AMPK activator 8

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AMPK activator 8 (compound 2) is an AMP-activated protein kinase (AMPK) activator with EC₅₀s of 11, 27, 4, 2, and 4 nM for rAMPK α1β1γ1, rAMPK α2β1γ1, rAMPK α1β2γ1, rAMPK α2β2γ1, rAMPK α2β2γ3, respectively. AMPK activator 8 can be used for the research of type 2 diabetes.

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

AMPK activator 8 Chemical Structure

CAS No. : 1852451-96-7

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NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

AMPK α1β1γ1

11 nM (EC₅₀)

AMPK α2β1γ1

27 nM (EC₅₀)

AMPK α1β2γ1

4 nM (EC₅₀)

AMPK α2β2γ1

2 nM (EC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
COS-7	EC₅₀	11 nM Compound: 28	Activation of human recombinant AMPK alpha1/beta1/gamma1 expressed in African green monkey COS7 cells assessed as increase in biotinylated AAC (1 to 120 residues) peptide phosphorylation at Ser-79 residue measured after 60 mins by Alphascreen assay Activation of human recombinant AMPK alpha1/beta1/gamma1 expressed in African green monkey COS7 cells assessed as increase in biotinylated AAC (1 to 120 residues) peptide phosphorylation at Ser-79 residue measured after 60 mins by Alphascreen assay	[PMID: 27727125]
COS-7	EC₅₀	2 nM Compound: 28	Activation of human recombinant AMPK alpha2/beta2/gamma1 expressed in African green monkey COS7 cells assessed as increase in biotinylated AAC (1 to 120 residues) peptide phosphorylation at Ser-79 residue measured after 60 mins by Alphascreen assay Activation of human recombinant AMPK alpha2/beta2/gamma1 expressed in African green monkey COS7 cells assessed as increase in biotinylated AAC (1 to 120 residues) peptide phosphorylation at Ser-79 residue measured after 60 mins by Alphascreen assay	[PMID: 27727125]
COS-7	EC₅₀	27 nM Compound: 28	Activation of human recombinant AMPK alpha2/beta1/gamma1 expressed in African green monkey COS7 cells assessed as increase in biotinylated AAC (1 to 120 residues) peptide phosphorylation at Ser-79 residue measured after 60 mins by Alphascreen assay Activation of human recombinant AMPK alpha2/beta1/gamma1 expressed in African green monkey COS7 cells assessed as increase in biotinylated AAC (1 to 120 residues) peptide phosphorylation at Ser-79 residue measured after 60 mins by Alphascreen assay	[PMID: 27727125]
COS-7	EC₅₀	4 nM Compound: 28	Activation of human recombinant AMPK alpha1/beta2/gamma1 expressed in African green monkey COS7 cells assessed as increase in biotinylated AAC (1 to 120 residues) peptide phosphorylation at Ser-79 residue measured after 60 mins by Alphascreen assay Activation of human recombinant AMPK alpha1/beta2/gamma1 expressed in African green monkey COS7 cells assessed as increase in biotinylated AAC (1 to 120 residues) peptide phosphorylation at Ser-79 residue measured after 60 mins by Alphascreen assay	[PMID: 27727125]
COS-7	EC₅₀	4 nM Compound: 28	Activation of human recombinant AMPK alpha2/beta2/gamma3 expressed in African green monkey COS7 cells assessed as increase in biotinylated AAC (1 to 120 residues) peptide phosphorylation at Ser-79 residue measured after 60 mins by Alphascreen assay Activation of human recombinant AMPK alpha2/beta2/gamma3 expressed in African green monkey COS7 cells assessed as increase in biotinylated AAC (1 to 120 residues) peptide phosphorylation at Ser-79 residue measured after 60 mins by Alphascreen assay	[PMID: 27727125]

In Vitro

AMPK activator 8 (compound 2) acts on rAMPK α1β1γ1, rAMPK α2β1γ1, rAMPK α1β1γ1, rAMPK α1β2γ1, rAMPK α2β2γ and rAMPK α2β2γ3 with the EC₅₀ value of 11 nM, 27 nM, 4 nM, 2 nM and 4 nM, respectively^[1].
AMPK activator 8 (compound 2) affects cell viability^[1].

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

Cell Viability Assay^[1]

Cell Line:	HepG2, C2C12 myoblasts
Concentration:	0.01-1000 μM
Incubation Time:	1 hour
Result:	Resulted in HepG2 and C2C12 myoblasts with the EC₅₀ value of 255 nM and 230 nM, respectively.

Molecular Weight

480.90

Formula

C₂₅H₂₁ClN₂O₆

CAS No.

1852451-96-7

SMILES

ClC1=C(C2=CC=C(C3=C(C=CC=C3O)O)C=C2)C=C4NC(O[C@H]5[C@]6([H])[C@]([C@@H](CO6)O)([H])OC5)=NC4=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]. Mathilde Muzerelle, et al. Novel activators of amp-activated protein kinases.WO2016001224A1

AMPK activator 8 Related Classifications

Metabolic Disease

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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.

Keywords:

AMPK activator 81852451-96-7AMPK activator8AMPK activator-8AMPKAMP-activated protein kinaseAMPK?activatortype 2 diabetesInhibitorinhibitorinhibit

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