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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
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.
Nat Commun, 2025, 16(1):7832
EMBO J, 2025, 10.1038/s44318-025-00564-4
J Immunother Cancer, 2025, 13(1)e009316
Verified customer review of Alisertib (MLN8237)
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.
Nat Commun, 2025, 16(1):1583
Cell Rep Med, 2025, 6(2):101964
Cell Rep, 2025, 44(2):115238
Verified customer review of Barasertib-HQPA (AZD2811)
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 this compound does not inhibit MKK1 activity in vivo.
Nat Cell Biol, 2025, 27(1):59-72
Nat Commun, 2025, 16(1):2277
Int J Biol Macromol, 2025, 292:139119
Verified customer review of Hesperadin
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.
Nat Commun, 2025, 16(1):7156
Adv Sci (Weinh), 2025, 12(28):e2502634
Adv Sci (Weinh), 2025, 12(36):e00028
Verified customer review of SP600125
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
Verified customer review of JNJ-7706621
S1048 Tozasertib (VX-680) 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 this compound with both Ki of 30 nM. It induces apoptosis and autophagy, and is in Phase 2.
Cell Rep Med, 2025, S2666-3791(25)00102-8
Biochim Biophys Acta Mol Cell Res, 2025, 1872(7):120001
Cell Death Dis, 2024, 15(1):56
Verified customer review of Tozasertib (VX-680)
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
Verified customer review of ZM 447439
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.
Nat Commun, 2024, 15(1):1041
Nat Commun, 2023, 14(1):5317
Mol Biol Cell, 2023, 34(5):ar47
Verified customer review of MLN8054
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.
Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
Sci Rep, 2024, 14(1):4303
bioRxiv, 2023, 10.1101/2023.08.08.552464
Verified customer review of MK-5108

Signaling Pathway Map