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
- A4489 TC-A 2317 hydrochloride Potent Aurora kinase A inhibitor (Ki = 1.2 nM compared to 101 nM for inhibition of Aurora kinase B).
- A4488 Anacardic acid Noncompetitive inhibitor of histone acetyltransferase (HAT) activity in PCAF and p300 (IC50 values are ~5.0 and ~8.5 μM respectively). Inhibits NF-κB activation. Also reported to selectively activate Aurora kinase A-mediated phosphorylation of histone H3. Exhibits antitumor, antimicrobial and antioxidant activity.
- A3939 XL228 XL228 is a protein kinase inhibitor targeting IGF1R, the AURORA kinases, FGFR1-3, ABL and SRC family kinases.
- A3804 SCH-1473759 SCH-1473759
- 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 .
- A4128 PF-03814735 PF-03814735 is a potent, orally bioavailable, reversible inhibitor of both Aurora1 and Aurora2 kinases with IC50 values of 0.8nM and 5nM, respectively .
- A4127 GSK1070916 GSK1070916 is a potent and selective inhibitor of Aurora B/C Kinase with Ki values of 0.38nM and 1.5nM, respectively .
- A4125 CYC116 CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A.
- A4124 TAK-901 TAK-901 is a novel inhibitor of Aurora A/B with IC50 of 21 nM/15 nM.