|Description||Hesperadin is an inhibitor of human Aurora B, which can prevent the phosphorylation of substrate with IC(50) of 40 nM. Growth of cultured bloodstream forms was also sensitive to Hesperadin (IC(50) of 50 nM). Hesperadin blocked nuclear division and cytokinesis but not other aspects of the cell cycle. Consequently, growth arrested cells accumulated multiple kinetoplasts, flagella and nucleoli, similar to the effects of RNAi-dependent knockdown of TbAUK1 in cultured bloodstream forms cells. Molecular models predicted high-affinity binding of Hesperadin to both conserved and novel sites in TbAUK1. Collectively, these data demonstrate that cell cycle progression is essential for infections with T. brucei and that parasite Aurora kinases can be targeted with small-molecule inhibitors.|
|Appearance||white solid powder|
Barasertib is an orally bioavailable, small-molecule, dihydrogen phosphate prodrug of the pyrazoloquinazoline Aurora kinase inhibitor AZD1152–hydroxyquinazolin...
SAR156497 is a selective Aurora A, B and C inhibitor with in vitro and in vivo efficacy IC50 value is 0.5 nM for Aurora A; 1.0 nM for Aurora B (incenp) and 3.0 ...
ENMD-2076 is an orally-active, Aurora A/angiogenic kinase inhibitor with a unique kinase selectivity profile and multiple mechanisms of action. ENMD-2076 has be...
ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM, 130 nM respectively, > 8 fold selectivity than Aurora C
AT-9283 is a broad spectrum kinase inhibitor that potently inhibits Aurora A, Aurora B, JAK2, JAK3, and c-ABL (IC50= 3, 3, 1.2, 1.1, and 4 nM, respectively). It...
Aurora A Inhibitor I
Aurora A Inhibitor I is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM. It is 1000-fold more selective for Aurora A than Aurora B.
SCH1473759 (HCl salt)
The hydrochloride salt form of SCH-1473759, a new sub-nanomolar Aurora A/B inhibitor which could result in cell death by inhibiting Aurora kinases. It is proved...
JNJ-7706621 is a novel cell cycle inhibitor that showed potent inhibition of several cyclin-dependent kinases (CDK) and Aurora kinases and selectively blocked p...
The Aurora kinases (A, B, and C) are a family of serine-threonine kinases that regulate various stages of mitotic function. With significant roles in cell cycle...
SCH-1473759 is a novel sub-nanomolar Aurora A/B inhibitor. SCH 1473759 was active against a large panel of tumor cell lines from different tissue origin and gen...
MK-5108 is a novel small molecule with potent inhibitory activity against Aurora-A kinase. Although most of the Aurora-kinase inhibitors target both Aurora-A an...
AMG 900 is a small-molecule inhibitor of Aurora kinases A, B and C with potential antineoplastic activity. Aurora kinase inhibitor AMG 900 selectively binds to ...
PHA-680632 is a is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM. PHA-680632 is also the first representative of a ...
GSK-1070916A is an ATP-competitive inhibitor of the serine/threonine kinases Aurora B and C with potential antineoplastic activity. Aurora B/C kinase inhibitor ...
PF-03814735 is an orally bioavailable, ATP-competitive, reversible small-molecule Aurora kinase inhibitor with potential antineoplastic activity. Aurora kinase ...
SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively. It is less potent to T...
AZD-1152HQPA is an active metabolite of Barasertib (AZD-1152), which is a novel acetanilide-substituted pyrazole-aminoquinazoline prodrug that is converted rap...
CCT129202 is an inhibitor of Aurora kinase activity and displays a favorable antineoplastic effect in preclinical studies. CCT129202 significantly reversed ABCB...
ENMD-2076 L-(+)-Tartaric acid
ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more selec...