AMPK (AMP-activated Protein Kinase)

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

click to view more

Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Catalog No. Information Product Use Citations Product Validations
S7306

Dorsomorphin 2HCl

Dorsomorphin 2HCl is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type Ⅰ BMP receptor activity.

S7317

WZ4003

WZ4003 is a highly specific NUAK kinase inhibitor with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2 in cell-base assays, respectively, without significant inhibition on 139 other kinases.

S7318

HTH-01-015

HTH-01-015 is a potent and selective NUAK1 inhibitor with IC50 of 100 nM, >100-fold selectivity over NUAK2.

S7840

Dorsomorphin

Dorsomorphin is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type I BMP receptor activity.

S2697

A-769662

A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM in cell-free assays, little effect on GPPase/FBPase activity.

S1802

AICAR (Acadesine)

AICAR (Acadesine) results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. Phase 3.

S2542

Phenformin HCl

Phenformin HCl is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class.

S7898

GSK621

GSK621 is a specific and potent AMPK activator.

Catalog No. Information Product Use Citations Product Validations
S7306

Dorsomorphin 2HCl

Dorsomorphin 2HCl is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type Ⅰ BMP receptor activity.

S7317

WZ4003

WZ4003 is a highly specific NUAK kinase inhibitor with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2 in cell-base assays, respectively, without significant inhibition on 139 other kinases.

S7318

HTH-01-015

HTH-01-015 is a potent and selective NUAK1 inhibitor with IC50 of 100 nM, >100-fold selectivity over NUAK2.

S7840

Dorsomorphin

Dorsomorphin is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type I BMP receptor activity.

Catalog No. Information Product Use Citations Product Validations
S2697

A-769662

A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM in cell-free assays, little effect on GPPase/FBPase activity.

2016, 12(2):432-8

2014, 74(1):298-308

2014, 55(7):1254-1266

S1802

AICAR (Acadesine)

AICAR (Acadesine) results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. Phase 3.

2015, 10.1111/bph.13120

2014, 111(8):1562-71

S2542

Phenformin HCl

Phenformin HCl is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class.

S7898

GSK621

GSK621 is a specific and potent AMPK activator.

2016, 11(8):e0161017

Tags: AMPK inhibition | AMPK activation | AMPK phosphorylation | AMPK activity | AMP-activated protein kinase pathway | AMPK activity assay | AMPK activators review | AMPK activity assay | AMPK inhibitor cancer | AMPK agonists | AMPK antagonist | AMPK inhibitor review