E6201(Synonyms: ER-806201)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

E6201 (Synonyms: ER-806201)

E6201 (ER-806201) 是一种 ATP 竞争性的 MEK1 和 FLT3 双重激酶抑制剂。E6201 抑制 MEK1 诱导的 ERK2 磷酸化，IC50 值为 5.2 nM，MKK4 诱导的 JNK 磷酸化，IC50 值为 91 nM，以及 MKK6 诱导的 p38 MAPK 磷酸化，IC50 值为 19 nM。具有抗肿瘤和抗银屑病功效。

E6201(Synonyms: ER-806201)

E6201 Chemical Structure

CAS No. : 603987-35-5

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生物活性

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[1][2].

IC50 & Target

MEK1

5.2 nM (IC50)

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: Human TNBC cell lines BT20, HCC70, MDA-MB-231, HCC1806, HCC1937, SUM149 and SUM159
Concentration: 0.00, 0.08, 0.16, 0.31, 0.63, 1.25, 2.50, 5.00, 10.0, 20.0 μM
Incubation Time: 5 days
Result: Inhibited TNBC cell proliferation and anchorage-independent colony formation in a dose-dependent manner.

Western Blot Analysis[3]

Cell Line: Human TNBC cell lines BT20, HCC70, MDA-MB-231, HCC1806, HCC1937, SUM149 and SUM159
Concentration: 1 μM
Incubation Time: 0, 1, 24 hours
Result: pERK expression level showed a rapid (apparent by 1 hour) and sustained (still apparent at 24 hours) decrease in the tested TNBC cell lines following treatment.

体内研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Nod.Scid gamma mice (age 4 to 6 weeks old) bearing MDA-MB-231-LM2 xenograft tumors[2]
Dosage: 30 mg/kg
Administration: Administered via tail vein injection three times per week for 17 days
Result: Compared with mice treated with vehicle control, the E6201-treated mice showed 60% tumor growth suppression.

分子量

389.44

Formula

C21H27NO6
CAS 号

603987-35-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

    [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.

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