Aurora kinases are a family of serine-threonine kinases of three highly homologous members, including aurora A kinase, aurora B kinase and aurora C kinase, which are responsible for chromosome assembly and segregation during mitosis. Aurora kinases are characterized by two domains: a regulatory domain in the NH2 terminus and a catalytic domain in the COOH terminus, in which an A-Box and a D-Box found correspondingly in each domain are responsible for protein degradation. Aurora A kinase plays an important role in centrosome function and duplication, mitotic entry and bipolar spindle assembly; while Aurora B kinase is the catalytic component of the chromosomal passenger complex regulating the accurate segregation of the chromatids at mitosis, histone modification and cytokinesis. Aurora C kinase is less studied and expressed restrictedly in the testes.
- Cat.No. Product Name Information
- A8807 MK-8745 MK-8745 is a potent and selective Aurora A inhibitor with IC50 of 0.6 nM, more than 450-fold selectivity for Aurora A over Aurora B.
- A3760 Reversine Reversine, a small synthetic purine analogue (2,6-disubstituted purine), has been shown to be effective in tumor suppression. These effects of reversine are due to the inhibition of Aurora A and B.
- A3214 AZD1152 AZD1152 is a highly selective inhibitor of Aurora kinases with IC50 values of 1.37 μM and 0.37 nM for Aurora A and Aurora B, respectively .
- A4113 ZM 447439 ZM 447439 is a novel, potent and selective inhibitor of Aurora kinase, a family of serine/threonine kinases essential for accurate chromosome segregation during cell division, that inhibits the activity of purified recombinant Aurora A and Aurora B proteins in vitro with 50% inhibition concentration IC50 values of 110 nM and 130 nM respectively and hence inhibits phosphorylation of histone H3 on serine 10.
- A4112 Barasertib (AZD1152-HQPA) Barasertib, previously known as AZD1152-hydroxyquinazoline pyrazol anilide (HQPA), is a potent aurora kinase inhibitor, which is resulted from rapid phosphatase-mediated cleavage of the precursor, AZD1152, in serum following parenteral administration in vivo.
- A4111 VX-680 (MK-0457,Tozasertib) VX-680 (also known as MK-0457 or tozasertib), discovered through a molecular screening campaign, is a potent inhibitor of pan-aurora kinase as well as other kinases including Src, GSK3β, Flt3, JAK2, BCR-Abl (wild type) and BCR-Abl (T315I mutant).
The orally bioavailable agent, MLN8237 (also known as alisertib), is a potent small-molecule inhibitor of Aurora A kinase (AAK) which is overexpressed in several types of tumor and associated with oncogenesis and tumor progression.
- C3823 Phthalazinone pyrazole
- B6014 BI-847325
- A4489 TC-A 2317 hydrochloride Potent Aurora kinase A inhibitor (Ki = 1.2 nM compared to 101 nM for inhibition of Aurora kinase B).