Ofirnoflastum

Overview

Ofirnoflastum (Ofirnoflast) is an orally active first-in-class allosteric NEK7 inhibitor with an IC 50 of 46 nM. Ofirnoflastum binds an allosteric site adjacent to NEK7’s ATP-binding pocket, induces conformational shifts, disrupts NEK7- NLRP3 binding, blocks NLRP3 inflammasome assembly, spares NEK7’s physiological functions, and suppresses caspase-1 , caspase-8 , NF-κB , and TNF activity. Ofirnoflastum reduces pro-inflammatory cytokine production, suppresses ASC specks, IL-1β release, pyroptotic cell death, and leukemic burden, induces apoptosis and erythroid differentiation, restores hematopoiesis, and improves outcomes in colitis models. Ofirnoflastum can be used for the research of myelodysplastic syndromes, chronic myelomonocytic leukemia, and acute myeloid leukemia.

Application

Products | Products > Disease Areas > Cancer | Products > Disease Areas > Blood or Cardio-cerebrovascular Disease | Products > Disease Areas > Inflammation or Immune System Disease | Products > Disease Areas > Leukemia/Lymphoma/Myeloma | Products > Disease Areas > Blood Disease | Products > Disease Areas > Acute Myeloid Leukemia | Products > Disease Areas > Myelodysplastic Syndrome | Products > Signaling Pathways > Cell Cycle/DNA Damage | Products > Signaling Pathways > Immunology/Inflammation | Products > Signaling Pathways > Apoptosis | Products > Signaling Pathways > NF-κB | Products > Research Areas > Inflammation/Immunology | Products > Research Areas > Cardiovascular Disease | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Immunotherapy | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Signaling Pathways > Pyroptosis | Products > Signaling Pathways > NF-κB | Products > Signaling Pathways > NEKs | Products > Signaling Pathways > NOD-like Receptor (NLR) | Products > Signaling Pathways > Caspase | Products > Signaling Pathways > Apoptosis

Product Information

• Catalog No.: HY-159520
• CAS No.: 2731294-23-6
• Molecular Formula: C23H19F4N7O2
• Molecular Weight: 501.44
• Purity: 99.93%
• Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
• Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution
• Availability: In-stock

Source

Original product source