AMPK Inhibitor

ARUK2010694 (Compound 20) is a potent and selective NUAK1 inhibitor with a pIC₅₀ of 8.7. ARUK2010694 also inhibits CDK2, CDK4 and CDK6 activity, with inhibitory rate of 13%, 63% and 32% at 1 μM. ARUK2010694 can be used for the research of neurological disease, such as Alzheimer’s disease (AD).

HK2-IN-4 is a selective hexokinase 2 (HK2) inhibitor with an IC₅₀ value of 0.79 μM and a K_d value of 0.41 μM. HK2-IN-4 blocks the interaction between HK2 and voltage-dependent anion channel 1 (VDAC1). HK2-IN-4 reduces lactate and ATP levels in cancer cells. HK2-IN-4 induces the production of apoptosis (apoptosis) markers in cancer cells, including increased p-AMPK/AMPK ratio and Bax levels, as well as decreased Bcl2 levels. HK2-IN-4 inhibits the proliferation of cancer cells with high HK2 expression. HK2-IN-4 can be used in research related to colorectal cancer and non-small cell lung cancer.

SIK-IN-3 (Compound 6B) is an inhibitor for salt-inducible kinase (SIK), which inhibits SKI1, SIK2 and SIK3 with IC₅₀s of 0.1, 0.3 and 0.8 nM, respectively. SIK-IN-1 inhibits the release of TNFa with IC₅₀ of 0.6 nM, stimulates the LPS (HY-D1056) -induced IL-10 release with EC₅₀ of 3 nM in human macrophages.

FGFR4-IN-23 (compound 48c) is a FGFR4 inhibitor with an IC₅₀ value of 2.9 nM against FGFR4^WT kinase. FGFR4-IN-23 inhibits the phosphorylation of FGFR4, AKT and MAPK.

AMPK-IN-6 (compound 13a) is potent AMPK inhibitor with an IC₅₀ value of 0.093 µM. AMPK-IN-6 induces apoptosis and inhibits autophagy. AMPK-IN-6 shows antiproliferative activity. AMPK-IN-6 has the potential for the research of pulmonary arterial hypertension.

Multi-kinase-IN-12 is a non-selective multi-target inhibitor, with IC₅₀ values against human targets as follows: Flt3 < 0.001 μM, c-Src 0.002 μM, KDR 0.004 μM, Eph-A2, MNK-1 and Flt1 0.011 μM, Lck 0.016 μM, Rsk1 0.21 μM, and α2 subunit of AMPK 0.041 μM. Multi-kinase-IN-12 can be used in research related to solid tumors.

SIK-IN-2 (Compound 45) is an inhibitor for salt-inducible kinase (SIK), which inhibits SKI1, SIK2 and SIK3 with IC₅₀s of 0.1, 0.2 and 0.4 nM, respectively. SIK-IN-2 inhibits the release of TNFa with IC₅₀ of 0.5 nM, stimulates the LPS (HY-D1056) -induced IL-10 release with EC₅₀ of 2 nM in human macrophages.

OICR19451 is an orally active dual NUAK1/NUAK2 and MARK2/MARK3 kinase inhibitor, with IC₅₀ values of 12 nM and 10 nM against NUAK1 and NUAK2, and 101 nM and 124 nM against MARK2 and MARK3, respectively. OICR19451 modulates the Hippo signaling pathway, increases the phosphorylation level of YAP, enhances the cytoplasmic localization of YAP/TAZ, and inhibits the expression of oncogenes. OICR19451 inhibits cancer cell growth, reduces metastasis, promotes tumor capsule formation, and improves mouse survival in an orthotopic breast cancer model. OICR19451 can be used for research related to triple-negative breast cancer.

SBI-0206965 (Standard) is the analytical standard of SBI-0206965 (HY-16966). This product is intended for research and analytical applications. SBI-0206965 is a potent, selective and cell permeable autophagy K_inase ULK1 inhibitor with IC₅₀s of 108 nM for ULK1 K_inase and 711 nM for the highly related K_inase ULK2. SBI-0206965 is also an AMPK inhibitor that can paradoxically increase Thr172 phosphorylation.

MARK-IN-2 (Standard) is the analytical standard of MARK-IN-2 (HY-101934). This product is intended for research and analytical applications. MARK-IN-2 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC₅₀ of 5 nM.

BAY-3827 (Standard) is the analytical standard of BAY-3827 (HY-112083). This product is intended for research and analytical applications. BAY-3827, a chemical probe, is a potent and selective AMPK inhibitor with IC₅₀ values of 1.4 nM at low (10 μM ATP concentration) and 15 nM at high (2 mM ATP concentration). BAY-3827 shows over 500-fold selectivity for most of the 331 K_inases. BAY-3827 prevents phosphorylation of acetyl-CoA carboxylase 1 and shows strongest anti-proliferative activity in androgen-dependent prostate cancer cell lines.

AMPK activator 16 (compound 6) is a AMP-activated protein kinase (AMPK) inhibitor. AMPK activator 16 shows the most efficient interactions with the key residues of AMPK and demonstrates significant activation of AMPK. AMPK activator 16 increases the expression of phosphorylated AMPK (p-AMPK) and its downstream signaling proteins, such as phosphorylated ACC (Acetyl-CoA Carboxylase) (p-ACC) and phosphorylated raptor (p-raptor), in N2a cells.

NEU-4438 is an antimalarial agent. NEU-4438 inhibits DNA synthesis, reduces AMPK-γ, and increases Clathrin heavy chain. NEU-4438 exhibits antiparasitic activity against Trypanosoma brucei. NEU-4438 reduces trypanosome tissue burden in a chronic HAT mouse model.

RMC-7977 (Standard) is the analytical standard of RMC-7977 (HY-156498). This product is intended for research and analytical applications. RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (K_d = 195 nM) and KRAS (G12V) (K_d = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRAS^G12C cancer models, and demonstrates good tolerability across various RAS cancer models.

STO-609 (Standard) is the analytical standard of STO-609 (HY-19805). This product is intended for research and analytical applications. STO-609 is a selective and cell-permeable inhibitor of the Ca²⁺/calmodulin-dependent protein K_inase K_inase (CaM-KK), with K_i values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 inhibits AMP-activated protein K_inase K_inase (AMPKK) activity in HeLa cell lysates with an IC₅₀ ~0.02 g/ml.

GSK-690693 (Standard) is the analytical standard of GSK-690693 (HY-10249). This product is intended for research and analytical applications. GSK-690693 is an ATP-competitive pan-Akt inhibitor with IC₅₀s of 2 nM, 13 nM, 9 nM for Akt1, Akt2 and Akt3, respectively. GSK-690693 is also an AMPK inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation.

Fenitrothion (Standard) is the analytical standard of Fenitrothion (HY-B1885). This product is intended for research and analytical applications. 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 (Standard) is the analytical standard of Dorsomorphin (HY-13418A). This product is intended for research and analytical applications. Dorsomorphin (BML-275) is a selective and ATP-competitive AMPK inhibitor (K_i=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).

Dorsomorphin (dihydrochloride) (Standard) is the analytical standard of Dorsomorphin (dihydrochloride). This product is intended for research and analytical applications. Dorsomorphin (Compound C) dihydrochloride is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).