Aurora Kinase
Aurora kinases are a family of serine-threonine kinases of three highly homologous members, including aurora A kinase, aurora B kinase and aurora C kinase, which are responsible for chromosome assembly and segregation during mitosis. Aurora kinases are characterized by two domains: a regulatory domain in the NH2 terminus and a catalytic domain in the COOH terminus, in which an A-Box and a D-Box found correspondingly in each domain are responsible for protein degradation. Aurora A kinase plays an important role in centrosome function and duplication, mitotic entry and bipolar spindle assembly; while Aurora B kinase is the catalytic component of the chromosomal passenger complex regulating the accurate segregation of the chromatids at mitosis, histone modification and cytokinesis. Aurora C kinase is less studied and expressed restrictedly in the testes.
Products for Aurora Kinase
- Cat.No. Product Name Information
- GC35216 AAPK-25 AAPK-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. AAPK-25 targets Aurora-A, -B, and -C with Kd values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with Kd values ranging from 55-456 nM.
- GC62433 AKI603 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.
- GC13198 AMG-900 A selective pan-Aurora kinase inhibitor
- GC10638 AT9283 A broad spectrum kinase inhibitor
- GC13332 Aurora A Inhibitor I A potent and selective inhibitor of Aurora A kinase
- GC33379 Aurora B inhibitor 1 Aurora B inhibitor 1 is an Aurora B (Aurora-1) inhibitor extracted from patent WO2007059299A1, compound 1-3, has a Ki value of <0.010 uM.
- GC38441 Aurora Kinase Inhibitor 3 A potent inhibitor of Aurora A kinase
- GC40667 Aurora Kinase Inhibitor II Aurora Kinase Inhibitor II is a selective and ATP-competitive Aurora kinase inhibitor with IC50s of 310 nM and 240 nM for Aurora A and Aurora B, respectively.
- GC15711 Aurora Kinase Inhibitor III Aurora Kinase Inhibitor III 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.
- GC67899 Aurora kinase inhibitor-8
- GC48971 AZD 1152 (hydrochloride) A prodrug for a potent Aurora B inhibitor
- GC14709 AZD1152
- GC14955 Barasertib (AZD1152-HQPA) A selective Aurora kinase B inhibitor
- GC17828 BI-847325 dual inhibitor of MEK and Aurora kinases
- GC42933 Binucleine 2 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.
- GC11310 CCT129202 An Aurora kinase inhibitor
- GC14566 CCT137690 An inhibitor of Aurora kinases and FLT3
- GC19092 CCT241736 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).
- GC48982 CD532 An inhibitor of Aurora A kinase activity and the Aurora A-N-Myc protein-protein interaction
- GC62189 CD532 hydrochloride 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.
- GC35651 Cenisertib 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.
- GC62145 Chiauranib 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.
- GC15106 CYC116 A potent Aurora kinase inhibitor
- GC15217 Danusertib (PHA-739358) A pan-Aurora kinase and Abl inhibitor
- GC68147 dAURK-4 hydrochloride
- GC16519 ENMD-2076 A multi-kinase inhibitor
- GC12145 ENMD-2076 L-(+)-Tartaric acid
- GC10008 GSK1070916 A potent inhibitor of Aurora B and C kinases
- GC17196 Hesperadin A multi-kinase inhibitor
- GC50050 Hesperadin hydrochloride Potent Aurora kinase B inhibitor
- GC34159 Ilorasertib (ABT-348) Ilorasertib (ABT-348) (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib (ABT-348) also is a potent VEGF, PDGF inhibitor. Ilorasertib (ABT-348) has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).
- GC38519 Ilorasertib hydrochloride Ilorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).
- GC12612 JNJ-7706621 A dual inhibitor of CDKs and Aurora kinases
- GC14592 KW 2449 A multi-kinase inhibitor
- GC33057 LY3295668 (AK-01) LY3295668 (AK-01) (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.
- GC17162 MK-5108 (VX-689) A potent inhibitor of Aurora kinases
- GC10442 MK-8745 Aurora A inhibitor,potent and selective
- GC12208 MLN8054 An inhibitor of Aurora A kinase
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GC12690
MLN8237 (Alisertib)
An Aurora A kinase inhibitor
- GC34692 NU6140 A Cdk2 inhibitor
- GC18074 PF-03814735 An inhibitor of Aurora A and B kinases
- GC10479 PHA-680632 An Aurora kinase inhibitor
- GC13668 Phthalazinone pyrazole Aurora A kinase inhibitor
- GC14651 Reversine A purine derivative
- GC16614 SCH-1473759
- GC37606 SCH-1473759 hydrochloride SCH-1473759 hydrochloride is an aurora inhibitor with IC50s of 4 and 13 nM for aurora A and B, respectively.
- GC25940 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.
- GC13837 SNS-314 Mesylate A pan-Aurora kinase inhibitor
- GC17455 TAK-632 A selective pan-Raf inhibitor
- GC11085 TAK-901 A non-selective inhibitor of Aurora kinases
- GC62482 TAS-119 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.
- GC16378 TC-A 2317 hydrochloride Potent Aurora kinase A inhibitor (Ki = 1.2 nM compared to 101 nM for inhibition of Aurora kinase B).
-
GC70030
Tinengotinib
Tinengotinib is a regulator of one or more protein kinases, such as Aurora kinase and VEGFR kinase. Tinengotinib has the potential to study diseases mediated by these kinase abnormalities, especially cancer-related diseases (excerpt from patent WO2018108079A1).
- GC11549 VX-680 (MK-0457,Tozasertib) An Aurora kinase inhibitor that regulates mitosis
- GC13102 XL228 A tyrosine kinase inhibitor
- GC14409 ZM 447439 Selective inhibitor of Aurora B kinase