1. MAPK/ERK Pathway
    Stem Cell/Wnt
  2. ERK
  3. ERK5-IN-4

ERK5-IN-4 

Cat. No.: HY-150606
Handling Instructions

ERK5-IN-4 (compound 34b) is a potent and selective inhibitor of extracellular signal-related kinase 5 (ERK5). ERK5-IN-4 inhibits ERK5 (full-length) and truncated ERK5 (ERK5 ΔTAD) kinase activity in HEK293 cells with an IC50 of 77 nM and 300 nM, respectively.

For research use only. We do not sell to patients.

ERK5-IN-4 Chemical Structure

ERK5-IN-4 Chemical Structure

CAS No. : 1888305-17-6

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Description

ERK5-IN-4 (compound 34b) is a potent and selective inhibitor of extracellular signal-related kinase 5 (ERK5). ERK5-IN-4 inhibits ERK5 (full-length) and truncated ERK5 (ERK5 ΔTAD) kinase activity in HEK293 cells with an IC50 of 77 nM and 300 nM, respectively[1].

IC50 & Target

ERK5

 

In Vitro

ERK5-IN-4 (compound 34b) is selective against MAP3K, p38 (IC50>30 μM) and BRD4 (IC50>20 μM), in contrast to many reported ERK5 inhibitors[1].
ERK5-IN-4 (0-100 μM; 72 h) suppresses ERK5 kinase activity in HEK293 cells and (0-1 μM; 72 h) induces paradoxical activation of ERK5 transcriptional activity, thus resulting in C-terminal transcriptional activation domain (TAD) separated from the nuclear localization sequence (NLS) and results ERK5 nuclear translocation[1].
ERK5-IN-4 inhibits cancer cells with GI50 of 19.6 μM (HEK293), 22.3 μM (A498), 25 μM (SJSA-1), 26.6 μM (MDA-MB-231) following a 72 h incubation[1].
ERK5-IN-4 exhibits kinome selectivity Kd of 1.2 μM, 0.29 μM, 0.046 μM, 0.061 μM, 0.18 μM, 0.38 μM, 1.3 μM, 0.42 μM, 0.22 μM, 2.8 μM against ABL1-nonphosphorylated, AURKA, CSF1R, DCAMKL1 (DCLK1), ERK5 (MAPK7), FGFR1, JAK3 (JH1domain-catalytic), KIT, LRRK2, MEK5 (MAP2K5)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3 μM
Incubation Time: 1 h
Result: Resulted upper phospho-ERK5 band with EGF stimulation and inhibition.
In Vivo

ERK5-IN-4 (compound 34b) (p.o.; 10 mg/kg) has low clearance and an oral bioavailability of 42% in the mouse[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Pharmacokinetic Parameters for ERK5-IN-4[1]
Dosage:
Administration:
Result:
Route Dose (mg/kg) Cl (mL/min/kg) Vd (L/kg) t1/2 (min) BA (%)
i.v. or p.o. 10 14 0.6 80 42
Molecular Weight

381.19

Formula

C16H11Cl2FN4O2

CAS No.
SMILES

O=C(C1=CC(C(C2=C(Cl)C=CC(Cl)=C2F)=O)=CN1)NC3=CN(C)N=C3

Shipping

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Storage

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

References
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ERK5-IN-4
Cat. No.:
HY-150606
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