ERK5-IN-4
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.
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- CAS No.: 1888305-17-6
- Formula: C16H11Cl2FN4O2
- Molecular Weight:381.19
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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ERK5 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A498 | GI50 |
22.3 nM
Compound: 34b
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Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
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[PMID: 35468293] |
| HEK293 | GI50 |
19.6 μM
Compound: 34b
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Antiproliferative activity against HEK293 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
Antiproliferative activity against HEK293 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
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[PMID: 35468293] |
| MDA-MB-231 | GI50 |
26.6 nM
Compound: 34b
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Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
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[PMID: 35468293] |
| SJSA-1 | GI50 |
25 nM
Compound: 34b
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Antiproliferative activity against human SJSA-1 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
Antiproliferative activity against human SJSA-1 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
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[PMID: 35468293] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:0.01, 0.03, 0.1, 0.3, 1, 3 μM
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Incubation Time:1 h
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Result:Resulted upper phospho-ERK5 band with EGF stimulation and inhibition.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Pharmacokinetic Parameters for ERK5-IN-4[1]
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Dosage:
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Administration:
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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
Chemical Information
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CAS No. 1888305-17-6
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Molecular Weight 381.19
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Formula C16H11Cl2FN4O2
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SMILES
O=C(C1=CC(C(C2=C(Cl)C=CC(Cl)=C2F)=O)=CN1)NC3=CN(C)N=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ERK5-IN-4 Related Classifications
HY-150606 Related Classifications
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