Aurora Kinase

Choose Selective Aurora Kinase Inhibitors

Aurora Kinase Signaling Pathway Map

Aurora Kinase Signaling Pathways

Aurora Kinase Products

  • All (34)
  • Aurora Kinase Inhibitors (31)
  • Aurora Kinase Antibodies (2)
  • Aurora Kinase Antagonist (1)
  • New Aurora Kinase Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1048 Tozasertib (VX-680, MK-0457) Tozasertib (VX-680, MK-0457) 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.
Cancer Res, 2022, canres.1707.2021
Mol Oncol, 2022, 16(1):219-249
Toxicol Sci, 2022, kfac008
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.
Cancers (Basel), 2022, 14(6)1575
Cancer Cell, 2021, S1535-6108(21)00383-4
Nucleic Acids Res, 2021, gkab584
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.
Mol Oncol, 2022, 16(1):219-249
Cell Rep, 2021, 37(6):109783
Dev Cell, 2021, 56(9):1253-1267.e10
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. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.
Cancers (Basel), 2021, 13(6)1205
Life Sci Alliance, 2021, 4(8)e202101019
Mol Cell, 2020, 80(6):1104-1122.e9
S1133 Alisertib (MLN8237) Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3.
Cell Rep, 2022, 38(9):110448
Oncogene, 2022, 10.1038/s41388-022-02256-3
Pharmacol Res, 2022, 179:106209
S1134 AT9283 AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl1(T315I). Phase 2.
Sci Rep, 2022, 12(1):7
Mol Syst Biol, 2021, 17(9):e10426
Cancers (Basel), 2021, 13(6)1205
S1147 Barasertib (AZD1152-HQPA) 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.
Cancers (Basel), 2022, 14(6)1537
Biomed Pharmacother, 2022, 147:112645
Mol Oncol, 2022, 16(1):219-249
S1154 SNS-314 SNS-314 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 Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. Phase 1.
Cancers (Basel), 2021, 13(6)1205
Cancers (Basel), 2019, 11(2)
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
S1171 CYC116 CYC116 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. Phase 1.
Nat Genet, 2020, 52(4):408-417
Reprod Biomed Online, 2019, 10.1016/j.rbmo.2019.05.019
Biomol Ther (Seoul), 2019, 27(3):311-317
S1181 ENMD-2076 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 RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2.
Cell, 2021, 184(2):334-351.e20
Sci Adv, 2021, 7(4)eabd7851
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
S1249 JNJ-7706621 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 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.
Cancers (Basel), 2021, 13(6)1205
Gland Surg, 2020, 9(2):558-574
EMBO J, 2019, 38(19):e101704
S1272 XL228 XL228 is a protein kinase inhibitor with IC50 of 5 nM, 1.4 nM, 3.1 nM, 1.6 nM, 6.1 nM and 2 nM for wild-type ABL kinase, ABL T315I, Aurora A, IGF-1R, SRC and LYN, respectively.
S1451 Aurora A Inhibitor I (TC-S 7010) Aurora A Inhibitor I (TC-S 7010) is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B. Aurora A Inhibitor I (TC-S 7010) triggers apoptosis through the ROS-mediated UPR signaling pathway.
EMBO Rep, 2021, e52387
Cancer Lett, 2021, 509:89-104
Nat Commun, 2020, 11(1):1308
S1454 PHA-680632 PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2/3.
Front Cell Dev Biol, 2020, 8:590449
Mol Cancer Res, 2019, 17(1):20-29
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
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. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Cancer Cell, 2022, S1535-6108(21)00662-0
Oxid Med Cell Longev, 2022, 2022:2048095
Int J Biol Sci, 2022, 18(5):2047-2059
S1519 CCT129202 CCT129202 is an ATP-competitive pan-Aurora inhibitor for Aurora A, Aurora B and Aurora C with IC50 of 0.042 μM, 0.198 μM and 0.227 μM, respectively. It is less potent to FGFR3, GSK3β, PDGFRβ, etc.
Aging (Albany NY), 2020, 7;12(9):8221-8240
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
PLoS One, 2014, 9(7):e102741
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.
Toxicol Sci, 2022, kfac008
Hum Cell, 2022, 10.1007/s13577-022-00675-8
Cancer Cell, 2021, S1535-6108(21)00383-4
S2018 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 selective for Aurora A than Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.
S2158 KW-2449 KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR. Phase 1.
Cell Rep Med, 2022, 3(1):100492
Front Pharmacol, 2021, 12:740529
Cell, 2020, 182(3):685-712.e19
S2718 TAK-901 TAK-901 is a novel inhibitor of Aurora A/B with IC50 of 21 nM/15 nM. It is not a potent inhibitor of cellular JAK2, c-Src or Abl. Phase 1.
Sci Adv, 2021, 7(4)eabd7851
EBioMedicine, 2021, 64:103220
Sci Rep, 2021, 11(1):7259
S2719 AMG-900 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. It is >10-fold selective for Aurora kinases than p38α, Tyk2, JNK2, Met and Tie2. Phase 1.
Toxicol Sci, 2022, kfac008
PLoS Biol, 2021, 19(1):e3001029
Toxicol Sci, 2021, kfaa189
S2740 GSK1070916 GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex. Phase 1.
Cancer Cell, 2021, S1535-6108(21)00383-4
Cancer Res, 2020, canres.1693.2020
Cancer Res, 2019, 79(19):5088-5101
S2744 CCT137690 CCT137690 is a highly selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 15 nM, 25 nM and 19 nM. It has little effect on hERG ion-channel.
Cancer Cell, 2021, S1535-6108(21)00383-4
Autophagy, 2021, 10.1080/15548627.2021.2008692
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
S2770 MK-5108 (VX-689) 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. MK-5108 (VX-689) induces autophagy. Phase 1.
Cancer Cell, 2021, S1535-6108(21)00383-4
Adv Sci (Weinh), 2021, e2103360
Anal Chem, 2021, 93(30):10653-10660
S2931 Aurora Kinase Inhibitor III Aurora kinase inhibitor III is a potent inhibitor of Aurora A kinase with an IC50 of 42 nM and has high selectivity for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR (IC50s = 386, 3,550, 591, 1,980, 2,510, 887, and >10,000 nM, respectively).
S6214New H-1152 dihydrochloride H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.
S7065 MK-8745 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.
S7843 BI-847325 BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.
Sci Rep, 2021, 11(1):9161
Curr Protoc, 2021, 1(6):e180
Nature, 2019, 569(7757):509-513
S8699 SNS-314 Mesylate 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 and less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2.
Cancers (Basel), 2021, 13(6)1205
Front Pharmacol, 2020, 30;11:543
Neuron, 2018, 97(3):555-570
S8782 LY3295668 LY3295668 (AK-01) is a potent, orally active and specific inhibitor of Aurora A kinase with Ki of 0.8 nM and 1038 nM for AURKA and AURKB, respectively.
Kaohsiung J Med Sci, 2021, 10.1002/kjm2.12469
S9658 SP-96 SP-96 is a potent, selective and non-ATP-competitive inhibitor of Aurora B with IC50 of 0.316 nM. SP-96 can be used for the research of triple negative breast cancer (TNBC).
A5065 Aurora A Rabbit Recombinant mAb Aurora A Rabbit Recombinant mAb detects endogenous levels of total Aurora A.
A5118 Aurora B Rabbit Recombinant mAb Aurora B Rabbit Recombinant mAb detects endogenous levels of total Aurora B.
S7588 Reversine Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.
Nat Commun, 2021, 12(1):4789
Nat Methods, 2020, 17(3):279-282
J Cell Physiol, 2020, 235(3):2441-2451
S1048 Tozasertib (VX-680, MK-0457) Tozasertib (VX-680, MK-0457) 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.
Cancer Res, 2022, canres.1707.2021
Mol Oncol, 2022, 16(1):219-249
Toxicol Sci, 2022, kfac008
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.
Cancers (Basel), 2022, 14(6)1575
Cancer Cell, 2021, S1535-6108(21)00383-4
Nucleic Acids Res, 2021, gkab584
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.
Mol Oncol, 2022, 16(1):219-249
Cell Rep, 2021, 37(6):109783
Dev Cell, 2021, 56(9):1253-1267.e10
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. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.
Cancers (Basel), 2021, 13(6)1205
Life Sci Alliance, 2021, 4(8)e202101019
Mol Cell, 2020, 80(6):1104-1122.e9
S1133 Alisertib (MLN8237) Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3.
Cell Rep, 2022, 38(9):110448
Oncogene, 2022, 10.1038/s41388-022-02256-3
Pharmacol Res, 2022, 179:106209
S1134 AT9283 AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl1(T315I). Phase 2.
Sci Rep, 2022, 12(1):7
Mol Syst Biol, 2021, 17(9):e10426
Cancers (Basel), 2021, 13(6)1205
S1147 Barasertib (AZD1152-HQPA) 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.
Cancers (Basel), 2022, 14(6)1537
Biomed Pharmacother, 2022, 147:112645
Mol Oncol, 2022, 16(1):219-249
S1154 SNS-314 SNS-314 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 Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. Phase 1.
Cancers (Basel), 2021, 13(6)1205
Cancers (Basel), 2019, 11(2)
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
S1171 CYC116 CYC116 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. Phase 1.
Nat Genet, 2020, 52(4):408-417
Reprod Biomed Online, 2019, 10.1016/j.rbmo.2019.05.019
Biomol Ther (Seoul), 2019, 27(3):311-317
S1181 ENMD-2076 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 RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2.
Cell, 2021, 184(2):334-351.e20
Sci Adv, 2021, 7(4)eabd7851
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
S1249 JNJ-7706621 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 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.
Cancers (Basel), 2021, 13(6)1205
Gland Surg, 2020, 9(2):558-574
EMBO J, 2019, 38(19):e101704
S1272 XL228 XL228 is a protein kinase inhibitor with IC50 of 5 nM, 1.4 nM, 3.1 nM, 1.6 nM, 6.1 nM and 2 nM for wild-type ABL kinase, ABL T315I, Aurora A, IGF-1R, SRC and LYN, respectively.
S1451 Aurora A Inhibitor I (TC-S 7010) Aurora A Inhibitor I (TC-S 7010) is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B. Aurora A Inhibitor I (TC-S 7010) triggers apoptosis through the ROS-mediated UPR signaling pathway.
EMBO Rep, 2021, e52387
Cancer Lett, 2021, 509:89-104
Nat Commun, 2020, 11(1):1308
S1454 PHA-680632 PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2/3.
Front Cell Dev Biol, 2020, 8:590449
Mol Cancer Res, 2019, 17(1):20-29
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
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. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Cancer Cell, 2022, S1535-6108(21)00662-0
Oxid Med Cell Longev, 2022, 2022:2048095
Int J Biol Sci, 2022, 18(5):2047-2059
S1519 CCT129202 CCT129202 is an ATP-competitive pan-Aurora inhibitor for Aurora A, Aurora B and Aurora C with IC50 of 0.042 μM, 0.198 μM and 0.227 μM, respectively. It is less potent to FGFR3, GSK3β, PDGFRβ, etc.
Aging (Albany NY), 2020, 7;12(9):8221-8240
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
PLoS One, 2014, 9(7):e102741
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.
Toxicol Sci, 2022, kfac008
Hum Cell, 2022, 10.1007/s13577-022-00675-8
Cancer Cell, 2021, S1535-6108(21)00383-4
S2018 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 selective for Aurora A than Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.
S2158 KW-2449 KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR. Phase 1.
Cell Rep Med, 2022, 3(1):100492
Front Pharmacol, 2021, 12:740529
Cell, 2020, 182(3):685-712.e19
S2718 TAK-901 TAK-901 is a novel inhibitor of Aurora A/B with IC50 of 21 nM/15 nM. It is not a potent inhibitor of cellular JAK2, c-Src or Abl. Phase 1.
Sci Adv, 2021, 7(4)eabd7851
EBioMedicine, 2021, 64:103220
Sci Rep, 2021, 11(1):7259
S2719 AMG-900 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. It is >10-fold selective for Aurora kinases than p38α, Tyk2, JNK2, Met and Tie2. Phase 1.
Toxicol Sci, 2022, kfac008
PLoS Biol, 2021, 19(1):e3001029
Toxicol Sci, 2021, kfaa189
S2740 GSK1070916 GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex. Phase 1.
Cancer Cell, 2021, S1535-6108(21)00383-4
Cancer Res, 2020, canres.1693.2020
Cancer Res, 2019, 79(19):5088-5101
S2744 CCT137690 CCT137690 is a highly selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 15 nM, 25 nM and 19 nM. It has little effect on hERG ion-channel.
Cancer Cell, 2021, S1535-6108(21)00383-4
Autophagy, 2021, 10.1080/15548627.2021.2008692
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
S2770 MK-5108 (VX-689) 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. MK-5108 (VX-689) induces autophagy. Phase 1.
Cancer Cell, 2021, S1535-6108(21)00383-4
Adv Sci (Weinh), 2021, e2103360
Anal Chem, 2021, 93(30):10653-10660
S2931 Aurora Kinase Inhibitor III Aurora kinase inhibitor III is a potent inhibitor of Aurora A kinase with an IC50 of 42 nM and has high selectivity for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR (IC50s = 386, 3,550, 591, 1,980, 2,510, 887, and >10,000 nM, respectively).
S6214New H-1152 dihydrochloride H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.
S7065 MK-8745 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.
S7843 BI-847325 BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.
Sci Rep, 2021, 11(1):9161
Curr Protoc, 2021, 1(6):e180
Nature, 2019, 569(7757):509-513
S8699 SNS-314 Mesylate 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 and less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2.
Cancers (Basel), 2021, 13(6)1205
Front Pharmacol, 2020, 30;11:543
Neuron, 2018, 97(3):555-570
S8782 LY3295668 LY3295668 (AK-01) is a potent, orally active and specific inhibitor of Aurora A kinase with Ki of 0.8 nM and 1038 nM for AURKA and AURKB, respectively.
Kaohsiung J Med Sci, 2021, 10.1002/kjm2.12469
S9658 SP-96 SP-96 is a potent, selective and non-ATP-competitive inhibitor of Aurora B with IC50 of 0.316 nM. SP-96 can be used for the research of triple negative breast cancer (TNBC).
A5065 Aurora A Rabbit Recombinant mAb Aurora A Rabbit Recombinant mAb detects endogenous levels of total Aurora A.
A5118 Aurora B Rabbit Recombinant mAb Aurora B Rabbit Recombinant mAb detects endogenous levels of total Aurora B.
S7588 Reversine Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.
Nat Commun, 2021, 12(1):4789
Nat Methods, 2020, 17(3):279-282
J Cell Physiol, 2020, 235(3):2441-2451
S6214New H-1152 dihydrochloride H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.
Tags: Aurora Kinase inhibition | Aurora Kinase cancer | Aurora A activation | Aurora A phosphorylation | Aurora B phosphorylation | Aurora B activation | Aurora Kinase assay | Aurora Kinase pathway | Aurora A and ic50 | Aurora Kinase inhibitors ic50 | Aurora Kinase inhibitor clinical trial | Aurora Kinase inhibitors as anticancer agents | Aurora Kinase inhibitor review