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Chromatin/Epigenetic

DNA Methyltransferase

(88)

Epigenetic Reader Domain

HIF/HIF Prolyl-Hydroxylase

(213)

Histone Acetyltransferase

(125)

Histone Demethylase

(196)

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

MK8722

T160991394371-71-1

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

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Doxorubicin hydrochloride

T102025316-40-9

Doxorubicin hydrochloride is an anthracycline antibiotic with cytotoxic and antitumor activity. It is an effective inhibitor of human DNA topoisomerase I and II, with IC50 values of 0.8 μM and 2.67 μM, respectively. In addition to inhibiting DNA topoisomerases, it can reduce the phosphorylation of AMPK and its downstream target, acetyl-CoA carboxylase. Doxorubicin hydrochloride also induces apoptosis and autophagy. In animal studies, it is commonly used to induce models of acute renal failure, chronic kidney injury, and heart failure.

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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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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 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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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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MK-0626

T68863690257-74-0

MK-0626 is an orally available dipeptidyl peptidase IV (DPP-4) inhibitor that attenuates hepatic steatosis and accumulation by enhancing AMPK activity.MK-0626 attenuates TAC-induced diabetic pancreatic islet injury by restoring the expression of GLP-1R.MK-0626 is able to increase circulating endothelial progenitor cell numbers and endothelial-type nitric oxide synthase expression by promoting neoangiogenesis.

$989

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RMC-7977

T812632765082-12-8

RMC-7977 is a highly selective inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS with anticancer activity for the study of solid tumors with KRAS G12C mutations.

$257

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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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Doxorubicin

T145623214-92-8

Doxorubicin (Adriamycin) is a fluorescent anthracycline antitumor antibiotic that inhibits Topoisomerase I/II, induces apoptosis and autophagy, downregulates the AMPK signaling pathway, and is commonly used in cancer chemotherapy as well as in models of nephritis and heart failure.

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AICAR

T14772627-69-2

AICAR (Acadesine) is an AMPK activator. AICAR has the functions of metabolic regulation, muscle function regulation, anti-cancer effect, neuroprotection and anti-aging.

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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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[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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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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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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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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SBI-0206965

T21281884220-36-3

SBI-0206965 is a potent, selective, and cell-permeable autophagy kinase ULK1 inhibitor with an IC50 of 108 nM for ULK1 kinase activity and 711 nM for ULK2.

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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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Levocarnitine propionate

T1182L20064-19-1

Levocarnitine propionate (L-Propionylcarnitine) is a propionyl-coenzyme A (Pro-CoA) derivative with anti-ischemic effects and high affinity for muscle L-carnitine transferase. Levocarnitine propionate enhances substrate oxidation and mitochondrial respiration in the heart of diabetic rats, reduces gastric ulcer area, induces mucosal recovery, and can be used to study acute respiratory distress syndrome and chronic gastric ulcers in Alzheimer's disease.

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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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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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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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Daphnetin

T2851486-35-1

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

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