Signaling Pathway

Aurora Kinase

Aurora Kinase

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Aurora kinases are serine/threonine kinases that are essential for cell proliferation. Aurora kinase helps the dividing cell dispense its genetic materials to its daughter cells. More specifically, Aurora kinases play a crucial role in cellular division by controlling chromatid segregation. Defects in this segregation can cause genetic instability, a condition which is highly associated with tumorigenesis. Three Aurora kinases have been identified in mammalian cells to date, Aurora A, Aurora B, Aurora C. Besides being implicated as mitotic regulators, these three kinases have generated significant interest in the cancer research field due to their elevated expression profiles in many human cancers. The human Aurora kinases present a similar domain organization, with a N-terminal domain of 39 to 129 residues in length, a protein kinase domain and a short C-terminal domain containing 15 to 20 residues. The N-terminal domain of three proteins share low sequence conservation, which determines selectivity during protein-protein interactions.

Aurora Kinase Inhibitors & Modulators (28)

Product Name Catalog No. Brief Description
Alisertib

HY-10971

Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM; has >200-fold higher selectivity for Aurora A than Aurora B.

AMG 900

HY-13253

AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A/B/C with IC50 of 5 nM/4 nM /1 nM;  >10-fold selective for Aurora kinases than p38α, Tyk2, JNK2, Met and Tie2.

AT9283

HY-50514

AT9283 is a small molecule a multi-targeted inhibitor with IC50s of 4, 1.2, 1.1 and approximate 3 nM for Bcr-Abl(T3151), JAK2 and JAK3, Aurora A and Aurora B, respectively.

Aurora A inhibitor I

HY-70061

Aurora A inhibitor I is a selective Aurora A inhibitor (Aurora A: IC50=0.0034 μM; Aurora B IC50=3.4 μM), (B/A ratio=1000).

AZD1152

HY-10127

AZD1152 (barasertib),  pro-drug of barasertib-hQPA(HY-10126), is a selective Aurora B kinase inhibitor, AZD1152 inhibited the proliferation various types of human leukemia cells with an IC50 ranging from 3 nM to 40 nM.

AZD1152-HQPA

HY-10126

AZD1152-HQPA is the active metabolite of AZD-1152, AZD1152-HQPA (Barasertib) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM, ~100 fold more selective for Aurora B over Aurora A.

CCT 137690

HY-10804

CCT 137690 is a potent inhibitor of Aurora kinases (IC50 values are 0.015, 0.019 and 0.025 μM at Aurora A, Aurora C and Aurora B respectively).

CCT129202

HY-12049

CCT129202 is a Aurora kinase inhibitor with IC50 of 0.042 ± 0.022, 0.198 ± 0.05, and 0.227 ± 0.064 μmol/L for Aurora A, Aurora B, and Aurora C, respectively.

CYC-116

HY-10558

CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM.

Danusertib

HY-10179

Danusertib (PHA-739358) is a pyrrolo-pyrazole and small molecule Aurora kinases inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively.

ENMD-2076

HY-10987A

ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα.

ENMD-2076 Tartrate

HY-10987

ENMD-2076 tartrate has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα.

GSK-1070916

HY-70044

GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM; displays >100-fold selectivity against the closely related Aurora A-TPX2 complex(IC50=490 nM).

Hesperadin

HY-12054

Hesperadin is a ATP-competitive inhibitor of Aurora B kinase with IC50 of  250 nM.

JNJ-7706621

HY-10329

JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6; also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.

MK-5108

HY-13252

MK-5108 (VX-689) is a highly selective Aurora A inhibitor with IC50 of 0.064 nM; 220- and 190-fold more selective for Aurora A than Aurora B/C.

MK-8745

HY-13819

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.

MLN8054

HY-10180

MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM; exhibits more than 40-fold selective for Aurora A than Aurora B.

PF-03814735

HY-14574

PF-03814735 is a novel, potent, orally bioavailable, reversible small-molecule Aurora kinase inhibitor with IC50 of 0.8, 5, 10 and 22 nM for Aurora A, Aurora B, Flt 1 and FAk, respectively.

PHA-680632

HY-10178

PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively.