ERK5-IN-4

Cat. No.: HY-150606: FAQs
Data Sheet Handling Instructions Technical Support

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

CAS No. : 1888305-17-6

Size		Stock
MOQ		Minimum order quantity
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All ERK Isoform Specific Products:

View All Isoforms

ERK ERK1 ERK2 ERK5 ERK8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

ERK5

Cellular Effect

Cell Line	Type	Value	Description	References
A498	GI₅₀	22.3 nM Compound: 34b	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	[PMID: 35468293]
HEK293	GI₅₀	19.6 μM Compound: 34b	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	[PMID: 35468293]
MDA-MB-231	GI₅₀	26.6 nM Compound: 34b	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	[PMID: 35468293]
SJSA-1	GI₅₀	25 nM Compound: 34b	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	[PMID: 35468293]

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 K_d 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.

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].

MedChemExpress (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)	V_d (L/kg)	t_1/2 (min)	BA (%)
i.v. or p.o.	10	14	0.6	80	42

Molecular Weight

381.19

Formula

C₁₆H₁₁Cl₂FN₄O₂

CAS No.

1888305-17-6

SMILES

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

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]. Miller DC, et al. Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor. J Med Chem. 2022 May 12. 65(9):6513-6540. [Content Brief]

ERK5-IN-4 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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.

Keywords:

ERK5-IN-41888305-17-6ERKExtracellular signal regulated kinasesHEK293HeLaextracellular signal-relatedkinaseERK5 ΔTADpharmacokineticInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #