hki

HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 (IC50s: 34 nM and 33 nM), effectively suppressing EGFR autophosphorylation (at Y1068), as well as AKT and MAPK phosphorylation.

HKI-357 dimaleate is an irreversible dual inhibitor of EGFR and ERBB2. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.

Neratinib (HKI-272) (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59/92 nM), respectively.

Neratinib maleate (HKI-272 maleate) is an irreversible, orally active and highly selective inhibitor of HER2 and EGFR with IC50 values of 59 nM and 92 nM, respectively.Neratinib maleate has antitumor activity and can be used to treat gastrointestinal, respiratory, genitourinary, and cutaneous and musculoskeletal diseases, and can be used to study breast and prostate cancer. used in the study of breast and prostate cancer.

MDL-102234 is an adenosine A1 receptor antagonist.

HBY-793 is an HIV-1 proteinase inhibitor.

HKI12134085 (compound 3), an orally administered nitrobenzothiazinone (BTZ) derivative, demonstrates antibacterial efficacy against Mycobacterium tuberculosis. This compound exhibits significant in vivo inhibitory potency within a BALB/c mouse model of Mycobacterium tuberculosis infection [1].

KHKI-01215 is an effective NUAK2 inhibitor with anticancer activity, inhibiting the proliferation of SW480 cancer cells and inducing apoptosis in SW480 cells. KHKI-01215 is used for cancer research.

KHKI-01128 is a NUAK2 inhibitor with an IC50 of 0.024 μM. It demonstrates effective anticancer activity against SW480 colorectal cancer cells.

Exo-α-Fucosidase, Elizabethkingia meningoseptica (EC 3.2.1.51), is a glycoside hydrolase capable of releasing free fucose.

KHK-IN-2 is a selective inhibitor of ketohexokinase with an IC50 value of 0.45 μM.

CHK-IN-1 is a dual inhibitor of CHK1 and CHK2 with antiproliferative activity.

KHK-IN-1 (KHK-IN-8) is a selective and cell membrane permeable inhibitor of ketohexokinase (KHK, IC50=12 nM; F=34%). KHK-IN-1 inhibits F1P production in HepG2 cell lysates with IC50 of 400 nM. KHK-IN-1 has potential for the study of obesity and diabetes.

Dehydroabiethylamine (NSC-2955) is an inducer of hepatic CYP2B activity. Dehydroabiethylamine inhibits pyruvate dehydrogenase kinases (PDKs) and intracellular cholesterol transport with anti-tumor activity.

Sodium dichloroacetate (BCA) , a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress a mitochondrial potassium-ion channel axis, trigger apoptosis in cancer cells, and inhibit tumor growth.

Dicoumarol (Dicumarol) is a hydroxycoumarin originally isolated from molding sweet-clover hay, with anticoagulant and vitamin K depletion activities. Dicoumarol is a competitive inhibitor of vitamin K epoxidereductase; thus, it inhibits vitamin K recycling and causes depletion of active vitamin K in blood. This prevents the formation of the active form of prothrombin and several other coagulant enzymes, and inhibits blood clotting.

KPLH1130, a specific pyruvate dehydrogenase kinase (PDK) inhibitor, enhances glucose tolerance in mice fed a high-fat diet (HFD). It effectively hinders macrophage polarization and mitigates proinflammatory reactions.

PDK4-IN-1 hydrochloride, an anthraquinone derivative, is a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an IC50 value of 84 nM.

KHK-IN-1 hydrochloride is a selective, cell-permeable, and efficient hexokinase (KHK) inhibitor, useful for studying diabetes and obesity.

VER-246608 is an effective and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (IC50s: 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively).VER-246608 disrupts Warburg metabolism and induces context-dependent cytosta

KHK-IN-7 (compound 2) is an inhibitor of ketohexokinase (KHK) and is utilized in research related to metabolic disorders.

JX06, a potent, selective and covalent PDK inhibitor, inhibits PDK1, PDK2 and PDK3 with IC50 of 49 nM, 101 nM and 313 nM respectively.

AZD7545 is a potent PDHK inhibitor.

MTX-211, an inhibitor of EGFR and PI3K, is used for the therapy of cancer and other diseases.