Aurora Kinase
Catalog No. | Inhibitor Name | Aurora A | Aurora B | Aurora C | Other |
---|---|---|---|---|---|
A10004 | Alisertib | **** | * | ||
A10981 | Tozasertib | **** | ** | *** | Bcr-Abl,FLT3 |
A10109 | Barasertib | * | **** | ||
A11009 | ZM 447439 | ** | * | LCK,Src,MEK1 | |
A10601 | MLN8054 | **** | * | LCK,PKA,CK2 | |
A10715 | Danusertib | *** | ** | ** | Abl,TrkA,RET |
A10095 | AT9283 | **** | **** | JAK3,JAK2,Abl1 (T315I) | |
A10494 | JNJ-7706621 | *** | *** | CDK2/CyclinE,CDK2/CyclinA,CDK1/CyclinB | |
A10448 | Hesperadin | * | TbAUK1 | ||
A10100 | Aurora A Inhibitor I | **** | * | * | |
A10508 | KW-2449 | ** | FLT3 (D835Y),Abl (T315I),FLT3 | ||
A10851 | SNS-314 Mesylate | *** | ** | **** | |
A10352 | ENMD-2076 | *** | * | FLT3,RET,VEGFR3/FLT4 | |
A10714 | PHA-680632 | ** | * | * | FGFR1,PLK1,FLT3 |
A11410 | MK-5108 | **** | |||
A10248 | CYC116 | *** | *** | VEGFR2,FLT3,CDK2/CyclinE | |
A11066 | AMG-900 | *** | **** | **** | p38α,TYK2,JNK2 |
A11171 | PF-03814735 | **** | *** | FLT1,FAK,TrkA | |
A10184 | CCT129202 | ** | * | * | |
A11168 | GSK1070916 | * | **** | *** | FLT1,Tie-2,SIK |
A11067 | TAK-901 | ** | *** | JAK3,c-Src,YES1 | |
A11081 | CCT137690 | *** | ** | ** | |
A13396 | MK-8745 | **** | * | ||
A10352 | ENMD-2076 L-(*)-Tartaric acid | *** | * | FLT3,RET,VEGFR3/FLT4 | |
A15762 | BI-847325 | ** | **** | *** | |
A13250 | Reversine | *** | *** | ** | human A3 adenosine receptor |
Notes:
1.Hover mouse over " " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
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Hesperadin
Catalog No. A10448 Aurora B Kinase inhibitorHesperadin is a human Aurora B inhibitor with an IC50 of 40 nM for the prevention of the phosphorylation of substrate. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo. Learn More -
BI-847325
Catalog No. A15762 MEK/Aurora InhibitorBI-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. Learn More -
AZD1152
Catalog No. A15011 Aurora B inhibitorAZD1152 is a pro-drug that rapidly undergoes phosphatase-mediated cleavage in serum to release barasertib-hQPA, a selective Aurora B kinase inhibitor that has shown preliminary activity in clinical studies of patients with acute myeloid leukemia (AML). Learn More -
SAR156497
Catalog No. A14382 Aurora Kinase inhibitorSAR156497 is an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy with IC50 = 0.5 nM (Aurora A), 1 nM (Aurora B / incenp), 3 nM (Aurora C / incenp) respectively SAR156497 combines high in vitro potency with satisfactory metabolic stability and limited CYP3A4 and PDE3 inhibition. Learn More -
MK-8745
Catalog No. A13396 Aurora Kinase A InhibitorMK-8745 is a novel Aurora-A specific inhibitor. It induces apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lineages. Learn More -
Reversine
Catalog No. A13250 human A3 adenosine receptor antagonist /Aurora inhibitorReversine 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. Learn More -
CYC116 (CYC-116)
Catalog No. A10248 Aurora Kinase inhibitorAurora kinase/VEGFR 2 inhibitor CYC116 inhibits Aurora kinases A and B and vascular endothelial growth factor receptor 2 (VEGFR2), resulting in disruption of the cell cycle, rapid cell death, and the inhibition of angiogenesis. Learn More -
ZM-447439
Catalog No. A11009 Aurora Kinase inhibitorZM 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. Learn More -
SNS-314
Catalog No. A10851 Aurora inhibitorSNS-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. Learn More -
MK-5108 (VX-689)
Catalog No. A11410 Aurora A Kinase inhibitorMK-5108, also known as VX-689, is a competitive inhibitor of the ATP-binding site of aurora A kinase. Learn More -
PHA-680632
Catalog No. A10714 Aurora inhibitorPHA-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. Learn More -
PF-03814735
Catalog No. A11171 Aurora A/B Kinase inhibitorPF-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. Learn More -
GSK1070916
Catalog No. A11168 Aurora Kinase B/C inhibitorGSK1070916 is a potent Aurora B/C kinase inhibitor (with IC50 of 3.5 nM/6.5 nM) with broad antitumor activity in tissue culture cells and human tumor xenograft models.
Learn More -
CCT129202
Catalog No. A10184 Aurora InhibitorCCT129202 is a representative of a structurally novel series of imidazopyridine small-molecule inhibitors of Aurora kinase activity. It shows high selectivity for the Aurora kinases over a panel of other kinases tested and inhibits proliferation in multiple cultured human tumor cell lines.
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CCT137690
Catalog No. A11081 Aurora Kinase inhibitorCCT137690 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. Learn More -
MLN8237 (Alisertib)
Catalog No. A10004 Aurora A Kinase inhibitorMLN8237 (Alisertib) 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. Phase 3.. Learn More -
AT9283
Catalog No. A10095 Aurora/JAK inhibitorAT9283 inhibits aurora kinase A and B and targets other tyrosine and serine/threonine kinases associated with myeloid cell proliferation. Learn More -
AZD1152-HQPA (Barasertib)
Catalog No. A10109 Aurora Kinase B inhibitorAZD 1152-HQPA is a highly potent and selective inhibitor of Aurora B, with Ki values to be 0.36 (Aurora B) and 1369 nM (Aurora A) respectively and has a high specificity versus a panel of 50 other kinases. Learn More -
VX-680 (MK-0457, Tozasertib)
Catalog No. A10981 Aurora Kinase inhibitorVX-680 is a potent and selective small-molecule inhibitor of the Aurora kinases. Learn More -
Danusertib (PHA-739358)
Catalog No. A10715 Aurora inhibitorDanusertib (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. Phase 2 Learn More -
MLN8054
Catalog No. A10601 Aurora A InhibitorMLN8054 is an inhibitor of Aurora A kinase, induces senescence in human tumor cells both in vitro and in vivo. Learn More -
JNJ-7706621
Catalog No. A10494 CDK/Aurora A/B InhibitorJNJ-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. Learn More -
ENMD-2076
Catalog No. A10352 Aurora A / FLT3 InhibitorENMD-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. Learn More -
KW-2449
Catalog No. A10508 FLT3/FGFR/Bcr-Abl/Aurora InhibitorKW-2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase. Learn More -
AMG 900
Catalog No. A11066 Aurora Kinase inhibitorAMG 900 is a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines. Learn More -
TAK-901
Catalog No. A11067 Aurora Kinase A/B inhibitorTAK-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. Learn More -
TC-S 7010 (Aurora A Inhibitor I)
Catalog No. A10100 Aurora A InhibitorAurora A Inhibitor I is a potent and selective inhibitor of Aurora A kinase (AurA), with IC50 values to be 3.4 nM (Aurora A) and unusually high selectivity 1000 fold against Aurora B; a useful tool compound for investigating the cellular role of Aurora A kinases.
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XL-228
Catalog No. A13069 IGF-1R, Aurora, FGFR, ABL, SRC inhibitorXL228 is a protein kinase inhibitor targeting IGF1R, the AURORA kinases, FGFR1-3, ABL and SRC family kinases. XL228 is an Aurora A inhibitor (IC50, f3 nmol/L) that has shown potent biochemical activity against ABL1 (Ki, 5 nmol/L), as well as the BCR-ABL1 T315I (Ki, 1.4 nmol/L) kinases. Learn More -
TC-A-2317 HCl
Catalog No. A13567 Aurora kinase A inhibitorTC-A-2317 hydrochloride is a potent Aurora kinase A inhibitor (Ki = 1.2 nM compared to 101 nM for inhibition of Aurora kinase B). Selective over 60 other kinases (IC50 values > 1000 nM). Exhibits good cell permeability and antitumor activity. Learn More -
SCH-1473759
Catalog No. A14059 Aurora A/B inhibitorSCH-1473759 is a novel sub-nanomolar Aurora A/B inhibitor with IC50 of 4 nM and 13 nM, respectively. Learn More -
HOI-07
Catalog No. A15970 -
LY3295668
Catalog No. A16869 Aurora A InhibitorLY3295668, also known as AK-01, is potent Aurora-A kinase inhibitor. Learn More -
AAPK-25
Catalog No. A19085 Aurora/PLK dual inhibitorAAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3Ser10 phosphorylation and followed by a surge in apoptosis. Learn More -
CCT241736
Catalog No. A21097 dual FLT3/Aurora kinase inhibitorCCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor. Learn More -
SCH-1473759 hydrochloride
Catalog No. A21711 Aurora inhibitorSCH-1473759 hydrochloride is an aurora inhibitor with IC50s of 4 and 13 nM for aurora A and B, respectively. Learn More -
Aurora Kinase Inhibitor 3
Catalog No. A19448 Aurora A kinase inhibitorAurora Kinase Inhibitor 3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50>10 μM. Learn More -
Aurora inhibitor 1
Catalog No. A19637 Aurora inhibitorAurora inhibitor 1 is a potent Aurora inhibitor with an IC50 of ?? 4 nM and ??13 nM for Aurora A and Aurora B kinase, respectively. Learn More