E6201 (Synonyms: ER-806201)

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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.

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E6201 Chemical Structure

CAS No. : 603987-35-5

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MEK1 MEK2 MEK5 MEK

Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

MEK1

5.2 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	26 nM Compound: 19; E6201	Antiproliferative activity against human BaF3 cells harboring D835Y mutant assessed as cell growth inhibition by trypan blue staining based assay Antiproliferative activity against human BaF3 cells harboring D835Y mutant assessed as cell growth inhibition by trypan blue staining based assay	[PMID: 35849914]
BaF3	IC₅₀	4.6 nM Compound: 19; E6201	Antiproliferative activity against human BaF3 cells harboring D835G mutant assessed as cell growth inhibition by trypan blue staining based assay Antiproliferative activity against human BaF3 cells harboring D835G mutant assessed as cell growth inhibition by trypan blue staining based assay	[PMID: 35849914]
BT-20	IC₅₀	10.14 μM Compound: 6; E6201	Anticancer activity against human BT-20 cells assessed as cell growth inhibition incubated for 5 days by sulforhodamine B staining based assay Anticancer activity against human BT-20 cells assessed as cell growth inhibition incubated for 5 days by sulforhodamine B staining based assay	[PMID: 33650861]
HCC1806	IC₅₀	2.5 μM Compound: 6; E6201	Anticancer activity against human HCC1806 cells assessed as cell growth inhibition incubated for 5 days by sulforhodamine B staining based assay Anticancer activity against human HCC1806 cells assessed as cell growth inhibition incubated for 5 days by sulforhodamine B staining based assay	[PMID: 33650861]
HCC1937	IC₅₀	3.73 μM Compound: 6; E6201	Anticancer activity against human HCC1937 cells assessed as cell growth inhibition incubated for 5 days by sulforhodamine B staining based assay Anticancer activity against human HCC1937 cells assessed as cell growth inhibition incubated for 5 days by sulforhodamine B staining based assay	[PMID: 33650861]
HCC70	IC₅₀	8.79 μM Compound: 6; E6201	Anticancer activity against human HCC70 cells assessed as cell growth inhibition incubated for 5 days by sulforhodamine B staining based assay Anticancer activity against human HCC70 cells assessed as cell growth inhibition incubated for 5 days by sulforhodamine B staining based assay	[PMID: 33650861]
MDA-MB-231	IC₅₀	0.25 μM Compound: 6; E6201	Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 5 days by sulforhodamine B staining based assay Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 5 days by sulforhodamine B staining based assay	[PMID: 33650861]
MOLM-13	IC₅₀	5 nM Compound: 19; E6201	Antiproliferative activity against human MOLM13 cells harboring FLT3-ITD mutant assessed as cell growth inhibition by Trypan blue staining based assay Antiproliferative activity against human MOLM13 cells harboring FLT3-ITD mutant assessed as cell growth inhibition by Trypan blue staining based assay	[PMID: 35849914]
MV4-11	IC₅₀	2 nM Compound: 19; E6201	Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as cell growth inhibition by trypan blue staining based assay Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as cell growth inhibition by trypan blue staining based assay	[PMID: 35849914]
SUM149PT	IC₅₀	0.21 μM Compound: 6; E6201	Anticancer activity against human SUM149 cells assessed as cell growth inhibition incubated for 5 days by sulforhodamine B staining based assay Anticancer activity against human SUM149 cells assessed as cell growth inhibition incubated for 5 days by sulforhodamine B staining based assay	[PMID: 33650861]
SUM-159-PT	IC₅₀	2.36 μM Compound: 6; E6201	Anticancer activity against human SUM159 cells assessed as cell growth inhibition incubated for 5 days by sulforhodamine B staining based assay Anticancer activity against human SUM159 cells assessed as cell growth inhibition incubated for 5 days by sulforhodamine B staining based assay	[PMID: 33650861]
THP-1	IC₅₀	56 nM Compound: 22, E6201	Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha production by PLAP reporter assay Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha production by PLAP reporter assay	[PMID: 20399648]

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].

MedChemExpress (MCE) 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.

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].

MedChemExpress (MCE) 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.

Clinical Trial

Molecular Weight

389.44

Formula

C₂₁H₂₇NO₆

CAS No.

603987-35-5

SMILES

OC1=C2C(/C=C/C[C@@H]([C@@H](C(/C=C\[C@H]([C@@H](OC2=O)C)C)=O)O)O)=CC(NCC)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

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]

E6201 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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