MEK Inhibitor

CI-1040 (Standard) is the analytical standard of CI-1040. This product is intended for research and analytical applications. CI-1040 (PD 184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.

PD-334581 (Standard) is the analytical standard of PD-334581 (HY-107619). This product is intended for research and analytical applications. PD-334581 is a MEK1 inhibitor.

RO4987655 (Standard) is the analytical standard of RO4987655. This product is intended for research and analytical applications. RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM for inhibition of MEK1/MEK2.

Mirdametinib (Standard) is the analytical standard of Mirdametinib (HY-10254). This product is intended for research and analytical applications. Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC₅₀ of 0.33 nM. Mirdametinib exhibits a Kiapp of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts.

JTP-70902, a p15^INK4b-inductive compound, is a MEK1/2 inhibitor. JTP-70902 exhibits potent antitumor effect.

Sorafenib (tosylate) (Standard) (Bay 43-9006 (tosylate) (Standard)) is the analytical standard of Sorafenib (tosylate) (HY-10201A). This product is intended for research and analytical applications. 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.

U0126 (Standard) is the analytical standard of U0126 (HY-12031A). This product is intended for research and analytical applications. U0126 is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC₅₀s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor.

CInQ-03 is an allosteric inhibitor of MEK1/2, with IC₅₀ values of 5 μM and 10 μM against MEK1 and MEK2, respectively. CInQ-03 inhibits the kinase activity of MEK1/2 and reduces the phosphorylation levels of downstream ERK1/2 and RSK. CInQ-03 suppresses both anchorage-dependent and anchorage-independent growth of colon cancer cells, the activity of AP-1 reporter gene in colon cancer cells, as well as EGF-induced growth, transformation and AP-1 reporter gene activity in HaCaT keratinocytes. CInQ-03 can be used in studies related to colon cancer.

Lidocaine-d₆ (Lignocaine-d₆) is deuterium labeled Lidocaine. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence. Lidocaine 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 is an amide derivative and has potential for the research of ventricular arrhythmia.

R-IMPP hydrochloride (PF-00932239 hydrochloride) is a PCSK9 translation inhibitor and a selective 80S ribosome binder. R-IMPP hydrochloride inhibits the KRAS/MEK/ERK signaling cascade. R-IMPP hydrochloride reduces LPS-induced nuclear translocation of NFkB P65. R-IMPP hydrochloride increases LDL-R levels in cells, promotes LDL-C uptake, and does not alter the secretion of transferrin or albumin. R-IMPP hydrochloride inhibits the growth of colorectal cancer (CRC) cells, organoids and xenografts carrying APC/KRAS mutations, as well as the number and burden of spontaneous mouse tumors. R-IMPP hydrochloride can be used in research related to colorectal cancer with APC/KRAS mutations, hepatic ischemia-reperfusion injury and hypercholesterolemia.

Aspartyl-alanyl-diketopiperazine (DA-DKP) (Standard) is the analytical standard of Aspartyl-alanyl-diketopiperazine (HY-107091). This product is intended for research and analytical applications. Aspartyl-alanyl-diketopiperazine is an immunomodulatory molecule and anti-inflammatory agent. Aspartyl-alanyl-diketopiperazine increases the level of active Rap1 in activated human T lymphocytes and reduces the phosphorylation levels of Ras, ATF-2, c-jun, MEK1, MEKK1, ERK1, JNK1,2,3, p38MAPK and MEF-2. Aspartyl-alanyl-diketopiperazine inhibits the production of pro-inflammatory cytokines, including the levels of IFN-γ and TNF-α. Aspartyl-alanyl-diketopiperazine can be used in studies of inflammatory immune responses.

DZ2002 (Standard) is the analytical standard of DZ2002. This product is intended for research and analytical applications. DZ2002 is an orally active, reversible and low-cytotoxic type III SAHH inhibitor (Ki=17.9 nM), with good immunosuppressive activity. DZ2002 prevents the development of experimental dermal fibrosis by reversing the profibrotic phenotype of various cell types. DZ2002 can be used in studies of autoimmune diseases such as lupus syndrome and systemic sclerosis.

Refametinib (Standard) is the analytical standard of Refametinib. This product is intended for research and analytical applications. Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.

PD 198306 (Standard) is the analytical standard of PD 198306 (HY-107620). This product is intended for research and analytical applications. PD 198306 is a selective MAPK/ERK-K_inase (MEK) inhibitor. PD 198306 results in an observable reduction in the Streptozocin induced increase in the level of active ERK1 and 2. Antihyperalgesic effects.

Trilinolein (Standard) is the analytical standard of Trilinolein (HY-128393). This product is intended for research and analytical applications. Trilinolein is an orally active triglyceride that inhibits the PI3K/Akt, Ras/MEK/ERK signaling pathways, and MMP-2. Trilinolein can reduce oxidative stress, induce apoptosis, and inhibit cell migration. Trilinolein can be used in the research fields of cardiovascular disease, cerebrovascular disease (such as cerebral ischemia), and non-small cell lung cancer.

Cobimetinib (racemate) (Standard) is the analytical standard of Cobimetinib (racemate). This product is intended for research and analytical applications. Cobimetinib racemate (GDC-0973 racemate; XL518 racemate) is the racemate of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.

G-479 is the inhibitor for MEK and hERG channel (IC₅₀=14 μM). G-479 inhibits the proliferation of HCT-116 and A375 with IC₅₀ of 0.049 μM and 0.004 μM. G-479 exhibits good metabolic stability in liver microsomes and good pharmacokinetic characteristics in rats.

Binimetinib (Standard) is the analytical standard of Binimetinib. This product is intended for research and analytical applications. Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC₅₀ of 12 nM.

U0126-EtOH (Standard) is the analytical standard of U0126-EtOH (HY-12031). This product is intended for research and analytical applications. U0126 (U0126-EtOH) is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC₅₀s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor.

Luvometinib-d (FCN-159-d) is the deuterated-labeled Luvometinib (HY-159846). Luvometinib is an orally potent MEK1/2 inhibitor. Luvometinib selectively blocks the MAPK signaling pathway by forming a ternary complex with MEKase and ATP, thereby reducing the phosphorylation level of ERK. Luvometinib induces cell cycle arrest and apoptosis, and inhibits cancer cell proliferation. Luvometinib can be used in relevant research on various solid tumors including melanoma, non-small cell lung cancer, colon cancer, and acute myeloid leukemia.