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Chromatin/Epigenetic Filter
Chromatin/EpigeneticAMPK
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.
Doxorubicin hydrochloride
Cited
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.
- $34
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CitedMetformin Cited
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.
- $39
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CitedDorsomorphin
Cited
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.
- $48
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CitedMetformin hydrochloride Cited
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.
- $33
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CitedMK8722
T160991394371-71-1
MK8722 is an effective and systemic activator of pan-AMPK.
- $31
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Glycycoumarin
TN170294805-82-0
Glycycoumarin is an estrogen agonist, it shows moderate inhibitory effects against CYP1A2 and CYP2B6.
- $35
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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].
- $38
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Dorsomorphin dihydrochloride Cited
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.
- $30
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CitedAICAR Cited
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.
- $30
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CitedEX229
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.
- $31
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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.
- $30
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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.
- $41
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A-769662 Cited
T2468844499-71-4
A-769662 is an effective, reversible AMPK activator(EC50=0.8 μM).
- $33
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Cited[6]-Gingerol Cited
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.
- $35
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CitedNorathyriol
TN19903542-72-1
Norathyriol is a potent PTP1B inhibitor with good cell permeability and oral availability.
- $152
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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.
- $31
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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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ARN-3236 Cited
T59931613710-01-2
ARN-3236 is an orally active and selective inhibitor of salt-inducible kinase 2 (SIK2), with IC50 values of <1 nM for SIK2, 21.63 nM for SIK1, and 6.63 nM for SIK3. ARN-3236 exhibits anti-cancer activity.
- $55
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CitedDemethyleneberberine
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.
- $61
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YLF-466D
T133681273323-67-3
YLF-466D (C24) is a novel AMPK activator that inhibits platelet aggregation.
- $52
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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.
- $30
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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.
- $40
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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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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.
- $79
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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.
- $54
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EB-3D
T79551839150-63-8
EB-3D is a potent and selective choline kinase alpha 1 (ChoKα1) inhibitor (IC50: 1 μM) with anti-cancer activity.
- $93
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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).
- $51
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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.
- $30
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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.
- $43
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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).
- $80
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Palmitelaidic Acid
T1950010030-73-6
Palmitelaidic Acid (trans-Palmitoleic acid) is one of the most abundant fatty acids in serum and tissue.
- $80
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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.
- $67
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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.
- $37
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STO-609 Cited
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).
- $35
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CitedASP4132
T84321640294-30-9
ASP4132 is an orally active AMPK activator (EC50 : 18 nM), has anti-cancer activity.
- $62
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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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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.
- $54
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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.
- $33
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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.
- $41
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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.
- $54
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Hernandezine
TN17316681-13-6
Hernandezine is an activator of AMPK activator and a selective reversing agent for ABCB1-mediated MDR in cancer cells.
- $156
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Flufenamic acid
T0858530-78-9
Flufenamic acid (Arlef) is an anthranilic acid derivative with analgesic, anti-inflammatory, and antipyretic properties. It is used in musculoskeletal and joint disorders and administered by mouth and topically.
- $33
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Ginkgolide K Cited
T8200153355-70-5
Ginkgolide K induces protective autophagy through the AMPK mTOR ULK1 signalling pathway. It possesses neuroprotective activity.
- $80
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CitedN,N-Didesethyl Sunitinib Hydrochloride
T60128873077-70-4
N,N-Didesethyl Sunitinib Hydrochloride is a potent AMPK inhibitor with IC50 of 393 nM and 141 nM for AMPKα1 and AMPK2,respectively.
- $195
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XMD-17-51 Trifluoroacetate
T91912436579-93-8
XMD-17-51 Trifluoroacetate is a pyrimido-diazepinone compound that regulates protein kinases.
- $68
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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.
- $42
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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).
- $30
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AICAR phosphate
T14149681006-28-0
AICAR phosphate (Acadesine phosphate) is an AMPK activator and inhibitor of autophagy, YAP, and mitophagy. It serves as an adenosine analog, regulating glucose and lipid metabolism, and inhibiting the production of pro-inflammatory cytokines and iNOS.
- $49
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