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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 hydrochlorideT102025316-40-9Doxorubicin 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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Cited - MetforminT8526657-24-9Metformin (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
SizeQTY Cited - DorsomorphinT1977866405-64-3Dorsomorphin (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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Cited - Metformin hydrochlorideT07401115-70-4Metformin 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
SizeQTY Cited - GlycycoumarinTN170294805-82-0Glycycoumarin is an estrogen agonist, it shows moderate inhibitory effects against CYP1A2 and CYP2B6.
- $74
SizeQTY - Dorsomorphin dihydrochlorideT61461219168-18-9Dorsomorphin 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
SizeQTY Cited - EX229TQ00281219739-36-2EX229 (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
SizeQTY - AICART14772627-69-2AICAR (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
SizeQTY Cited - MK8722T160991394371-71-1MK8722 is an effective and systemic activator of pan-AMPK.
- $31
SizeQTY - AldometanibT601222904601-67-6Aldometanib (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].
- $83
SizeQTY - Bempedoic acidT3625738606-46-7Bempedoic 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
SizeQTY - HTH-01-015T23741613724-42-7In houseHTH-01-015 is a selective NUAK1 inhibitor with an IC50 of 100 nM.
- $37
SizeQTY - 8-ChloroadenosineT1966134408-14-58-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.
- $68
SizeQTY - A-769662T2468844499-71-4A-769662 is an effective, reversible AMPK activator(EC50=0.8 μM).
- $33
SizeQTY Cited - Platycodin DT388958479-68-8Platycodin 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.
- $52
SizeQTY Cited - GSK-1070916T6129942918-07-2GSK-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
SizeQTY - [6]-GingerolT340523513-14-6[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
SizeQTY Cited - NorathyriolTN19903542-72-1Norathyriol is a potent PTP1B inhibitor with good cell permeability and oral availability.
- $152
SizeQTY - ARN-3236T59931613710-01-2ARN-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
SizeQTY Cited - AMPK-IN-3T627452417674-27-0AMPK-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
SizeQTY - EpiberberineT5S23616873-09-21. 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
SizeQTY - BritanninT579333627-28-0Britannin, a sesquiterpene lactone, inhibits proliferation and induces apoptosis through the mitochondrial signaling pathway in human breast cancer cells.
- $40
SizeQTY - YLF-466DT133681273323-67-3YLF-466D (C24) is a novel AMPK activator that inhibits platelet aggregation.
- $52
SizeQTY - YKL-06-061T55762172617-15-9YKL-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
SizeQTY - Urolithin BT132651139-83-9Urolithin 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.
- $42
SizeQTY - Beta-HydroxyisovalerylshikoninTN14407415-78-3Beta-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
SizeQTY - DK419T151372102672-22-8In houseDK419 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
SizeQTY - DemethyleneberberineT4S080025459-91-0Demethyleneberberine, 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
SizeQTY - Palmitelaidic AcidT1950010030-73-6Palmitelaidic Acid (trans-Palmitoleic acid) is one of the most abundant fatty acids in serum and tissue.
- $80
SizeQTY - EB-3DT79551839150-63-8EB-3D is a potent and selective choline kinase alpha 1 (ChoKα1) inhibitor (IC50: 1 μM) with anti-cancer activity.
- $93
SizeQTY - MOTS-c(Human) Acetate（1627580-64-6 free）TP2312MOTS-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
SizeQTY - AMPK activator 2 hydrochloride( 2410961-69-0 Free base)T60675LAMPK 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
SizeQTY - Mogroside VT297888901-36-4Mogroside 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
SizeQTY - ASP4132T84321640294-30-9ASP4132 is an orally active AMPK activator (EC50 : 18 nM), has anti-cancer activity.
- $62
SizeQTY - XanthoangelolT1335462949-76-2Xanthoangelol, 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.
- $148
SizeQTY - KahweolTN18286894-43-5Kahweol 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
SizeQTY - Buformin hydrochlorideT200291190-53-0Buformin hydrochloride (NSC-528218) is a potent AMPK activator,an oral antidiabetic drug of the biguanide class. Buformin delays the absorption of glucose from the gastrointestinal tract increases insulin sensitivity and glucose uptake into cells and inhibits synthesis of glucose by the liver. Biguanides may antagonize the action of glucagon, thus reducing fasting glucose levels.
- $30
SizeQTY - BrazilinT6S1784474-07-71. 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
SizeQTY - Onjisaponin BTN114035906-36-6Onjisaponin B induces autophagy via the AMPK-mTOR signaling pathway, increases the NGF level and accelerates both the removal of mutant huntingtin and A53T α±-synuclein, it may have potential therapeutic effects on Parkinson disease, Alzheimer disease and Huntington disease.
- $93
SizeQTY - STO-609T354652029-86-4STO-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
SizeQTY Cited - MARK4 inhibitor 1T119472271081-58-2MARK4 inhibitor 1 inhibits cancer cell proliferation, metastasis and induces apoptosis. MARK4 inhibitor 1 is a potent microtubule affinity-regulating kinase 4 (MARK4) inhibitor, with an IC50 of 1.54 μM.
- $77
SizeQTY - WZ4003T62911214265-58-3WZ4003, 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
SizeQTY - Cimiracemoside CTN1499256925-92-5Cimiracemoside C (Cimicifugoside M) is an active component of Cimicifuga racemosa. It activates AMPK and has the potential activity against diabetes.
- $54
SizeQTY - Ginkgolide KT8200153355-70-5Ginkgolide K induces protective autophagy through the AMPK mTOR ULK1 signalling pathway. It possesses neuroprotective activity.
- $80
SizeQTY Cited - AMAROGENTINT549721018-84-8Amarogentin is mainly extracted from Swertia and Gentiana roots. It plays cemopreventive therapeutic role during liver carcinogenesis through modulation of cell cycle and apoptosis
- $33
SizeQTY Cited - HernandezineTN17316681-13-6Hernandezine is an activator of AMPK activator and a selective reversing agent for ABCB1-mediated MDR in cancer cells.
- $156
SizeQTY - Flufenamic acidT0858530-78-9Flufenamic 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
SizeQTY - Ginkgolide CT275015291-76-6Ginkgolide C (BN-52022), a natural product, can enhance the cardiac function of rats in the body.
- $50
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