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E6201

MCE China：E6201

Brand：MedChemExpress (MCE)

Cat. No.HY-15496

CAS：603987-35-5

Synonyms：ER-806201

Storage：Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping：Room temperature in continental US; may vary elsewhere.

Description：E6201 (ER-806201) is an ATP-competitive dual kinase inhibitor of MEK1 and FLT3. E6201 inhibits MEK1- induced ERK2 phosphorylation with an IC50 value of 5.2 nM, MKK4-induced JNK phosphorylation with an IC50 value of 91 nM, and MKK6-induced p38 MAPK phosphorylation with an IC50 value of 19 nM. Anti-tumor and anti-psoriasis efficacy.

In Vitro：E6201 is an inhibitor of MEKK1 and MEK families but not the MAPK family. E6201 inhibits MEKK1- induced phosphorylation of MEK1, MKK4, and MKK6 with IC50 values of 31, 522, and 65 nM, respectively. E6201 has no effect on other MAPK family enzymes such as ERK2, JNKs, and p38 MAPK at 10 μM[1]. E6201 inhibits LPS-induced TNF transcription with an IC50 value of 50±14 nM, but does not suppress β-actin transcription at 3 μM and only slightly at 10 μM[1]. E6201 inhibits the receptor tyrosine kinases VEGFR2, PDGFR, hepatocyte growth factor receptor, and EGFR with IC50 values of 350, 860, 1100, and 5400 nM, respectively, as well as the nonreceptor tyrosine kinase Syk with an IC50 value of 460 nM. E6201 does not inhibit ZAP-70 or IKK at 10 μM or PKC activity at 100 μM[1]. E6201 inhibits IL-2 production 48 h after stimulation with the T-cell mitogen PHA-P, with an IC50 value of 18 nM[1]. E6201 inhibits the proliferation of EGF-stimulated human keratinocytes with an IC50 value of 160 nM[1]. E6201 suppresses IL-8 production in human keratinocytes 24 h after stimulation with IL-1α or TNFα, with IC50 values of 60 and 30 nM, respectively[1]. E6201 inhibits TNFα, IL-1, IL-6, and IL-8 production from human PBMCs with IC50 values of 20, 16, 52, and 53 nM, respectively[1]. E6201 (0.08-20.0 μM) significantly inhibited triple-negative breast cancer (TNBC) cell proliferation and anchorage-independent colony formation in a dose-dependent manner[2]. E6201 (1 μM) inhibits expression of phospho-ERK and induces G1 phase cell cycle arrest, and apoptosis in TNBC[2].

In Vivo：E6201 (30 mg/kg; administered via tail vein injection three times per week) inhibits TNBC xenograft tumor growth. E6201 strongly inhibits pERK and Ki-67 expression in xenograft tumor tissues[2].

IC50 & Target：MEK1 5.2 nM (IC50)

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References：

[1]. Masaki Goto, et al. E6201 [(3S,4R,5Z,8S,9S,11E)-14-(ethylamino)-8, 9,16-trihydroxy-3,4-dimethyl-3,4,9,19-tetrahydro-1H-2-benzoxacyclotetradecine-1,7(8H)-dione], a novel kinase inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK)-1 and MEK kinase-1: in vitro characterization of its anti-inflammatory and antihyperproliferative activities. J Pharmacol Exp Ther. 2009 Nov;331(2):485-95.  [Content Brief]

[2]. Jangsoon Lee, et al. Anti-tumor and anti-metastasis efficacy of E6201, a MEK1 inhibitor, in preclinical models of triple-negative breast cancer. Breast Cancer Res Treat. 2019 Jun;175(2):339-351.  [Content Brief]