Search Result
Results for "
Aurora kinases
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-151971
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Aurora Kinase
Polo-like Kinase (PLK)
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Cancer
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Aurora Kinases-IN-3 (Compound 15a) is an orally active AURKB inhibitor that elicits an AURKB-suppressive activity by disrupting the mitotic localization of AURKB, rather than inhibiting its phosphorylation of H3 at Ser10 .
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- HY-112273
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Aurora Kinase
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Cancer
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CD532 is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 also can directly interact with AURKA and induces a global conformational shift. CD532 can be used for the research of cancer .
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- HY-150592
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Aurora Kinase
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Cancer
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Aurora Kinases-IN-2 (compound 12Aj) is a potent Aurora kinases inhibitor with IC50 values of 90 and 152 nM for Aurora A and Aurora B. Aurora Kinases-IN-2 arrests cell cycle at G2/M phase by regulating cyclin B1 and cdc2. Aurora Kinases-IN-2 can be used for cancer research .
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- HY-149354
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Aurora Kinase
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Cancer
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Aurora Kinases-IN-4 (Compound 11c) is a covalent and ATP competitive aurora kinase A inhibitor (IC50: 1.7 nM). Aurora Kinases-IN-4 inhibits cell proliferation in SJSA-1, MDA-MB-231, A54, HeLa cells with IC50s of 4.27, 1.54, 3.08, 6.99 μM. Aurora Kinases-IN-4 can be used for research of triple negative breast cancer (TNBC) .
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- HY-122370A
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Aurora Kinase
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Cancer
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Tripolin B is an ATP-competitive Aurora kinase inhibitor with IC50 values of 2.5 µM and 6 µM for Aurora A and Aurora B kinases, respectively. Tripolin B does not inhibit Aurora kinase in cells .
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- HY-149693
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Aurora Kinase
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Cancer
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Aurora kinase inhibitor-11 (compound 25) is an inhibitor of Aurora Kinase with an IC50 of 0.14 μM. Aurora kinase inhibitor-11 has anticancer activity .
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- HY-160447
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Aurora Kinase
FAK
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Cancer
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FAK/aurora kinase-IN-1 is a FAK and aurora kinase inhibitor with IC50 values of 6.61 nM and 0.91 nM, respectively. FAK/aurora kinase-IN-1 shows anticancer effects (WO2018019252A1; compound 11) .
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- HY-149694
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Aurora Kinase
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Cancer
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Aurora Kinase Inhibitor-12 (Compound 1a ) is the inhibitor of aurora kinase which is a key enzyme that is implicated in tumor growth .
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- HY-144438
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Aurora Kinase
LIM Kinase (LIMK)
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Cancer
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Aurora/LIM kinase-IN-1 (Compound F114) is a potent and dual inhibitor of aurora and lim kinase. Aurora kinases and lim kinases are involved in neoplastic cell division and cell motility, respectively. Aurora/LIM kinase-IN-1 inhibits GBM proliferation and invasion. Aurora/LIM kinase-IN-1 is a promising new scaffold for dual aurora/lim kinase inhibitors that may be used in future agent development efforts for GBM, and potentially other cancers .
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- HY-115932
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Aurora Kinase
Apoptosis
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Cancer
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Aurora kinase-IN-1 (Compound 9) is a potent inhibitor of aurora kinase. Aurora kinase-IN-1 upregulates the expression of G1 cell cycle inhibitory proteins including p21 and p27, and G1 progressive cyclin D1, and downregulates G1-to-S progressive cyclins, resulting in cell cycle arrest at the G1/S boundary. Aurora kinase-IN-1 also induces apoptosis. Aurora kinase-IN-1 is a lead compound for chemotherapeutic agents .
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- HY-112273A
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Aurora Kinase
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Cancer
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CD532 hydrochloride is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 hydrochloride has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 hydrochloride also can directly interact with AURKA and induces a global conformational shift. CD532 hydrochloride can be used for the research of cancer .
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- HY-129727
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Others
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Others
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(E)-MS0019266 is a potent inhibitor of DNA damage repair. (E)-MS0019266 inhibits ribonucleotide reductase by generating reactive oxygen species. (E)-MS0019266 also reduces expression of genes related to cell cycle arrest and mitosis, including polo-like kinase 1, kinesin family member 20a, cyclin B1 and aurora kinase A. (E)-MS0019266 is promising for research of inhibitors of ribonucleotide reductase and polo-like kinase 1 .
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- HY-130665
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PROTACs
CDK
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Cancer
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TL12-186 is a Cereblon-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A (IC50=73 nM) and CDK9/cyclin T1 (IC50=55 nM) .
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- HY-112355
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Aurora Kinase
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Cancer
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Aurora kinase inhibitor-2 is a selective and ATP-competitive Aurora kinase inhibitor with IC50s of 310 nM and 240 nM for Aurora A and Aurora B, respectively .
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- HY-144991
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Aurora Kinase
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Cancer
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Aurora kinase inhibitor-8 is a highly selective inhibitor of the Aurora kinases.
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- HY-147703
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Aurora Kinase
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Cancer
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Aurora kinase inhibitor-9 (compound 9d) is a potent AURKA/B dual aurora kinase inhibitor with IC50s of 0.093, 0.09 µM for Aurora A, Aurora B, respectively. Aurora kinase inhibitor-9 shows broad spectrum anti-proliferative activity .
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- HY-111506
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Aurora Kinase
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Cancer
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Aurora inhibitor 1 is a potent Aurora inhibitor with an IC50 of ≤ 4 nM and ≤13 nM for Aurora A and Aurora B kinase, respectively .
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- HY-147993
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Aurora Kinase
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Cancer
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Aurora kinase inhibitor-10 (Compound 6c) is an orally active Aurora B inhibitor with an IC50 of 8 nM. Aurora kinase inhibitor-10 shows antitumor activity .
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- HY-14711
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Aurora Kinase
Autophagy
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Cancer
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Reversine is a novel class of ATP-competitive Aurora kinase inhibitor with IC50s of 400, 500 and 400 nM for Aurora A, Aurora B and Aurora C, respectively.
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- HY-112373
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Aurora Kinase
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Others
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Aurora 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 of >10 μM. Aurora kinase inhibitor-3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket .
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- HY-18161
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FLT3
Aurora Kinase
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Cancer
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CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A Kd, 7.5 nM, IC50, 38 nM; Aurora-B Kd, 48 nM), FLT3 kinase (Kd, 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd, 38 nM) and FLT3(D835Y) (Kd, 14 nM).
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- HY-123610
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Aurora Kinase
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Cancer
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BRD-7880 is a potent and highly specific inhibitor of Aurora Kinase B (AURKB) and Aurora Kinase C (AURKC), with IC50 values of 7 nM and 12 nM, respectively .
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- HY-10128
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- HY-10179
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PHA-739358
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Aurora Kinase
Autophagy
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Cancer
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Danusertib is a pyrrolo-pyrazole and aurora kinase inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively.
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- HY-124330
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(E)-Tripolin A
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Aurora Kinase
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Others
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Tripolin A ((E)-Tripolin A) is a specific non-ATP competitive Aurora A kinase inhibitor, with IC50 values of 1.5 μM and 7 μM for Aurora A and Aurora B, respectively .
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- HY-12049
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Aurora Kinase
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Cancer
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CCT129202 is an aurora kinase inhibitor with IC50s of 42, 198, and 227 nM for aurora A, B and C, respectively.
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- HY-141512
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JB170
1 Publications Verification
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PROTACs
Aurora Kinase
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Cancer
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JB170 is a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC50=28 nM) by linking Alisertib, to the Cereblon-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase .
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- HY-10178
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Aurora Kinase
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Cancer
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PHA-680632 is an aurora kinase inhibitor with IC50s of 27, 135 and 120 nM for aurora A, B and C, respectively.
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- HY-N3737
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Aurora Kinase
PERK
Reactive Oxygen Species
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Cancer
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Derrone, a prenylated isoflavones, is an Aurora kinase inhibitor, with IC50 values of 6 and 22.3 μM against Aurora B and Aurora A, respectively. Derrone shows anti-tumor activity .
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- HY-13253
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AMG 900
3 Publications Verification
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Aurora Kinase
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Cancer
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AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor with IC50 of 5 nM, 4 nM and 1 nM for Aurora A, B and C, respectively.
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- HY-146037
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Apoptosis
Aurora Kinase
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Cancer
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Aurora A inhibitor 2 (Compound 16h) is a potent Aurora A kinase inhibitor with an IC50 of 21.94 nM. Aurora A inhibitor 2 induces caspase-dependent apoptosis in MDA-MB-231 cells .
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- HY-10804
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Aurora Kinase
Apoptosis
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Cancer
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CCT 137690 is a potent and orally available aurora kinase inhibitor with IC50s of 15, 25, and 19 nM for aurora A, B and C, respectively.
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- HY-103266
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Aurora Kinase
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Cancer
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TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity .
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- HY-121998
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Aurora Kinase
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Others
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Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki=0.36 μM), a kinase involved in cell division. It is specific for Drosophila Aurora B kinase, inhibiting it in a dose-dependent manner, with minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 μM. Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells. It prevents Drosophila S2 cells from assembling a contractile ring during cell division when used at a concentration of 40 μM but does not affect ring ingression, suggesting that Aurora B kinase activity is not required for that step.
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- HY-12003
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Aurora Kinase
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Cancer
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SNS-314 mesylate is a potent and selective aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively .
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- HY-108344
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Aurora Kinase
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Cancer
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SNS-314 is a potent and selective aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively .
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- HY-123279
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Aurora Kinase
CDK
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Cancer
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OM137 is an aurora kinase inhibitor, with an IC50 of 21.7 μM (Aurora A kinase) and 2.4 μM (Aurora B kinase). OM137 also inhibits Cdk1/cyclinB and Cdk5/p25 with an approximate IC50 of 20 μM. OM137 reduces spindle checkpoint-signaling proteins (Mad2 and BubR1) at the kinetochores of chromosomes .
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- HY-13819
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- HY-10329
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Aurora Kinase
CDK
Apoptosis
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Cancer
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JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2, with IC50s of 9 nM, 3 nM, 11 nM, and 15 nM for CDK1, CDK2, aurora-A and aurora-B, respectively .
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- HY-10057
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Aurora Kinase
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Cancer
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AT9283 hydrochloride is a multi-targeted kinase inhibitor with anti-tumor activity. AT9283 hydrochloride has been found to effectively inhibit Aurora A and Aurora B kinases, thereby affecting cell proliferation and survival. AT9283 hydrochloride can also inhibit several other kinases, including JAK2 and Abl (T315I) .
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- HY-10180
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Aurora Kinase
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Cancer
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MLN8054 is a potent, selective and orally available aurora A kinase inhibitor with an IC50 of 4 nM.
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- HY-121895
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Aurora Kinase
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Cancer
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BI 831266 is a potent and selective inhibitor of Aurora kinase B with antitumor activity .
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- HY-137377
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Aurora Kinase
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Cancer
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TAS-119 is a potent, selective and orally active Aurora A inhibitor with an IC50 of 1.0 nM. TAS-119 shows high selectivity for Aurora A over other protein kinases, including Aurora B (IC50 of 95 nM). TAS-119 has potent antitumor activites .
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- HY-156378
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Aurora Kinase
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Cancer
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Aurora A inhibitor 3 (Compound 5h) inhibits Aurora-A kinase with an IC50 value of 0.78 μM. Aurora A inhibitor 3 is cytotoxic, with GI50 values of 0.12 μM and 0.63 μM for MCF-7 and MDA-MB-231 cells, respectively .
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- HY-13252
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- HY-113894
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Aurora Kinase
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Cancer
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Retreversine is an inactive control for Reversine. Reversine is a novel class of ATP-competitive Aurora kinase inhibitor .
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- HY-145601
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TT 00420
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Aurora Kinase
VEGFR
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Cancer
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Tinengotinib is the modulator of one or more protein kinases such as Aurora kinase and VEGFR kinase. Tinengotinib has the potential for the research of these kinase abnormalities diseases mediated, especially cancer-related diseases (extracted from patent WO2018108079A1) .
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- HY-10971A
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MLN 8237 sodium
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Aurora Kinase
Autophagy
Apoptosis
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Cancer
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Alisertib (MLN 8237) sodium is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib sodium induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity .
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- HY-10971
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Alisertib
Maximum Cited Publications
49 Publications Verification
MLN 8237
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Aurora Kinase
Autophagy
Apoptosis
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Cancer
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Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity .
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- HY-10339
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- HY-144307
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Aurora Kinase
PKC
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Cancer
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Aurora A/PKC-IN-1 (Compound 2e) is a potent dual inhibitor of Aurora A (AurA) and PKC (α, β1, β2, and θ) kinases with IC50s of 6.9 nM and 16.9 nM for AurA and PKCα, respectively. Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells and antimetastatic activity .
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- HY-10161
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VX 680; MK-0457
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Aurora Kinase
Autophagy
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Cancer
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Tozasertib (VX 680; MK-0457) is an inhibitor of Aurora A/B/C kinases with Kis of 0.6, 18, 4.6 nM, respectively.
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- HY-114258
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AK-01
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Aurora Kinase
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Cancer
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LY3295668 (AK-01) is a potent, orally active and highly specific Aurora-A kinase inhibitor, with Ki values of 0.8 nM and 1038 nM for AurA and AurB, respectively.
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- HY-112809
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Syk
Src
LRRK2
GSK-3
JAK
VEGFR
Aurora Kinase
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Inflammation/Immunology
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GSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.1. GSK2646264 also inhibits other kinases with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin .
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- HY-164455
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Aurora Kinase
JAK
STAT
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Inflammation/Immunology
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AJI-214 is a dual-target inhibitor of Aurora kinase A and JAK2. AJI-214 directly blocks Aurora kinase A to inhibit T cell mitotic progression and cell polarity, and inhibits JAK2 activation to inhibit STAT3 phosphorylation, thereby reducing the differentiation of TH1 and TH17 cells. AJI-214 can be used in studies on regulating immune responses and preventing graft-versus-host disease (GVHD) .
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- HY-125956
-
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Aurora Kinase
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Cancer
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Aurkin A is an allosteric inhibitor for the interaction between Aurora A Kinase (also known also Aurka) and TPX2, through targeting the TPX2 binding sites with Kd of 3.77 μM .
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- HY-164454
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Aurora Kinase
JAK
STAT
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Inflammation/Immunology
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AJI-100 is a dual-target inhibitor of Aurora kinase A and JAK2 with IC50 values ??of 12.7 nM and 18.5 nM, respectively. AJI-100 directly blocks Aurora kinase A to inhibit T cell mitosis and cell polarity, and inhibits JAK2 activation to inhibit STAT3 phosphorylation, thereby reducing the differentiation of TH1 and TH17 cells. AJI-100 can be used in studies on regulating immune responses and preventing graft-versus-host disease (GVHD) .
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- HY-123697
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Aurora Kinase
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Cancer
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VE-465 is an Aurora kinase inhibitor. VE-465 induces cancer cell apoptosis. VE-465 has anticancer effects in multiple tumor models .
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- HY-N3634
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EGFR
TAM Receptor
Tie
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Cancer
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Corylifol C is a potent protein kinase inhibitor with IC50 valueS of 8.7, 3.0, 2.1, 6.4, 4.5, 6.2, 2.3, 1.2, 5.1 μg/ml for ARK5, Aurora-A, Aurora-B, AXL, B-RAF-VE, CDK4/CycD1, TIE2, EGF-R, EPHB4, respectively .
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- HY-15749
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- HY-158038
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Aurora Kinase
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Cancer
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AurkA allosteric-IN-1 (compound 6h) is an Aurora A (AurkA) inhibitor (IC50: 6.50 μM) that inhibits the catalytic activity and non-catalytic functions of Aurora A. Aurora A regulates the assembly of the bipolar mitotic spindle and the fidelity of chromosome segregation during mitosis and has non-catalytic functions. AurkA allosteric-IN-1 blocks the interaction of AurkA with the activator TPX2 by binding to the Y pocket of AurkA .
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- HY-124526
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Ibcasertib; CS2164
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VEGFR
PDGFR
c-Kit
Aurora Kinase
c-Fms
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Cancer
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Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF-1R, with IC50 values ranging from 1-9 nM. Chiauranib has strongly anticancer effects .
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- HY-123159
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Aurora Kinase
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Cancer
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AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells .
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- HY-13072
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AS-703569; R-763
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Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
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Cancer
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Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
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- HY-156863
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- HY-50514
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AT9283
5 Publications Verification
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JAK
Aurora Kinase
Bcr-Abl
FLT3
Apoptosis
Autophagy
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Cancer
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AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo .
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- HY-157396
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Aurora Kinase
Apoptosis
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Cancer
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JAB-2485 is a potent and selective Aurora kinase A (AURKA) inhibitor, with an IC50 of 0.33 nM. JAB-2485 exhibits around 1700-fold selectivity for AURKA over AURKB. JAB-2485 induces cell cycle arrest and apoptosis. JAB-2485 can be used for the research of cancer .
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- HY-13072B
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AS-703569 benzoate; R-763 benzoate
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Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
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Cancer
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Cenisertib (AS-703569) benzoate is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib benzoate induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib benzoate inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
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- HY-119618
-
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Endogenous Metabolite
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Cancer
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R1498 is a multi-target kinase inhibitor with anti-angiogenic and anti-proliferative activities. R1498 mainly targets targets such as Aurora kinase and VEGFR2, which are associated with tumor development. R1498 showed moderate in vitro growth inhibition in a variety of tumor cells, with IC50 values in the micromolar range. R1498 showed anti-tumor efficacy superior to sorafenib in a variety of gastric cancer and hepatocellular carcinoma xenograft models, with tumor growth inhibition rates exceeding 80%, and tumor shrinkage was observed in some models. R1498 showed a 10-30% tumor shrinkage rate in three xenograft models derived from human primary gastric cancer tumors, further demonstrating its inhibitory potential. R1498 effectively inhibited Aurora A activity in vivo and reduced tumor vascularization .
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- HY-18955
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MEK
Aurora Kinase
Apoptosis
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Cancer
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BI-847325 is an ATP competitive dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively. BI-847325 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-10058
-
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JAK
Aurora Kinase
Bcr-Abl
FLT3
Apoptosis
Autophagy
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Cancer
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AT9283 lactic acid is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 lactic acid inhibits growth and survival of multiple solid tumors in vitro and in vivo .
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- HY-10987A
-
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Aurora Kinase
FLT3
VEGFR
FGFR
PDGFR
Src
Apoptosis
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Cancer
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ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
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- HY-114302
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CCB02
1 Publications Verification
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Microtubule/Tubulin
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Cancer
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CCB02 is a selective CPAP-tubulin interaction inhibitor, binding to tubulin and competing for the CPAP binding site of β-tubulin, with an IC50 of 689 nM, and shows potent anti-tumor activity. CCB02 shows no inhibition on the cell cycle- and centrosome-related kinases, or the phosphorylation status of Aurora A, Plk1, Plk2, CDK2, and CHK1 .
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- HY-10987
-
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Aurora Kinase
FLT3
VEGFR
FGFR
Src
PDGFR
Apoptosis
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Cancer
|
ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
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- HY-12564
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Aurora Kinase
Apoptosis
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Cancer
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Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC50 of 0.031 μM. Phthalazinone pyrazole can arrests mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells. Phthalazinone pyrazole suppresses the epithelial-mesenchymal transition (EMT) during the differentiation of hepatocyte-like cells (HLCs) from human embryonic stem cells .
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- HY-116423
-
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NEKs
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Cancer
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JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-116423A
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NEKs
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Cancer
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JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 (hydrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-15720B
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ROCK
Aurora Kinase
CaMK
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Neurological Disease
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Glycyl H-1152 hydrochloride (compound 18) is a glycyl derivative of Rho-kinase inhibitors H-1152 dihydrochloride. Glycyl H-1152 hydrochloride inhibits ROCKII, Aurora A, CAMKII and PKG, with IC50s of 0.0118, 2.35, 2.57 and 3.26 μM respectively. Glycyl H-1152 hydrochloride has higher selective than H-1152 hydrochloride .
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- HY-162470
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Aurora Kinase
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Cancer
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DBPR728 is an acyl prodrug of 6K465 that carries fewer hydrogen bond donors. 6K465 acts as an Aurora kinase inhibitor that destabilizes MYC family cancer proteins and has antitumor efficacy. DBPR728 has the potential to inhibit cancers that overexpress C-MYC and N-MYC, with a 10-fold increase in oral bioavailability compared to 6K465 .
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- HY-W395613
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Aurora Kinase
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Cancer
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TY-011 is an Aurora A/B kinase inhibitor. TY-011 induces abnormal microtubule-kinetochore attachment, leading to DNA damage and apoptosis (Apoptosis) in human gastric cancer cells, and ultimately inhibits cancer cell proliferation, with an IC50 value ranging from 0.11 to 4.49 μM in human gastric cancer cell lines. TY-011 has potential applications in gastric cancer research .
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- HY-123919
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PROTACs
Anaplastic lymphoma kinase (ALK)
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Cancer
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TL13-112 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.14 nM. TL13-112 also prompts the degradation of additional kinases including Aurora A, FER, PTK2 and RPS6KA1 with IC50 values of 8550 nM, 42.4 nM, 25.4 nM, and 677 nM, respectively. TL13-112 is comprised of the conjugation of Ceritinib?(HY-15656) and the Cereblon ligand of Pomalidomide (HY-10984) .
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- HY-125090
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Aurora Kinase
c-Myc
Bcr-Abl
Histone Methyltransferase
Apoptosis
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Cancer
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PHA-680626 is an effective inhibitor of the interaction between Aurora-A and N-Myc. PHA-680626 inhibits kinase activity of AURKA and Bcr-Abl, and induces N-Myc degradation. PHA-680626 decreases phosphorylation of CrkL and histone H3. PHA-680626 shows anti-proliferative and pro-apoptotic activity on Imatinib (HY-15463)-resistant chronic myeloid leukemia cell lines and primary CD34+ cells .
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- HY-122582
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PROTACs
Anaplastic lymphoma kinase (ALK)
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Cancer
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TL13-12 is a potent and selective?ALK-PROTAC?degrader and inhibits?ALK?activity with an IC50 value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC50 values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the Cereblon ligand of Pomalidomide (HY-10984) .
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- HY-115862
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Adenosine Receptor
PARP
Aurora Kinase
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Cardiovascular Disease
Cancer
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Benzo[c][1,8]naphthyridin-6(5H)-one exhibits low micromolar affinity to human adenosine receptor (AR) A1 and hA2A, with Ki of 4.6 and 4.8 μM. Benzo[c][1,8]naphthyridin-6(5H)-one is inhibitor for poly ADP-ribose polymerase-1 (PARP-1) and aurora kinase A, with IC50 of 0.311 and 5.5 μM .
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- HY-10320G
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BIRB 796 (GMP)
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p38 MAPK
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Cancer
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Doramapimod GMP (BIRB 796 GMP) is an orally active inhibitor for p38 MAPK, with IC50s of 38, 65, 200 and 520 nM, for p38α, p38β, p38γ, p38δ. Doramapimod exhibits cytotoxicity and antitumor activity against multiple myeloma, synergizes with multidrug resistance protein 1 (ABCB1) and aurora kinase inhibitor VX680, promoting their antitumor efficacy against oral epidermoid carcinoma and cervical cancer. Doramapimod also exhibits anti-inflammatory activity .
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- HY-167854
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Others
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Cancer
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KW-2450 Free base is a potent multikinase inhibitor targeting Aurora A and B kinases, demonstrating significant antitumor activity against triple-negative breast cancer (TNBC). KW-2450 Free base effectively reduces cell viability, promotes apoptosis, and inhibits colony formation and mammosphere formation in TNBC cells. KW-2450 Free base significantly suppresses the growth of TNBC xenografts, leading to tetraploid accumulation followed by apoptosis or the survival of octaploid cells. KW-2450 Free base enhances the efficacy of combination therapy with the MEK inhibitor selumetinib, resulting in a synergistic antitumor effect in TNBC models. KW-2450 Free base also acts as an orally bioavailable inhibitor of IGF-1R and IR tyrosine kinases, contributing to its potential antineoplastic activity by inhibiting tumor cell proliferation and inducing apoptosis.
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HY-L004
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2,345 compounds
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DNA is prone to numerous forms of damage that can injure cells and impair fitness. Cells have developed an array of mechanisms to repair these injuries. Proliferating cells are especially vulnerable to DNA damage due to the added demands of cellular growth and division. Cell cycle checkpoints represent integral components of DNA repair that coordinate cooperation between the machinery of the cell cycle and several biochemical pathways that respond to damage and restore DNA structure. By delaying progression through the cell cycle, checkpoints provide more time for repair before the critical phases of DNA replication, when the genome is replicated, and of mitosis, when the genome is segregated. Loss or attenuation of checkpoint function may increase spontaneous and induced gene mutations and chromosomal aberrations by reducing the efficiency of DNA repair.
MCE owns a unique collection of 2,345 cell cycle/DNA damage-related compounds which can be used in the research of the same.
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N3737
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- HY-N3634
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Structural Classification
Leguminosae
Source classification
Phenols
Polyphenols
Psoralea corylifolia L.
Plants
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EGFR
TAM Receptor
Tie
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Corylifol C is a potent protein kinase inhibitor with IC50 valueS of 8.7, 3.0, 2.1, 6.4, 4.5, 6.2, 2.3, 1.2, 5.1 μg/ml for ARK5, Aurora-A, Aurora-B, AXL, B-RAF-VE, CDK4/CycD1, TIE2, EGF-R, EPHB4, respectively .
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Cat. No. |
Product Name |
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Classification |
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- HY-116423
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Alkynes
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JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-116423A
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Alkynes
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JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 (hydrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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