MEK Inhibitor

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.

Sorafenib-d₃ (Donafenib) tosylate is the deuterated-labeled Sorafenib tosylate (HY-10201A). Sorafenib (Bay 43-9006) tosylate is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib tosylate induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib tosylate inhibits tumor growth and metastasis in mouse and rat models. Sorafenib tosylate can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.

(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-7 (compound WX086) is potent, orally active and selective MEK inhibitor (MEK1 IC₅₀ = 29.62 nM). MEK-IN-7 inhibits HT29 and A375 cell proliferation with IC₅₀s of 0.62 and 0.40 nM. MEK-IN-7 inhibits tumor growth in a HL-29 xenograft mouse model. MEK-IN-7 can be used for melanoma and colon cancer research.

GW284543 (UNC10225170) hydrochloride is a selective MEK5 inhibitor. GW284543 reduces pERK5, and decreases endogenous MYC protein.

RO5068760 is a potent, orally active and selective non-ATP-competitive MEK1/2 inhibitor with an IC₅₀ of 0.025 μM for MEK1. RO5068760 significantly inhibits MAPK pathway activity, thereby inducing G1 cell cycle arrest and apoptosis to inhibit cancer cell growth. RO5068760 exhibits significant efficacy in a broad spectrum of tumors with aberrant MAPK pathway activation. RO5068760 can be used for melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), and pancreatic cancer research.

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.

PHI-501 is a dual inhibitor targeting RAF/DDR. PHI-501 exhibits significant anti-proliferative effects in melanoma cell lines and significantly inhibits the colony formation of drug-resistant cells. PHI-501 strongly inhibits ERK and AKT phosphorylation. PHI-501 downregulates the gene sets in drug-resistant cells of TNFA-NFKB, IL6-JAK-STAT3, and KRAS signaling pathways as well as the epithelial-mesenchymal transition (EMT) signaling pathways. PHI-501 demonstrates significant anti-tumor effects in the SK-MEL3DR xenograft model. PHI-501 can be used for research on the problem of drug resistance in melanoma.

AKT1-IN-13 is an orally active AKT1 inhibitor with an IC₅₀ of 5.17 μM. AKT1-IN-13 also exhibits high inhibitory activity against PAK1, PKA, MAP2K1 (MEK1 / MAPKK1) and MAPK1 (ERK2). AKT1-IN-13 induces cell apoptosis, activates the pro-apoptotic protein BAX, inhibits the anti-apoptotic protein Bcl-2, and activates caspase 3 simultaneously. As a cytotoxic agent, AKT1-IN-13 exerts a killing effect on orthotopically transplanted liver cancer in an AKT1-dependent manner. AKT1-IN-13 can be used in studies related to hepatocellular carcinoma.

PROTAC SOS1 degrader-6 is a selective SOS1 PROTAC degrader with a DC₅₀ of 43-130 nM. PROTAC SOS1 degrader-6 induces ubiquitination and degradation of SOS1 via the ubiquitin-proteasome system by recruiting the E3 ligase VHL. PROTAC SOS1 degrader-6 reduces the levels of phosphorylated MEK and ERK. PROTAC SOS1 degrader-6 exerts antiproliferative effects in KRAS-driven cancer cells. PROTAC SOS1 degrader-6 can be used in research related to KRAS^G12C-mutant cancers and chronic myeloid leukemia.

MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC₅₀ values of 28 nM for MEK1, and 3 nM each for BRAF and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer.

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.

MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC₅₀ values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines.

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.

KZ-02 is an orally active dual MEK1/Pim-1 kinase inhibitor, with an IC₅₀ of 1.07 nM against MEK1 and an IC₅₀ of 1.34 μM against Pim-1. KZ-02 reduces the phosphorylation levels of ERK and Cdc25C, and promotes the proteasomal degradation of Pim-1 protein. KZ-02 inhibits cancer cell growth and exerts anti-tumor effects. KZ-02 can be used in the research of colorectal cancer.