Aurora B Selective Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S1147 Barasertib (AZD1152-HQPA)

Barasertib (AZD1152-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM, ~3700 fold more selective for Aurora B over Aurora A. Phase 1.

Selective Aurora B, IC50: 0.37 nM
S1529 Hesperadin

Hesperadin potently inhibits Aurora B with IC50 of 250 nM. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo.

Selective Aurora B (human), IC50: 250 nM
S1134 AT9283

AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM; also potent to Aurora A/B, Abl(T315I). Phase 2.

Pan Aurora B, IC50: ~3.0 nM
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.

Pan Aurora B-INCENP, IC50: 3.5 nM
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.

Pan Aurora B, IC50: 4 nM
S2725 PF-03814735

PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.

Pan Aurora B, IC50: 5 nM
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.

Pan Aurora B, Ki: 9 nM
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.

Pan Aurora B, IC50: 13 nM
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. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.

Pan Aurora B, IC50: 15 nM
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.

Pan Aurora B-INCENP, IC50: 15 nM
S1048 VX-680 (Tozasertib, MK-0457)

VX-680 (Tozasertib, MK-0457) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. Phase 2.

Pan Aurora B, Ki app: 18 nM
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.

Pan Aurora B, IC50: 25 nM
S1154 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. It is less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. Phase 1.

Pan Aurora B, IC50: 31 nM
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, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2.

Pan Aurora B, IC50: 79 nM
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.

Pan Aurora B, IC50: 130 nM
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.

Pan Aurora B, IC50: 135 nM
S1100 MLN8054

MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM. It is more than 40-fold selective for Aurora A than Aurora B. Phase 1.

Pan Aurora B, IC50: 172 nM
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.

Pan Aurora B, IC50: 198 nM
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.

Pan Aurora B, IC50: 280 nM
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.

Pan Aurora B, IC50: 350 nM
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 VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.

Pan Aurora B, IC50: 350 nM
S1133 Alisertib (MLN8237)

Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM. It has >200-fold higher selectivity for Aurora A than Aurora B. Phase 3.

Pan Aurora B, IC50: 396.5 nM
S1451 Aurora A Inhibitor I

Aurora 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.

Pan Aurora B, IC50: 3.4 μM