Search results for: 'research-area pi3k-akt-signaling s6-kinase'
- HesperadinCatalog No. :A4118Aurora B kinase inhibitorHersperadin is an ATP-competitive small molecule inhibitor of Aurora B kinase, which is one of the three Aurora family kinases involved in the regulation of cell division, with half maximal inhibitory concentration IC50 of 250 nM, where the sulphonamide group of hersperadin inserts into the ATP-pocket in the catalytic cleft of Aurora B kinase and extends into the adjacent hydrophobic pocket. Hersperadin has been found to prevent the phosphorylation of Aurora B, where the Ser-10 phosphorylation of Aurora B in mitosis serves as a biomarker for mitotic progression, with IC50 of 40 nM leading to inhibition of chromosome alignment and segregation.
- CYC116Catalog No. :A4125Potent Aurora A/B inhibitorCYC116 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.
- Barasertib (AZD1152-HQPA)Catalog No. :A4112Aurora Kinase B inhibitor, Potent and selectiveBarasertib, 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.
- Aurora A Inhibitor ICatalog No. :A4126Aurora A inhibitorAurora 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.
- PHA-680632Catalog No. :A4122Aurora kinase inhibitor,novel and potentPHA-680632 is a novel and potent inhibitor of Aurora kinases, a small family of serine/threonine kinases regulating mitosis in chromosome segregation and cell division, that inhibits the activity of all three Aurora kinases with 50% inhibition concentration IC50 values of 27 nM, 135 nM and 120 nM for Aurora A, B and C kinases respectively.
- TC-A 2317 hydrochlorideCatalog No. :A4489Aurora kinase A inhibitor,potent and selectivePotent Aurora kinase A inhibitor (Ki = 1.2 nM compared to 101 nM for inhibition of Aurora kinase B).
- JNJ-7706621Catalog No. :A4115Potent CDK/Aurora kinase inhibitor
JNJ-7706621 is a dual inhibitor of cyclin-dependent kinases (CDK) and Aurora kinases that potently inhibits CDK1, CDK2, CDK3, CDK4, CDK6, Aurora-A, and Aurora-B in vitro with 50% inhibition concentration IC50 values of 0.009, 0.004, 0.003, 0.058, 0.253, 0.175, 0.011 and 0.015 μmol/L respectively.
- MLN8054Catalog No. :A4114Aurora A inhibitorMLN8054 is a potent of Aurora A kinase (AAK) inhibitor consisting of a benzazepine core scaffold with a fused amino pyrimidine and an aryl carboxylic acid which represents an unprecedented kinase inhibitor framework.
- AZD1152Catalog No. :A3214Aurora B kinase inhibitor,highly potent and selective
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 .
- PF-03814735Catalog No. :A4128Aurora A/B inhibitorPF-03814735 is a potent, orally bioavailable, reversible inhibitor of both Aurora1 and Aurora2 kinases with IC50 values of 0.8nM and 5nM, respectively .