AMPK

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1208 Doxorubicin (Adriamycin) HCl 20 mg/mL 100 mg/mL <1 mg/mL
S1113 GSK690693 <1 mg/mL 39 mg/mL <1 mg/mL
S1321 Urolithin B <1 mg/mL 42 mg/mL 12 mg/mL
S3296 Hispidulin -1 mg/mL 100 mg/mL -1 mg/mL
S3299 Demethyleneberberine -1 mg/mL 3 mg/mL -1 mg/mL
S0177 XMD-17-51 2 mg/mL 81 mg/mL 10 mg/mL
S7306 Dorsomorphin (Compound C) 2HCl 94 mg/mL <1 mg/mL <1 mg/mL
S7317 WZ4003 <1 mg/mL 7 mg/mL <1 mg/mL
S7318 HTH-01-015 <1 mg/mL 58 mg/mL 30 mg/mL
S8274 STO-609 <1 mg/mL 8 mg/mL <1 mg/mL
S8161 ON123300 <1 mg/mL 29 mg/mL <1 mg/mL
S7840 Dorsomorphin (Compound C) <1 mg/mL 1 mg/mL '2 mg/mL
S1033 Nilotinib (AMN-107) <1 mg/mL 27 mg/mL <1 mg/mL
S2697 A-769662 <1 mg/mL 72 mg/mL <1 mg/mL
S1802 AICAR (Acadesine) <1 mg/mL 51 mg/mL <1 mg/mL
S1323 7-Methoxyisoflavone <1 mg/mL 30 mg/mL <1 mg/mL
S9604 IM156 <1 mg/mL 63 mg/mL 20 mg/mL
S8953 ASP4132 <1 mg/mL 100 mg/mL <1 mg/mL
S0795 O-304 <1 mg/mL 20 mg/mL <1 mg/mL
S0411 BAM 15 <1 mg/mL 68 mg/mL <1 mg/mL
S1396 Resveratrol <1 mg/mL 45 mg/mL <1 mg/mL
S2542 Phenformin HCl 48 mg/mL 48 mg/mL 12 mg/mL
S5284 Adenosine 5'-monophosphate monohydrate -1 mg/mL 9 mg/mL -1 mg/mL
S8335 PF-06409577 <1 mg/mL 68 mg/mL 68 mg/mL
S7898 GSK621 <1 mg/mL 97 mg/mL <1 mg/mL
S8654 ex229 (compound 991) <1 mg/mL 12 mg/mL <1 mg/mL
S8803 MK-3903 <1 mg/mL 91 mg/mL <1 mg/mL
S9096 ligustroflavone -1 mg/mL 100 mg/mL -1 mg/mL
S2942 EB-3D 25 mg/mL 50 mg/mL 15 mg/mL
S7953 ETC-1002 <1 mg/mL 68 mg/mL <1 mg/mL
S9116 Chikusetsusaponin IVa -1 mg/mL 100 mg/mL -1 mg/mL
S4561 Danthron <1 mg/mL 4 mg/mL <1 mg/mL
S6221 Methyl cinnamate -1 mg/mL 32 mg/mL -1 mg/mL

AMPK製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1208

Doxorubicin (Adriamycin) HCl

Doxorubicin (Adriamycin, NSC 123127, DOX) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage, mitophagy and apoptosis in tumor cells. Doxorubicin reduces basal phosphorylation of AMPK. Doxorubicin is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation.

S1113

GSK690693

GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.

S1321

Urolithin B

Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. Urolithin B suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.

S3296

Hispidulin

Hispidulin (Dinatin), an active natrual ingredient in a number of traditional Chinese medicinal herbs, exhibits inhibitory activity against the oncogenic protein kinase Pim-1 with IC50 of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Hispidulin exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway.

S3299

Demethyleneberberine

Demethyleneberberine (DMB), a component of Cortex Phellodendri Chinensis (CPC), significantly alleviates the weight loss and diminishes myeloperoxidase (MPO) activity, while significantly reduces the production of pro-inflammatory cytokines, such as interleukin (IL)-6 and tumor necrosis factor-α (TNF-α), and inhibits the activation of NF-κB signaling pathway. Demethyleneberberine (DMB) potentially ameliorates NAFLD (Non-alcoholic fatty liver disease) by activating AMPK pathways.

S0177

XMD-17-51

XMD-17-51 is a potent and highly selective inhibitor of NUAK1.

S7306

Dorsomorphin (Compound C) 2HCl

Dorsomorphin 2HCl (BML-275, Compound C) 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. Dorsomorphin induces autophagy in cancer cell line.

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.

S8274

STO-609

STO-609 is a specific inhibitor of the Ca2+/Calmodulin-dependent protein kinase kinase(CaM-KK) that inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with Ki values of 80 and 15 ng/ml, respectively, and also inhibits their autophosphorylation activities. STO-609 inhibits AMPKK activity and inhibits autophagy.

S8161

ON123300

ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET, and Fyn, respectively.

S7840

Dorsomorphin (Compound C)

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.

S1033

Nilotinib (AMN-107)

Nilotinib (AMN-107) is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.

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, NSC105823), an AMPK activator, results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. AICAR (Acadesine) induces mitophagy. Phase 3.

S1323

7-Methoxyisoflavone

7-Methoxyisoflavone (MIF) is a potent activator of adenosine monophosphate-activated protein kinase (AMPK).

S9604

IM156

IM156, a metformin derivative, is a potent activator of AMPK that increases AMPK phosphorylation. IM156 blocks oxidative phosphorylation (OXPHOS) through the inhibition of complex I and increases apoptosis. IM156 ameliorates various types of fibrosis and inhibits tumors.

S8953

ASP4132

ASP4132 is a potent and orally active activator of Adenosine Monophosphate-Activated Protein Kinase (AMPK) with EC50 of 0.018 μM. ASP4132 is used as a clinical candidate for the treatment of human cancer.

S0795

O-304

O-304 (O-304X) is an orally available pan-activator of AMPK activated protein kinase (AMPK). O-304 (O-304X) exhibits a great potential as a novel drug to treat type 2 diabetes (T2D) and associated cardiovascular complications.

S0411

BAM 15

BAM 15 is a novel mitochondrial protonophore uncoupler capable of protecting mammals from acute renal ischemic-reperfusion injury and cold-induced microtubule damage. BAM 15 is also a potent AMPK activator. BAM 15 attenuates transportation-induced apoptosis in iPS-differentiated retinal tissue.

S1396

Resveratrol

Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.

S2542

Phenformin HCl

Phenformin HCl is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class. It activates AMPK, increasing activity and phosphorylation.

S5284

Adenosine 5'-monophosphate monohydrate

Adenosine 5'-monophosphate monohydrate (5'-AMP) is an activator of a class of protein kinases known as AMP-activated protein kinase (AMPK).

S8335

PF-06409577

PF-06409577 is orally bioavailable AMPK activator with EC50 of 7 nM for α1β1γ1 in the TR-FRET assay and it shows no detectable inhibition of hERG in a patch-clamp assay (100 μM) and was not an inhibitor (IC50 > 100 μM) of the microsomal activities of major human cytochrome P450 isoforms.

S3832

Euphorbiasteroid

Euphorbiasteroid, a component of Euphorbia lathyris L., inhibits adipogenesis of 3T3-L1 cells through activation of the AMPK pathway and induces HL-60 cells to apoptosis via promoting Bcl-2/Bax apoptotic signaling pathway in a dose-dependent manner.

S7898

GSK621

GSK621 is a specific and potent AMPK activator.

S8654

ex229 (compound 991)

EX229 (compound 991) is a potent AMPK activator that is 5-10-fold more potent than A769662 in activating AMPK.

S8803

MK-3903

MK-3903 is a potent and selective AMPK activator with an EC50 of 8 nM for α1 β1 γ1 subunit. It activates 10 of the 12 pAMPK complexes with EC50 values in the range of 8-40 nM and maximal activation >50%.

S9096

ligustroflavone

Ligustroflavone, isolated from the leaves of Turpinia montana, shows high antioxidant capacity and is reported to be an AMPK activator.

S2942

EB-3D

EB-3D is a potent and selective inhibitor of choline kinase α (ChoKα) with IC50 of 1 μM for ChoKα1. EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells.

S7953

ETC-1002

ETC-1002,also known as Bempedoic acid, is an orally available, once-daily LDL-C lowering small molecule designed to lower elevated levels of LDL-C and to avoid side effects associated with existing LDL-C lowering therapies.ETC-1002 is an activator of hepatic AMP-activated protein kinase (AMPK). It has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).

S9116

Chikusetsusaponin IVa

Chikusetsusaponin IVa (Calenduloside F), a major active ingredient of triterpenoid saponins, has numerous pharmacological activities, including cytotoxic activity against various cancer cells, anti-inflammatory activity, prevention of dental caries and induction of genta-micin nephrotoxicity. Chikusetsusaponin IVa is a novel AMPK activator.

S4561

Danthron

Danthron (Chrysazin, Antrapurol) functions in regulating glucose and lipid metabolism by activating AMPK. Danthron is a natural product extracted from the traditional Chinese medicine rhubarb. Danthron used to be a laxativa and now is currently used as an antioxidant in synthetic lubricants, in the synthesis of experimental antitumor agents, as a fungicide and as an intermediate for making dyes.

S6221

Methyl cinnamate

Methyl cinnamate, an active component of Zanthoxylum armatum, is a widely used natural flavor compound with antimicrobial and tyrosinase inhibitor activities. Methyl Cinnamate Inhibits Adipocyte Differentiation via Activation of the CaMKK2--AMPK Pathway in 3T3-L1 Preadipocytes.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1208

Doxorubicin (Adriamycin) HCl

Doxorubicin (Adriamycin, NSC 123127, DOX) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage, mitophagy and apoptosis in tumor cells. Doxorubicin reduces basal phosphorylation of AMPK. Doxorubicin is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation.

S1113

GSK690693

GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.

S1321

Urolithin B

Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. Urolithin B suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.

S3296

Hispidulin

Hispidulin (Dinatin), an active natrual ingredient in a number of traditional Chinese medicinal herbs, exhibits inhibitory activity against the oncogenic protein kinase Pim-1 with IC50 of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Hispidulin exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway.

S3299

Demethyleneberberine

Demethyleneberberine (DMB), a component of Cortex Phellodendri Chinensis (CPC), significantly alleviates the weight loss and diminishes myeloperoxidase (MPO) activity, while significantly reduces the production of pro-inflammatory cytokines, such as interleukin (IL)-6 and tumor necrosis factor-α (TNF-α), and inhibits the activation of NF-κB signaling pathway. Demethyleneberberine (DMB) potentially ameliorates NAFLD (Non-alcoholic fatty liver disease) by activating AMPK pathways.

S0177

XMD-17-51

XMD-17-51 is a potent and highly selective inhibitor of NUAK1.

S7306

Dorsomorphin (Compound C) 2HCl

Dorsomorphin 2HCl (BML-275, Compound C) 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. Dorsomorphin induces autophagy in cancer cell line.

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.

S8274

STO-609

STO-609 is a specific inhibitor of the Ca2+/Calmodulin-dependent protein kinase kinase(CaM-KK) that inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with Ki values of 80 and 15 ng/ml, respectively, and also inhibits their autophosphorylation activities. STO-609 inhibits AMPKK activity and inhibits autophagy.

S8161

ON123300

ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET, and Fyn, respectively.

S7840

Dorsomorphin (Compound C)

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.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1033

Nilotinib (AMN-107)

Nilotinib (AMN-107) is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.

2020, 8 pii: blood

2020, 9 pii: S1097-2765(20)30189-1

2020, 6(40)eaba6584

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.

2020, 34(3):4702-4717

2020, 10.1194/jlr.RA119000542

2020, 10:956

S1802

AICAR (Acadesine)

AICAR (Acadesine, NSC105823), an AMPK activator, results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. AICAR (Acadesine) induces mitophagy. Phase 3.

2020, 8;11(6):427

2020, 10.1096/fj.202001168RR

2020, 22(2):e13131

S1323

7-Methoxyisoflavone

7-Methoxyisoflavone (MIF) is a potent activator of adenosine monophosphate-activated protein kinase (AMPK).

S9604

IM156

IM156, a metformin derivative, is a potent activator of AMPK that increases AMPK phosphorylation. IM156 blocks oxidative phosphorylation (OXPHOS) through the inhibition of complex I and increases apoptosis. IM156 ameliorates various types of fibrosis and inhibits tumors.

S8953

ASP4132

ASP4132 is a potent and orally active activator of Adenosine Monophosphate-Activated Protein Kinase (AMPK) with EC50 of 0.018 μM. ASP4132 is used as a clinical candidate for the treatment of human cancer.

S0795

O-304

O-304 (O-304X) is an orally available pan-activator of AMPK activated protein kinase (AMPK). O-304 (O-304X) exhibits a great potential as a novel drug to treat type 2 diabetes (T2D) and associated cardiovascular complications.

S0411

BAM 15

BAM 15 is a novel mitochondrial protonophore uncoupler capable of protecting mammals from acute renal ischemic-reperfusion injury and cold-induced microtubule damage. BAM 15 is also a potent AMPK activator. BAM 15 attenuates transportation-induced apoptosis in iPS-differentiated retinal tissue.

S1396

Resveratrol

Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.

2020, 133:115252

2020, 13;295(11):3485-3496

2020, 19(4):3269-3277

S2542

Phenformin HCl

Phenformin HCl is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class. It activates AMPK, increasing activity and phosphorylation.

2019, 178(5):1102-1114

2019, 10(1):3856

2017, 292(7):2830-2841

S5284

Adenosine 5'-monophosphate monohydrate

Adenosine 5'-monophosphate monohydrate (5'-AMP) is an activator of a class of protein kinases known as AMP-activated protein kinase (AMPK).

S8335

PF-06409577

PF-06409577 is orally bioavailable AMPK activator with EC50 of 7 nM for α1β1γ1 in the TR-FRET assay and it shows no detectable inhibition of hERG in a patch-clamp assay (100 μM) and was not an inhibitor (IC50 > 100 μM) of the microsomal activities of major human cytochrome P450 isoforms.

S3832

Euphorbiasteroid

Euphorbiasteroid, a component of Euphorbia lathyris L., inhibits adipogenesis of 3T3-L1 cells through activation of the AMPK pathway and induces HL-60 cells to apoptosis via promoting Bcl-2/Bax apoptotic signaling pathway in a dose-dependent manner.

S7898

GSK621

GSK621 is a specific and potent AMPK activator.

2020, 12(18):18522-18544

2019, 10(1-:2987

2019, 26(13):3613-3628

S8654

ex229 (compound 991)

EX229 (compound 991) is a potent AMPK activator that is 5-10-fold more potent than A769662 in activating AMPK.

2019, 29(10):3331-3348

S8803

MK-3903

MK-3903 is a potent and selective AMPK activator with an EC50 of 8 nM for α1 β1 γ1 subunit. It activates 10 of the 12 pAMPK complexes with EC50 values in the range of 8-40 nM and maximal activation >50%.

S9096

ligustroflavone

Ligustroflavone, isolated from the leaves of Turpinia montana, shows high antioxidant capacity and is reported to be an AMPK activator.

S2942

EB-3D

EB-3D is a potent and selective inhibitor of choline kinase α (ChoKα) with IC50 of 1 μM for ChoKα1. EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells.

S7953

ETC-1002

ETC-1002,also known as Bempedoic acid, is an orally available, once-daily LDL-C lowering small molecule designed to lower elevated levels of LDL-C and to avoid side effects associated with existing LDL-C lowering therapies.ETC-1002 is an activator of hepatic AMP-activated protein kinase (AMPK). It has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).

2020, 25

S9116

Chikusetsusaponin IVa

Chikusetsusaponin IVa (Calenduloside F), a major active ingredient of triterpenoid saponins, has numerous pharmacological activities, including cytotoxic activity against various cancer cells, anti-inflammatory activity, prevention of dental caries and induction of genta-micin nephrotoxicity. Chikusetsusaponin IVa is a novel AMPK activator.

S4561

Danthron

Danthron (Chrysazin, Antrapurol) functions in regulating glucose and lipid metabolism by activating AMPK. Danthron is a natural product extracted from the traditional Chinese medicine rhubarb. Danthron used to be a laxativa and now is currently used as an antioxidant in synthetic lubricants, in the synthesis of experimental antitumor agents, as a fungicide and as an intermediate for making dyes.

S6221

Methyl cinnamate

Methyl cinnamate, an active component of Zanthoxylum armatum, is a widely used natural flavor compound with antimicrobial and tyrosinase inhibitor activities. Methyl Cinnamate Inhibits Adipocyte Differentiation via Activation of the CaMKK2--AMPK Pathway in 3T3-L1 Preadipocytes.

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