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Chromatin/Epigenetic

DNA Methyltransferase

(38)

Epigenetic Reader Domain

HIF/HIF Prolyl-Hydroxylase

(76)

Histone Acetyltransferase

(48)

Histone Demethylase

(92)

Histone Methyltransferase

Methionine Adenosyltransferase (MAT)

PI3K/Akt/mTOR signaling

AMPK

AMPK (AMP-activated protein kinase) is an enzyme that plays a role in cellular energy homeostasis. It consists of three proteins (subunits) that together make a functional enzyme. The net effect of AMPK activation is stimulation of hepatic fatty acid oxidation andketogenesis, inhibition of cholesterol synthesis, lipogenesis, and triglyceride synthesis, inhibition of adipocyte lipolysis and lipogenesis, stimulation of skeletal muscle fatty acid oxidation and muscle glucose uptake by pancreatic beta-cells. AMPK acts as a metabolic master switch regulating several intracellular systems including the cellular uptake of glucose, the β-oxidation of fatty acids and the biogenesis of glucose transporter 4 (GLUT4) and mitochondria.

Filter HomeSignaling PathwaysPI3K/Akt/mTOR signaling-Chromatin/EpigeneticAMPK

Doxorubicin hydrochloride

T102025316-40-9

Doxorubicin hydrochloride (Adriamycin) belongs to the anthracycline class of antibiotics and is an inhibitor of human DNA topoisomerase I II (IC50=0.8 2.67 μM). Doxorubicin hydrochloride exhibits cytotoxicity and antitumor activity. Doxorubicin hydrochloride reduces the phosphorylation of AMPK and its downstream target protein acetyl coenzyme A carboxylase, and induces apoptosis and autophagy.

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MK8722

T160991394371-71-1

MK8722 is an effective and systemic activator of pan-AMPK.

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Dorsomorphin

T1977866405-64-3

Dorsomorphin (BML-275) is an AMPK inhibitor (Ki=109 nM) that is selective and ATP-competitive. Dorsomorphin inhibits the BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy, and possesses antitumor activity.

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Metformin

T8526657-24-9

Metformin (1,1-Dimethylbiguanide) is an AMPK activator with blood-brain barrier permeability. Metformin may improve glycemic control by increasing insulin sensitivity and decreasing intestinal glucose uptake, and is commonly used in type 2 diabetes research.

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Glycycoumarin

TN170294805-82-0

Glycycoumarin is an estrogen agonist, it shows moderate inhibitory effects against CYP1A2 and CYP2B6.

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Metformin hydrochloride

T07401115-70-4

Metformin hydrochloride (1,1-Dimethylbiguanide hydrochloride), a widely used anti-diabetic drug, exhibits potential anti-Y properties by inhibiting the proliferation of various Y cells, including colon and prostate.

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AICAR

T14772627-69-2

AICAR (Acadesine) is an AMPK activator that causes ZMP accumulation, thereby mimicking the stimulatory effect of AMP on both AMPK and AMPKK. It is commonly used in research related to diabetes, cardiovascular diseases, and tumors.

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Dorsomorphin dihydrochloride

T61461219168-18-9

Dorsomorphin dihydrochloride (BML-275 2HCl) is a potent, selective and ATP-competitive AMPK inhibitor (Ki: 109 nM) and does not exhibit significant activity on structurally related kinases.

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EX229

TQ00281219739-36-2

EX229 (C991) is an allosteric activator of AMPK, with Kds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1, and α1β2γ1, respectively.

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Aldometanib

T601222904601-67-6

Aldometanib (LXY-05-029) is an orally active aldolase inhibitor that prevents FBP from binding to v-ATPase-associated aldolase and activates lysosomal AMPK, useful in metabolic homeostasis research [1].

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GSK-1070916

T6129942918-07-2

GSK-1070916 (GSK-1070916A) is a reversible and ATP-competitive inhibitor of Aurora B C with IC50 of 3.5 nM 6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex. Phase 1.

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[6]-Gingerol

T340523513-14-6

[6]-Gingerol ((S)-(+)-[6]Gingerol), an antioxidant, protects HL-60 cells from oxidative stress. It has protective effects for Yous tumors in the pancreas, ovaries, breast tissue, the bowel, among other tissues.

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Bempedoic acid

T3625738606-46-7

Bempedoic acid (ETC1002) 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. Bempedoic acid(ETC1002) is absorbed rapidly in the small intestine and enters the liver through cell surface receptors different from those transporters that selectively take up statins. Bempedoic acid(ETC1002) is a regulator of lipid and carbohydrate metabolism.

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Platycodin D

T388958479-68-8

Platycodin D may stimulate TNF-α synthesis or inhibit degradation of TNF-α mRNA. Platycodin D (10 30 μM) suppresses prostaglandin E2 production in rat peritoneal macrophages stimulated by the protein kinase C activator 12-O-tetradecanoyl phorbol 13-acetate (TPA). Platycodin D and D3 are useful as expectorant agents in the treatment of various airway diseases, they can increase mucin release from rat and hamster tracheal surface epithelial cell culture and also from intact rat trachea upon nebulization.

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MOTS-c(Human) Acetate（1627580-64-6 free）

TP2312

MOTS-c(Human) Acetate is a mitochondrial-derived peptide. MOTS-c(human) acetate induces the accumulation of AMP analog AICAR, increases activation of AMPK and expression of its downstream GLUT4. MOTS-c(human) acetate induces glucose uptake and improves insulin sensitivity. MOTS-c(human) acetate has implications in the regulation of obesity, diabetes, exercise, and longevity.

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WZ4003

T62911214265-58-3

WZ4003, a highly selective NUAK kinase inhibitor, is with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2, respectively. It is no significant inhibition on 139 other kinases.

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A-769662

T2468844499-71-4

A-769662 is an effective, reversible AMPK activator(EC50=0.8 μM).

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DK419

T151372102672-22-8In house

DK419 is an orally active inhibitor of Wnt β-catenin signaling, with an IC50 of 0.19 μM. DK419 decreases protein lelvels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin.It also induces production of pAMPK.

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Norathyriol

TN19903542-72-1

Norathyriol is a potent PTP1B inhibitor with good cell permeability and oral availability.

$152

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Demethyleneberberine

T4S080025459-91-0

Demethyleneberberine, which is composed of a potential antioxidant structure, could penetrate the membrane of mitochondria and accumulate in mitochondria either in vitro or in vivo.Demethyleneberberine suppresses CYP2E1, hypoxia inducible factor α, and inducible nitric oxide synthase, which contributes to oxidative stress and restored sirtuin 1 AMP-activated protein kinase peroxisome proliferator-activated receptor-γ coactivator-1α pathway-associated fatty acid oxidation in chronic ethanol-fed mice.

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Ginkgolide K

T8200153355-70-5

Ginkgolide K induces protective autophagy through the AMPK mTOR ULK1 signalling pathway. It possesses neuroprotective activity.

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YLF-466D

T133681273323-67-3

YLF-466D (C24) is a novel AMPK activator that inhibits platelet aggregation.

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Beta-Hydroxyisovalerylshikonin

TN14407415-78-3

Beta-Hydroxyisovalerylshikonin is an inhibitor of protein-tyrosine kinases such as v-Src and EGFR, and has been shown to induce apoptosis in several human tumor cell lines. Beta-Hydroxyisovalerylshikonin significantly decreased viability of HCT116 cells (IC50 values = 30.9 μg mL).

$139

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8-Chloroadenosine

T1966134408-14-5

8-Chloroadenosine (NSC-354258) is a 5' AMP-activated protein kinase agonist potentially for the treatment of chronic lymphocytic leukemia. 8-chloroadenosine activity is associated with inhibition of the mTOR pathway.8-Chloroadenosine (NSC-354258) is a nucleoside analog; metabolized in vivo to 8-Chloro-ATP. Incorporates into RNA during transcription and inhibits RNA synthesis. Exhibits cytotoxicity in MM.1S, RPMI-8226, and U266 cancer cell lines; induces G2 M cell cycle arrest and mitotic catastrophe in A549 and H1299 cells. 8-Chloroadenosine (NSC-354258) has been shown to deplete ATP and inhibit tumor growth in hematological malignancies as well as in lung and breast cancer cell lines.

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YKL-06-061

T55762172617-15-9

YKL-06-061 is a selective salt-inducible kinase (SIK) inhibitor with IC50 values of 6.56 nM 1.77 nM 20.5 nM for SIK1 2 3, respectively.

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BAY-3827

T733502377576-35-5

BAY-3827 is a potent and selective AMPK inhibitor with potential antitumor activity, demonstrating antiproliferative effects in an androgen-dependent prostate cancer model and inhibiting the phosphorylation of acetyl CoA carboxylase 1 (ACC-1).

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AMPK-IN-3

T627452417674-27-0

AMPK-IN-3 is a novel, selective and potent AMPK inhibitor with inhibitory effects on AMPK (α2), AMPK (α1) and KDR, with IC50 values of 60.7, 107 and 3820 nM, respectively.AMPK-IN-3 showed anticancer activity in K562 cells.

$109

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PF-249

T246261467059-70-6

PF-249 (PF-06685249) is a β1-selective AMPK with an EC50 of 12 nM for AMPK α1β1γ1 and can be used in studies about diabetic nephropathy.

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Kahweol

TN18286894-43-5

Kahweol has anticarcinogenic, anti-angiogenic,and anti-inflammatory activities, it can block the LPS-induced activation of NF-kappaB by preventing IkappaB degradation and inhibiting IkappaB kinase activity.

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Mogroside V

T297888901-36-4

Mogroside V is a widely used sweetener, has in vitro AMPK activating effect, it also has anti-inflammatory potential in murine macrophages and a murine ear edema model, and has the potential to protect against LPS-induced airway inflammation in a model of ALI. Mogroside V has antioxidant properties and possesses tumor growth inhibitory activity in pancreatic cancer models.

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RGX-202

T7535353-09-3

RGX-202 (β-GPA) is a creatine analog that alters skeletal muscle energy expenditure. It reduces cellular ATP, creatine, and phosphocreatine levels and stimulates AMP-activated protein kinase (AMPK), activating PPARγ coactivator 1α (PGC-1α).

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STO-609

T354652029-86-4

STO-609 is a specific and cell-permeable inhibitor of the Ca2+ calmodulin-dependent protein kinase kinase (CaM-KK) for recombinant CaM-KKα KKβ (Ki: 80 15 ng mL).

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AMPK activator 2 hydrochloride( 2410961-69-0 Free base)

T60675L

AMPK activator 2 hydrochloride is a fluoroguanidine-containing derivative that up-regulates the AMPK signaling pathway and down-regulates mTOR 4EBP1 p70S6K.AMPK activator 2 hydrochloride inhibits the proliferation and migration of human cancer cell lines (UMUC3, T24, A549).

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Vaccarin

T388153452-16-7

Vaccarin is a major flavonoid glycoside in Vaccariae semen, its biotransformation pathways involves methylation, hydroxylation, glycosylation and deglycosylation.

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HTH-01-015

T23741613724-42-7In house

HTH-01-015 is a selective NUAK1 inhibitor with an IC50 of 100 nM.

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Epiberberine

T5S23616873-09-2

1. Epiberberine may be caused drug interactions based on CYP2D6 enzyme. 2. Epiberberine has anti-adipogenic effect is mediated by downregulation of the Raf MEK1 ERK1 2 and AMPKα Akt pathways during 3T3-L1 adipocyte differentiation. 3. Epiberberine, as the brightest FSA emitter among the alkaloids, can also serve as an efficient conformation probe for HTG DNA and discriminate the DNA G-quadruplex from the RNA counterpart.

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ASP4132

T84321640294-30-9

ASP4132 is an orally active AMPK activator (EC50 : 18 nM), has anti-cancer activity.

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Britannin

T579333627-28-0

Britannin, a sesquiterpene lactone, inhibits proliferation and induces apoptosis through the mitochondrial signaling pathway in human breast cancer cells.

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XMD-17-51 Trifluoroacetate

T91912436579-93-8

XMD-17-51 Trifluoroacetate is a pyrimido-diazepinone compound that regulates protein kinases.

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Pomolic acid

TN209713849-91-7

Pomolic acid has anti-cancer, anti-inflammatory and apoptotic activities, it can induce apoptosis in SK-OV-3 cells, which is mediated by the mitochondrial-mediated intrinsic and death receptor-induced extrinsic pathways.

$113

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Urolithin B

T132651139-83-9

Urolithin B is one of the gut microbial metabolites of ellagitannins and is found in diverse plant foods, including pomegranates, berries, walnuts, tropical fruits, and medicinal herbs. Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα, and suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass. Urolithin B has anti-inflammatory and antioxidant effects.

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N,N-Didesethyl Sunitinib

T60128873077-70-4

N,N-Didesethyl Sunitinib is a potent AMPK inhibitor with IC50 of 393 nM and 141 nM for AMPKα1 and AMPK2,respectively.

$147

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Xanthoangelol

T1335462949-76-2

Xanthoangelol, which can be extracted from Angelica keiskei, inhibits obesity-induced inflammatory responses.Xanthoangelol has antimicrobial activity, inhibits monoamine oxidase, and induces apoptosis in neuroblastoma and leukemia cells.

$123

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Brazilin

T6S1784474-07-7

1. Brazilin (Braziletto) exhibits anti-hepatotoxic, antiplatelet effects. 2. Brazilin has cancer preventive effect, may inhibit T24 cell growth and trigger cell death through a c-Fos-mediated and tumor cell specific signaling pathway. 3. Brazilin has anti-inflammatory property, can suppress mastitis and high glucose-induced vascular inflammatory process related with the inhibition of oxidative stress, CAMs expression, and NF-κB activation in HUVEC; may be useful to treat chronic inflammatory disorders including rheumatoid arthritis.

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Cimiracemoside C

TN1499256925-92-5

Cimiracemoside C (Cimicifugoside M) is an active component of Cimicifuga racemosa. It activates AMPK and has the potential activity against diabetes.

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Adenosine 5'-monophosphate monohydrate

T0853L18422-05-4

Adenosine 5'-monophosphate monohydrate (5'-AMP) , also known as 5'-adenylic acid, is a nucleotide that is used as a monomer in RNA. It is an ester of phosphoric acid and the nucleoside adenosine. Adenosine 5'-monophosphate monohydrate consists of a phosphate group, the sugar ribose, and the nucleobase adenine. As a substituent it takes the form of the prefix adenylyl-.

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Phenformin hydrochloride

T1453834-28-6

Phenformin hydrochloride (Phenformin HCl) is an agent belonging to the biguanide class of antidiabetics with antihyperglycemic activity.

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GSK-690693

T6285937174-76-0

GSK-690693 is a pan-Akt inhibitor targeting Akt1 2 3 with IC50 of 2 nM 13 nM 9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.

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