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(9)
Cell Cycle/Checkpoint Filter
Cell Cycle/Checkpoint Chromatin/EpigeneticAMPK
(119)
Aurora Kinase
(77)
DNA Methyltransferase
(35)
Epigenetic Reader Domain
(297)
HDAC
(207)
HIF
(64)
HIF/HIF Prolyl-Hydroxylase
(72)
Histone Acetyltransferase
(42)
Histone Demethylase
(83)
Histone Methyltransferase
(203)
HuR
(3)
JAK
(162)
Methionine Adenosyltransferase (MAT)
(10)
PAD
(10)
PARP
(144)
PKC
(162)
Pim
(35)
Sirtuin
(92)
Aurora Kinase
Aurora kinases are serine/threonine kinases that are essential for cell proliferation. They are phosphotransferase enzymes that help the dividing cell dispense its genetic materials to its daughter cells. More specifically, Aurora kinases play a crucial role in cellular division by controlling chromatid segregation. Defects in this segregation can cause genetic instability, a condition which is highly associated with tumorigenesis.
Alisertib
Cited
T22411028486-01-2
Alisertib (MLN 8237) is a specific Aurora A inhibitor (IC50: 1.2 nM). The selectivity of Alisertib(MLN 8237) is >200-fold higher for Aurora A than Aurora B.
- $50
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CitedBarasertib
T14371722543-31-9
AZD1152 is a pro-drug of Barasertib (AZD1152)-hQPA. Which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.
- $42
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SP600125
Cited
T3109129-56-6
SP600125 (JNK Inhibitor II) is a JNK inhibitor that inhibits JNK1, JNK2, and JNK3 (IC50=40/40/90 nM) with oral potency, reversibility, and ATP-competitive properties. SP600125 inhibits autophagy and induces apoptosis.
- $41
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CitedGSK-1070916
T6129942918-07-2
GSK-1070916 (GSK-1070916A) 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.
- $41
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MK-5108
T60681010085-13-8
MK-5108 (VX-689) is a highly potent and specific Aurora-A kinase inhibitor with an IC50 value of 0.064 nM.
- $34
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LY3295668
T158151919888-06-4In house
LY3295668 (AK-01) is a selective inhibitor of Aurora A, with Ki values of 0.8 nM for Aurora A and 1038 nM for Aurora B.
- $145
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PF 477736
T6028952021-60-2
PF 477736 (PF-736,PF-00477736) is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (CSF1R), Ret and Yes.
- $45
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MBM-55
T119602083622-09-5
MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM. MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.
- $187
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Ilorasertib
TQ00591227939-82-3
Ilorasertib (ABT-348) (ABT-348) is an ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora A Aurora B Aurora C (IC50s: 120 nM 7 nM 1 nM). It also suppresses RET tyrosine kinase, PDGFRβ, and Flt1 (IC50s: 7 nM, 3 nM, and 32 nM).
- $33
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Danusertib Cited
T2094827318-97-8
Danusertib (PHA-739358) is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in tumor cells in which Aurora kinases are overexpressed.
- $54
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CitedChiauranib
T355701256349-48-0
Chiauranib is a multi-target inhibitor against tumor angiogenesis and exhibits potent anticancer effects. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF1R, with IC50 values ranging from 1-9 nM.
- $83
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Reversine Cited
T1825656820-32-5
Reversine, a small synthetic purine analogue (2, 6-disubstituted purine), is a potent inhibitior of Aurora A B C(IC50s=150-500 nM).
- $32
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CitedTozasertib Cited
T2509639089-54-6
Tozasertib (MK-0457) is a pan-Aurora kinase inhibitor (Kis: 0.6 18 4.6 nM for Aurora A Aurora B Aurora C). It shows selectivity against more than 190 different kinases.
- $62
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CitedHesperadin Cited
T6532422513-13-1
Hesperadin(IC50=250 nM) effectively inhibits Aurora B. It potently reduces the activity of AMPK, MAPKAP-K1, MKK1, Lck, CHK1 and PHK, but it could not inhibit MKK1 activity in vivo.
- $33
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CitedTAS-119
T347871453099-83-6
TAS-119 (TAS-2104) is an orally available, selective and potent inhibitor of Aurora A with an IC50 of 1.0 nM.TAS-119 also inhibits Aurora B with an IC50 of 95 nM.TAS-119 has a higher affinity for Aurora A than for Aurora B.TAS-119 exhibits potent antitumor activity and potential antimitotic activity. TAS-119 has potent anti-tumor activity and potential anti-mitotic activity.
- $98
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Aurora B inhibitor 1
T12010937276-52-3
Aurora B inhibitor 1 is an Aurora B (Aurora-1) inhibitor (Ki <0.010 µM) with potential anticancer activity for cancer research.
- $700
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AMG 900
T6380945595-80-2
AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A B C with IC50 values of 5 nM, 4 nM, and 1 nM, respectively. It exhibits over 10-fold selectivity for Aurora kinases compared to p38α, Tyk2, JNK2, Met, and Tie2. [Phase 1].
- $44
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SP-96
T412562682114-54-9
SP-96 is a highly effective and selective inhibitor of Aurora B with an IC50 of 0.316 nM. SP-96 shows selective growth inhibition in NCI60 screening, including MDA-MD-468 (GI50=107 nM). SP-96 can be used in triple negative breast cancer studies.
- $67
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XU1
T2917053439-81-9In house
XU1（Benzo[c][1,8]naphthyridin-6(5h)-One） is an Aurora protein kinase inhibitor used for the treatment of diseases suitable for inhibition, regulation or modulation of kinase signaling.
- $328
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AT9283 Cited
T3068896466-04-9
AT9283 (J-504568) is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).
- $39
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CitedVX-11e
T3166896720-20-0
VX-11e (TCS ERK 11e) is a potent, selective, and orally bioavailable ERK(Extracellular Signal-Regulated Kinase) inhibitor; antitumor agent.
- $50
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CCT129202
T6435942947-93-5
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.
- $39
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Centrinone
T149271798871-30-3
Centrinone (LCR-263) (LCR-263) is a reversible inhibitor of polo-like kinase 4 (PLK4; Ki:0.16 nM).
- $56
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CYC-116
T6458693228-63-6
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.
- $33
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MBM-55S
T119612083624-07-9In house
MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.
- $195
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CCT 137690
T26111095382-05-0
CCT 137690 is a highly specific and oral-available aurora kinase inhibitor, for aurora A(IC50=15 nM ), B(IC50=25 nM) and C(IC50=19 nM).
- $51
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Barasertib-HQPA Cited
T2602722544-51-6
Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM, demonstrating approximately 3,700-fold greater selectivity for Aurora B over Aurora A.
- $43
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CitedCD532
T501101639009-81-6
CD532 is A highly potent Aurora A kinase inhibitor with an IC50 value of 45 nM. CD532 can block Aurora A kinase activity, drive MYCN degradation, and can directly interact with AURKA and induce global conformational transformation. CD532 can be used to study cancer.
- $33
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JNJ-7706621
T6126443797-96-4
JNJ-7706621 is a potent aurora kinase inhibitor that also inhibits CDK1 and CDK2.
- $43
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TAK-901 Cited
T2709934541-31-8
TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others.
- $66
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CitedKW-2449
T23411000669-72-6
KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 (IC50: 6.6 nM), modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-1R, EGFR.
- $33
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MLN8054 Cited
T6315869363-13-3
MLN8054 is a potent and selective Aurora A kinase inhibitor with an IC50 of 4 nM.
- $48
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CitedCCT241736
T44281402709-93-6
CCT241736 is an orally bioavailable dual FLT3/Aurora kinase inhibitor that also inhibits clinically relevant FLT3-resistant mutants including FLT3-ITD and FLT3, CCT241736, an advanced analog of CCT137690, is a preclinical development candidate for the treatment of human malignancies, and in particular AML in adults and children.
- $55
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TAK-632 Cited
T18861228591-30-7
TAK-632, a potent pan-Raf inhibitor (GenScript, 2020), is characterized by its molecular weight [M] for [C 22 H 19 FN 2 O 2] of 362.4 by LC-MS, with a purity of 99% (HPLC). The compound exhibits white to off-white solid form and has a melting point [M] ranging from 178°C to 182°C (GenScript, 2020). Its solubility profile includes DMSO, in which it is soluble to 100mM (GenScript, 2020).
- $35
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CitedGW843682X
T15454660868-91-7
GW843682X (GW843682) is a selective and ATP-competitive inhibitor of PLK1 and PLK3 (IC50s = 2.2 nM and 9.1 nM).
- $32
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XL228
T17267898280-07-4
XL228 is an inhibitor of multi-targeted tyrosine kinase (IC50s: 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src, and Lyn, respectively).
- $51
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ZM-447439
T6077331771-20-1
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.
- $45
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PHA-680632
T6338398493-79-3
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.
- $39
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URMC-099
T60571229582-33-5
URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19 42 14 150 nM, for MLK1 MLK2 MLK3 DLK), and also inhibits LRRK2 activity (IC50: 11 nM).
- $52
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TCS7010 Cited
T67671158838-45-9
TCS7010 (Aurora A Inhibitor I) 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.
- $30
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CitedG-749
T26201457983-28-6
G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants.
- $40
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ENMD-2076
T2358934353-76-1
ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα.
- $47
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AAPK-25
T102152247919-28-2
AAPK-25 is a potent and selective Aurora PLK dual inhibitor with anti-tumor activity, causing mitotic delay and arresting cells in prometaphase, followed by increased apoptosis. It targets Aurora-A -B -C with Kd values ranging from 23-289 nM.
- $87
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BI-847325
T67851207293-36-4
BI-847325 is a selective dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively.
- $45
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PF-03814735
T6936942487-16-3
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.
Inquiry
NU6140
T16359444723-13-1
NU6140 is a selective inhibitor of CDK2-cyclin A (IC50, 0.41 μM). It shows 10- to 36-fold selectivity over other CDKs. NU6140 also effectively inhibits Aurora A and Aurora B (IC50s: 67 and 35 nM, respectively). It also enhances the apoptotic effect and has anti-cancer activity.
- $35
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