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Aurora Kinase Inhibitors

Aurora kinases are serine/threonine kinases which play the key role in cell prefabrication. The Aurora protein kinase family, including Aurora A, Aurora B and Aurora C, is associated to the stability of chromosome. Aurora A which plays a crucial role in each step of mitosis is expressed widely in proliferating normal tissues. Aurora A interacts with transforming acid coiled-coil (TACC) proteins to regulate the maturation of centrosomes. Aurora A also interacts Ajuba, a LIM protein, to regulate mitotic entry by recruiting the cyclin B1/CDK1 complex to the centrosome. Aberrant expression of aurora A has been found in various tumor types. Aurora A interacts with and inactivates the tumor suppressor p53, facilitating MDM-2-mediated degradation of p53 in cancer cell lines. Aurora B kinase, a chromosome passenger protein which comprises inner centrosome protein (INCENP) and survivin, is overexpressed in a variety of human cancers. The few available studies found that Aurora C was overexpressed in colorectal, breast, and prostate cancers.

Other Cell Cycle Related Inhibitors

CDK ROCK Wee1 Chk PLK APC MPS1 Rho Myc DYRK

Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
S1529 Hesperadin Hesperadin potently inhibits Aurora B with IC50 of 250 nM in a cell-free assay. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo.
Nat Commun, 2026, 17(1)2284
Int J Mol Sci, 2026, 27(6)2627
Nat Cell Biol, 2025, 27(1):59-72
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S1147 Barasertib-HQPA (AZD2811) Defosbarasertib (AZD1152-HQPA, AZD2811, INH-34, Barasertib-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1.
Genome Biol, 2026, 27(1)125
Nat Commun, 2025, 16(1):1583
Cell Rep Med, 2025, 6(2):101964
Verified customer review of Barasertib-HQPA (AZD2811)
S1133 Alisertib (MLN8237) Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay, and it has >200-fold higher selectivity for Aurora A than Aurora B. This compound induces cell cycle arrest, apoptosis and autophagy. Phase 3.
EMBO Mol Med, 2026, 10.1038/s44321-026-00437-1
Cancer Lett, 2026, 646:218435
Int J Nanomedicine, 2026, 21:443375
Verified customer review of Alisertib (MLN8237)
S1460 SP600125 SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. This compound is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase A，FLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. It inhibits autophagy and activates apoptosis.
Research (Wash D C), 2026, 9:1190
Anal Chem, 2026, 98(10):7247-7261
iScience, 2026, 29(5):115396
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S1249 JNJ-7706621 JNJ-7706621 is a 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 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.
Cell Rep Med, 2025, S2666-3791(25)00231-9
EMBO Rep, 2025, 10.1038/s44319-025-00573-8
Adv Biol Regul, 2025, 95:101072
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S1048 Tozasertib (VX-680, MK-0457) Tozasertib (VX-680) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and BCR-ABL tyrosine kinase, which are inhibited by the Tozasertib with both Ki of 30 nM. Tozasertib induces apoptosis and autophagy. Phase 2.
bioRxiv, 2026, 2026.01.11.698900
ACS Appl Bio Mater, 2026, 9(8):3753-3767
Cell Rep Med, 2025, S2666-3791(25)00102-8
Verified customer review of Tozasertib (VX-680, MK-0457)
S1103 ZM 447439 ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc.
Cell Metab, 2025, S1550-4131(25)00334-1
Cell Rep, 2025, 44(2):115238
Diabetologia, 2025, 68(9):1997-2010
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S1100 MLN8054 MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM in Sf9 insect cell. It is more than 40-fold selective for Aurora A than Aurora B. Phase 1.
Molecular Cancer Therapeutics, September 28, 2018, 2575-2585
Nature Communications, March 31, 2016, 11117
Cell Cycle, July 9, 2013, 2598-2607
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S1107 Danusertib (PHA-739358) Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. It induces apoptosis, cell cycle arrest, and autophagy. This compound is in Phase 2.
Elife, 2024, 12RP92324
Sci Rep, 2024, 14(1):4303
Environ Mol Mutagen, 2024, 10.1002/em.22604
Verified customer review of Danusertib (PHA-739358)
S2770 MK-5108 MK-5108 (VX-689) is a highly selective Aurora A inhibitor with IC50 of 0.064 nM in a cell-free assay and is 220- and 190-fold more selective for Aurora A than Aurora B/C, while it inhibits TrkA with less than 100-fold selectivity. This compound induces autophagy. Phase 1.
Molecular Cancer Therapeutics, September 2017, 1934-1941
Apoptosis, October 2018, 492-511
Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
Verified customer review of MK-5108

Signaling Pathway Map