MEK Inhibitor

Saucerneol is a lignans that can be isolated from Saururus chinensis. Saucerneol inhibits LPS-induced or Con A-induced lymphocytes proliferation. Saucerneol inhibits mixed lymphocyte response. Saucerneol also inhibits mitogens-induced cytokines secretion.

Map2k1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Map2k1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

MEK-IN-5 is a potent MEK inhibitor and NO donor. MEK-IN-5 significantly reduces the levels of pMEK and pERK in a dose-dependent and time-dependent manner. MEK-IN-5 induces apoptosis in MDA-MB-231 cells.

Avutometinib (CH5126766) (potassium) is a RAF/MEK clamp that potently inhibits RAF/MEK kinase activity and induces dominant negative RAF-MEK complexes preventing phosphorylation of MEK by ARAF, BRAF and CRAF. Avutometinib (potassium) shows anti-proliferative potency across tumor cell lines carrying KRAS mutations including PDAC cell lines. Avutometinib (potassium) induces tumor inhibition and increases survival in a KRAS/p53 pancreatic cancer mouse model. Avutometinib (potassium) is promising for research of low-grade-serous-ovarian-carcinoma (LGSOC), ovarian cancer and pancreatic ductal adenocarcinoma (PDAC).

L-783277 (Compound 4) is a MEK inhibitor (IC₅₀ = 4 nM). L-783277 has potent inhibitory activity against a variety of kinases, including VEGFR2/3, FLT1/3/4, MEK1/2, KDR, and PDGFRα, but has low selectivity for the kinase community. L-783277 inhibits viability (IC₅₀ = 22 mM) and cell proliferation (IC₅₀ = 21 mM) of H295R cells. L-783277 could be used in research on cancers such as adrenocortical carcinoma.

Lidocaine-d₆ (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor.

Envometinib (Compound B) is a dual-MEK inhibitor that works through Deep Cyclic Inhibition (DCI). Envometinib has antitumor activity in various in vivo models. Envometinib can be studied in RAS and RAF mutated cancer such as colorectal cancer and melanoma.

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

(E/Z)-BIX02188 is a MEK5/ERK5 pathway inhibitor. (E/Z)-BIX02188 inhibits the catalytic function of purified MEK5 enzyme.(E/Z)-BIX02188 can be used for the role of MEK5/ERK5 pathway in various biological systems .

MEK-IN-8 (Compound 30) is a MEK inhibitor (IC₅₀: < 5 nM for pMEK in A549 cells). MEK-IN-8 can be used in tumor research.

MAP2K1 Human Pre-designed siRNA Set A contains three designed siRNAs for MAP2K1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

MEK4 inhibitor-2 is a novel MEK4 inhibitor against pancreatic adenocarcinoma with an IC₅₀ value of 83 nM.

Trametinib-¹³C₆ is the ¹³C-labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC₅₀s of about 2 nM. Trametinib activates autophagy and induces apoptosis.

Polygalasaponin F (Standard) is the analytical standard of Polygalasaponin F. This product is intended for research and analytical applications. Polygalasaponin F is an orally active triterpenoid saponin monomer. Polygalasaponin F downregulates the expression of Bax, p53, caspase-3, NF-κB p65 and MEK1; restores and upregulates the expression of Bcl-2; activates the PI3K/Akt signaling pathway; inhibits the phosphorylation of p38 MAPK, nuclear translocation of NF-κB, TLR4-mediated signaling pathway, mitophagy (Mitophagy) and ROS production; enhances cell viability and suppresses apoptosis (Apoptosis). Polygalasaponin F maintains mitochondrial function, alleviates Ca²⁺ overload, upregulates pCREB and BDNF, preserves cell viability and inhibits the release of inflammatory cytokines. Polygalasaponin F alleviates lung injury induced by influenza A H1N1 and cerebral ischemia-reperfusion injury. Polygalasaponin F is applicable to researches related to Parkinson's disease, cerebral ischemia, pneumonia induced by influenza A H1N1, stroke and Alzheimer's disease.

MEK1/C-Raf-IN-1 (Compound 14d) is a MEK1/C-Raf inhibitor with IC₅₀ values of 97 and 23 nM, respectively. MEK1/C-Raf-IN-1 has antitumor activity.

CML-IN-1 (compound 7) is a potent anticancer agent. CML-IN-1 displays very good induced-apoptosis effect for human chronic myeloid leukemia (CML) cell line K562. CML-IN-1 exerts its effect via a significantly reduced protein phosphorylation of PI3K/Akt signal pathway. CML-IN-1 (compound 4) also inhibits cell proliferation by suppressing the MEK/ERK signaling pathway in colorectal cancer.

LLS30 is an anticancer agent. LLS30 suppresses MEK/ERK pathway. LLS30 has anti-cancer effects against ovarian cancer, prostate cancer, and malignant peripheral nerve sheath tumors. LLS30 shows synergistic anti-cancer effect with Enzalutamide (HY-70002) or Docetaxel (HY-B0011).

Cucurbitacin IIa (Hemslecin A) (Standard) is the analytical standard for Cucurbitacin IIa (HY-N1988). This product is used for research and analytical applications. Cucurbitacin IIa is an orally active, blood-brain barrier-penetrating EGFR inhibitor with an IC₅₀ of 1.455 nM for human EGFR. Cucurbitacin IIa induces caspase-3 dependent cell apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton through actin aggregation, blocks the cell cycle at the G2/M phase, and inhibits the EGFR-MAPK signaling pathway to exert anti-inflammatory activity. Cucurbitacin IIa can be used in research on inflammatory-related diseases, depression, and non-small cell lung cancer and other cancers.

Sophocarpine (Standard) is the analytical standard of Sophocarpine (HY-N0103). This product is intended for research and analytical applications. Sophocarpine is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage.

Pimasertib hydrochloride is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor.