khk

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

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.

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

Evocalcet (KHK7580) has an activating effect on the calcium-sensing receptor (CaSR).

Ketohexokinase inhibitor 1 is a ketohexokinase inhibitor (IC50s: 8.4 nM and 66 nM for KHK-C and KHK-A, respectively).

Brodalumab (AMG 827) is a human monoclonal IgG2 antibody targeting the interleukin 17 receptor (IL-17R), commonly used as an immunosuppressant in treating psoriasis.

Rocatinlimab represents a highly specialized humanized IgG1 monoclonal antibody specifically engineered to target the OX40 receptor (CD134) with exceptional binding affinity. It effectively facilitates the measurable blockade of the OX40-OX40L co-stimulatory axis while simultaneously inducing the targeted depletion of OX40-positive activated T cells through antibody-dependent cellular cytotoxicity (ADCC) across various preclinical experimental models to evaluate the restoration of immune homeostasis during strictly monitored laboratory observation periods.

KHK-IN-3 (Example 1), a ketohexokinase (KHK) inhibitor, plays a crucial role in the study of various diseases including kidney disease, nonalcoholic steatohepatitis (NASH), diabetes, and heart failure. KHK, a pivotal rate-limiting enzyme and fructokinase, facilitates the metabolism of fructose by catalyzing the transformation of fructose into fructose-1-phosphate (FIP) utilizing ATP. This process lacks feedback inhibition, leading to the buildup of metabolites involved in lipogenesis, gluconeogenesis, and oxidative phosphorylation [1].

KHK-IN-5 (Compound 18), a KHK inhibitor, is employed in the study of nonalcoholic fatty liver disease (NAFLD), nonalcoholic steatohepatitis (NASH), and type 2 diabetes (T2DM).

KHK-IN-6 (compound 33) acts as a KHK inhibitor with an IC50 of 0.6nM.

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

KHK-IN-4 (compound 14) is a potent inhibitor of ketohexokinase (KHK), suitable for researching fructose metabolism diseases [1].

KHK-2898 represents a highly specialized humanized monoclonal antibody specifically engineered to target the CD98 heavy chain (CD98hc/SLC3A2) with exceptional binding affinity to the human and monkey LAT1/CD98hc complex. It effectively facilitates the measurable blockade of amino acid transport and the induction of potent antibody-dependent cellular cytotoxicity (ADCC) across various preclinical experimental models to evaluate the disruption of tumor nutrient uptake and metabolic homeostasis during strictly monitored laboratory observation periods and functional cell viability assays.

KHK-2866 is a humanized monoclonal antibody targeting Heparin-Binding Epidermal Growth Factor-like Growth Factor (HB-EGF). By binding to HB-EGF, KHK-2866 blocks its interaction with EGFR and HER4 receptors, thereby inhibiting the proliferation and survival of tumor cells. HB-EGF is frequently overexpressed in various solid tumors, making it a key therapeutic target.

KHK-6 is an inhibitor of serine/threonine kinase hematopoietic progenitor kinase 1 (HPK 1), with an IC50 of 20 nM. This compound enhances cytokine production induced by CD3/CD28 and upregulates the expression of CD69, CD25, and HLA-DR markers on CD4+ and CD8+ T cells. Additionally, KHK-6 augments the T cell-mediated cytotoxicity against SKOV3 and A549 cells.

KHK2823 is a humanized monoclonal antibody targeting human CD123/IL3RA. The recommended isotype control for this compound is human IgG1 kappa, serving as an isotype control. KHK2823 is applicable in leukemia-related research.

KHK6640 is a humanized antibody specific to amyloid beta oligomers. It demonstrates high efficacy in improving cognitive function in various rodent models of Alzheimer's disease. KHK6640 is applicable for research on neurological disorders such as Alzheimer's disease.

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.

BI-9787 is a zwitterionic inhibitor of ketohexokinase (KHK), demonstrating IC50 values of 12 nM for hKHK-A and 12.8 nM for hKHK-C. It exhibits good metabolic stability in rat hepatocytes and favorable pharmacokinetic properties in vivo in rats.

GS-1291269 is a potent neutral ketohexokinase (KHK) inhibitor, exhibiting IC50 values of 0.38 nM for KHK-C and 2.1 nM for KHK-A. In a rat fructose challenge model, GS-1291269 effectively reduces fructose-1-phosphate (F1P) levels in the liver and kidneys. It is applicable in the study of renal diseases and metabolic dysfunction-associated steatotic liver disease (MASLD).

(αR)-BI-9787 is the enantiomer of BI-9787. BI-9787 serves as an inhibitor of the zwitterionic ketohexokinase (KHK).