Hesperadin – 10 mg

Brand:
Cayman
CAS:
422513-13-1
Storage:
-20
UN-No:
Non-Hazardous - /

Hesperadin is a multi-kinase inhibitor.{42010,42011,18314} It inhibits human Aurora kinase B (IC50 = 250 nM) and its T. brucei homolog Aurora kinase-1 (IC50 = 40 nM) in in vitro kinase assays.{42010,42011} Hesperadin (1 µM) inhibits AMPK, LCK, MKK1, MAPKAP-K1, CHK1, and PHK in a panel of 25 kinases.{42010} It also inhibits MEKK2 in ATPase and transphosphorylation assays with IC50s of 60 and 34 nM, respectively.{18314} Hesperadin (50-100 nM) induces polyploidy and defects in cytokinesis and spindle assembly as well as inhibits proliferation of HeLa cells and overrides mitotic arrest induced by paclitaxel (Item No. 10461) or monastrol (Item No. 15044).{42010} Hesperadin also induces toxicity in HepG2 cells with a toxic concentration (TC50) value of less than 0.2 µM.{42013} It inhibits replication of clinical isolates of influenza A and B viruses with EC50s ranging from 0.22 to 2.21 µM in a plaque formation assay.{42012} Hesperadin inhibits the growth of T. brucei, L. major promastigotes and amastigotes, and P. falciparum with EC50 values ranging from 0.01 to 2.37 µM, but has less activity against T. cruzi (EC50 = 39 µM).{42013}  

 

Available on backorder

SKU: 24199 - 10 mg Category:

Description

A multi-kinase inhibitor; inhibits human Aurora kinase B (IC50 = 250 nM) and the T. brucei homolog Aurora kinase-1 (IC50 = 40 nM); inhibits AMPK, LCK, MKK1, MAPKAP-K1, CHK1, and PHK in a panel of 25 kinases at 1 µM; inhibits MEKK2 in ATPase and transphosphorylation assays (IC50s = 60 and 34 nM, respectively); induces polyploidy and defects in cytokinesis and spindle assembly as well as inhibits proliferation of HeLa cells and overrides paclitaxel- and monastrol-induced mitotic arrest from 50-100 nM; induces toxicity in HepG2 cells (TC50 = 50 = 0.22-2.21 µM); inhibits the growth of T. brucei, L. major promastigotes and amasigotes, and P. falciparum (EC50s = 0.01-2.37 µM),


Formal name: N-[2,3-dihydro-2-oxo-3-[(3Z)-phenyl[[4-(1-piperidinylmethyl)phenyl]amino]methylene]-1H-indol-5-yl]-ethanesulfonamide

Synonyms: 

Molecular weight: 516.7

CAS: 422513-13-1

Purity: ≥98%

Formulation: A crystalline solid


Product Type|Biochemicals|Antiparasitics|Antiprotozoals||Product Type|Biochemicals|Antivirals||Product Type|Biochemicals|Kinase Inhibitors|Aurora||Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death||Research Area|Cancer|Cell Signaling|Aurora Signaling||Research Area|Cell Biology|Cell Signaling|ERK/MAPK Signaling||Research Area|Cell Biology|Cytoskeleton & Motor Proteins||Research Area|Endocrinology & Metabolism|Nutrient Sensing||Research Area|Immunology & Inflammation||Research Area|Infectious Disease|Parasitic Diseases|African Sleeping Sickness||Research Area|Infectious Disease|Parasitic Diseases|Chagas Disease||Research Area|Infectious Disease|Parasitic Diseases|Malaria||Research Area|Infectious Disease|Viral Diseases|Influenza