts SOS1-KRAS interaction, inhibits SOS1-mediated nucleotide exchange on KRAS mutants, and suppresses RAS-MAPK signaling. SL43 exerts antiproliferative activity against KRAS-mutant cancer cells, induces early apoptosis and G1 phase cell cycle arrest, and reduces phosphorylated MEK and ERK levels. SL43 suppresses tumor growth in a colorectal cancer xenograft model.

ST-168 is an orally active MEK/PI3K inhibitor with an IC₅₀ of 182 nM against MEK1 and IC₅₀ values ​​of 69.2, 41.7, 1482 and 2293 nM against PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ respectively. ST-168 completely inhibits the phosphorylation of ERK1/2 and AKT and induces cancer cell death in a 3D tumor sphere model. ST-168 demonstrates significant antitumor effects in the A375 melanoma mouse model. ST-168 improves the ocular toxicity profile of MEK inhibitors, showing lower caspase activation levels, indicating reduced apoptosis induction. ST-168 can be used in melanoma research.

SMK-17 is a selective, non-ATP-competitive MEK1/MEK2 inhibitor with IC₅₀s of 62 nM and 56 nM, respectively. SMK-17 binds to the allosteric pocket of MEK1/2. SMK-17 induces apoptosis in tumor cell lines harboring β-catenin mutations.

Nuvrumetinib (PAS-004) is a macrocyclic MEK inhibitor. Nuvrumetinib functionally inhibits MEK1/2, thereby suppressing pERK in tumors. Nuvrumetinib inhibits the proliferation of NRAS-mutant cancer cells. Nuvrumetinib can be used in studies related to NRAS^G12C-mutant solid tumors, neurofibromatosis type 1 (NF1), RASopathies and laminopathies.

Map2k2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Map2k2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Binimetinib-d₃ (MEK162-d₃) is deuterium labeled Binimetinib. Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC₅₀ of 12 nM.

(R)-PD 0325901CL is an isomer of PD 0325901CL. PD 0325901CL is a selective inhibitor of mitogen-activated protein kinase kinase (MEK) involved in cancer research. PD 0325901CL inhibits the growth of cancer cells in vitro and in vivo.

Swerchirin is an orally active, plant-derived xanthone that acts as an inhibitor of the Raf/MEK/ERK signaling pathway. Swerchirin downregulates the expression of phosphorylated MEK and phosphorylated ERK, induces mitochondrial apoptosis and cell cycle arrest, regulates Bcl-2 family proteins, triggers cytochrome c release, activates caspases, and drives PARP cleavage. Swerchirin reduces blood glucose levels in rat models under fasting, fed, glucose-loaded conditions, and following treatment with Tolbutamide (HY-B0401). Swerchirin can be used in research related to ovarian cancer, liver injury, and diabetes.

X-370 is a PI3Kδ inhibitor (IC₅₀ = 7 nM). X-370 inhibits the survival of leukemia cells, inducing G1 arrest and apoptosis. X-370 blocks PDK1 binding and phosphorylation of MEK1/2, eliminating Akt and Erk1/2 signaling. X-370 can be used in research on B-cell acute lymphoblastic leukemia (B-ALL).

Map2k5 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Map2k5 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

PD-254552 is a MEK inhibitor. PD-254552 exhibits hepatotoxicity and gastrointestinal toxicity in mice.