AMPK Inhibitor

MARK-IN-1 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC₅₀ of <0.25 nM.

α-Terpineol (with oral activity) can be found in Eucalyptus globulus Labill. α-Terpineol exhibits strong antimicrobial activity against periodontopathic and cariogenic bacteria.α-Terpineol possesses antifungal activity against T. mentagrophytes, and the activity might lead to irreversible cellular disruption. In addition, α-Terpineol exhibits antineuropathic and anti-inflammatory activities. α-Terpineol can be utilized in research related to diarrhea, neuropathic pain, infections, and inflammation.

MARK-IN-4 (Compound 18) is a MARK inhibitor with an IC₅₀ of 1 nM. MARK-IN-4 is applicable to Alzheimer's disease research.

AMPK-IN-4 (compound 19) is a potent inhibitor of (AMPK(α1) and AMPK(α2) with IC₅₀s of 393 nM and 141 nM, respectively. AMPK-IN-4 plays an important role in cancer research.

Maduramicin ammonium (Maduramycin ammonium) is isolated from the actinomycete Actinomadura rubra. Maduramicin ammonium (Maduramycin ammonium) is an anticoccidial agent for the the treatment of Eimeria spp., E. adenoeides, E. gallopavonis, and E. dispersa infection. Maduramicin ammonium (Maduramycin ammonium) induces cell apoptosis in chicken myocardial cells via intrinsic and extrinsic pathways.

Methyl succinate is a mitochondrial complex II substrate. Methyl succinate can bypass the inhibition of complex I by Metformin (HY-B0627), restore mitochondrial electron transfer, and reduce AMPK phosphorylation. Methyl succinate is capable of protecting MIN6 β-cells and primary rat β-cells from biguanide-induced toxicity and apoptosis in vitro. Methyl succinate can be used in the research of diseases such as diabetes mellitus.

AD1058 is an orally active, selective, and BBB-permeable inhibitor of ATR (IC₅₀: 1.6 nM). AD1058 exhibits anticancer activity by inhibiting tumor cell proliferation, inducing cell cycle arrest, and promoting apoptosis. AD1058 is suitable for research on advanced malignancies and brain metastases.

Rubrofusarin gentiobioside (Rrubrofusarin-6-β-gentiobioside) is an orally active weak inhibitor of PTP1B and MAO-A (IC₅₀ >100 μM), and its glycosylation modification results in lower biological activity than its aglycone Rubrofusarin (HY-130307). Rubrofusarin gentiobioside promotes AMPK phosphorylation in an LKB1-independent manner and inhibits the mTOR signaling pathway, thereby downregulating the expressions of PPARγ, C/EBPα, as well as FAS, LPL and aP2. Rubrofusarin gentiobioside inhibits lipid accumulation, reduces body weight and epididymal white adipose tissue volume, improves fatty liver, and shows no cytotoxicity to hepatocytes. Rubrofusarin gentiobioside is widely used in obesity-related studies.

PKC-iota inhibitor 1 is a protein kinase C-iota (PKC-ι) inhibitor with an IC₅₀ value of 0.34 μM. PKC-iota inhibitor 1 can be used for the study of cancer.

MARK4 inhibitor 1 is a potent and selective microtubule affinity-regulating kinase 4 (MARK4) inhibitor, with an IC₅₀ of 1.54 μM. MARK4 inhibitor 1 inhibits cancer cell proliferation, metastasis and induces apoptosis.

Fenitrothion is a broad-spectrum and orally active insecticide/acaricide. Fenitrothion inhibits cholinesterase, AMPKα and IRS1/PI3K/AKT. Fenitrothion causes Apoptosis, reduces SOD activity. Fenitrothion shows insecticidal effect against Rhyzopertha dominica and Tribolium castaneum adults. Fenitrothion is widely used in cotton crops, vegetable crops, fruit crops and field crops, especially rice. Fenitrothion can be used for brain and spleen toxicology studies.

Dorsomorphin dihydrochloride (GMP) is the GMP level of Dorsomorphin dihydrochloride (HY-13418). GMP guidelines are used to produce Dorsomorphin dihydrochloride (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. Dorsomorphin dihydrochloride (GMP) is a potent, selective and ATP-competitive AMPK inhibitor. Dorsomorphin dihydrochloride (GMP) can be used for the research of induced differentiation of pluripotent stem cells (PSCs).

SIK-IN-1 (Compound 53) is an inhibitor for salt-inducible kinase (SIK), which inhibits SIK1, SIK2 and SIK3 with IC₅₀s of 0.1, 0.4 and 1.5 nM, respectively. SIK-IN-1 inhibits the release of TNFa with IC₅₀ of 0.5 nM, stimulates the LPS (HY-D1056) -induced IL-10 release with EC₅₀ of 4 nM in human macrophages.

Alloc-DOX (N-Alloc doxorubicin) is a Doxorubicin (HY-15142A) prodrug. The combination of a catalyst (such as nano-palladium) and alloc-DOX leads to a decrease in cell viability and tumour growth.

8-Bromo-AMP (8-Bromoadenosine 5'-monophosphate) is an AMP analog. 8-Bromo-AMP inhibits ADP-dependent glucokinase (ADPGK). 8-Bromo-AMP competitively inhibits ADPGK by binding to the nucleotide-binding site, inducing conformational changes, and acting on catalytic residues. 8-Bromo-AMP non-competitively inhibits rat adenylate kinase isozymes AK-M, AK II, and AK III. 8-Bromo-AMP inhibits T cell activation-induced ROS production and ROS-dependent IL-2 and IκB expression. 8-Bromo-AMP is used in research on cancer and myocardial ischemia-reperfusion injury.

KHKI-01128 is a NUAK2 inhibitor, with an IC₅₀ of 0.024 μM. KHKI-01128 exhibits potent anticancer activity against SW480 colorectal cancer cells.

10Z-Hymenialdisine ((Z)-Hymenialdisine) is a natural bioactive pyrrole alkaloid. 10Z-Hymenialdisine is a pan kinase inhibitor, and has anticancer activities.

Kazinol U inhibits melanogenesis through the inhibition of tyrosinase-related proteins via AMPK activation.

UCB9386 is the selective and brain penetrant inhibitor for Nuak1 with a pIC₅₀ of 10.1. UCB9386 inhibits Nuak2 and Kak2 with an inhibition rate of ca. 50% at 10 nM.

Dox-btn2 is a biotin labeled Doxorubicin (HY-15142A), with a biotin label at the point of conjugation to doxorubicin at 3'-NH₂. Dox-btn2 can be used for cell imaging. While Doxorubicin is mainly accumulated in the nucleus, while Dox-btn2 is mainly located in the cytoplasm.