Aurora A
Aurora A kinase (AURKA) is a conserved serine/threonine kinase that primarily regulates centrosome maturation, centrosome separation, and bipolar spindle assembly during mitosis, thereby supporting accurate chromosome segregation and cell-cycle progression[1][2]. Mechanistically, AURKA functions within mitotic spindle regulatory networks and is activated through interactions with spindle-associated cofactors such as TPX2, which promotes spatial control of kinase activity during mitosis[3][4]. Through its role in microtubule organization and spindle formation, AURKA contributes to the maintenance of genomic stability, whereas dysregulated AURKA activity is associated with abnormal mitotic progression and chromosomal instability in cancer models[1][5]. In disease-relevant experimental systems, aberrant Aurora kinase signaling has been linked to tumor development and progression, supporting the use of AURKA as a molecular target in studies of mitotic control and oncogenic transformation[5][6]. Compared with related isoforms, Aurora B predominantly regulates chromosome-microtubule attachment, spindle checkpoint signaling, chromosome alignment, and cytokinesis as a core component of the chromosomal passenger complex, whereas AURKA mainly functions at centrosomes and spindle poles during early mitosis[1][2][3]. This spatial and functional distinction provides an important framework for isoform-selective experimental design and interpretation of mitotic phenotypes[1][3]. For research applications, Aurora kinase inhibitors are widely used to investigate mitotic signaling pathways and chromosome segregation mechanisms, and selective targeting strategies continue to be explored in anticancer research models[6].
References:
- [1]. Willems E, et al. The functional diversity of Aurora kinases: a comprehensive review. Cell Div. 2018 Sep 19;13:7. [Content Brief]
- [2]. Carmena M, et al. The cellular geography of aurora kinases. Nat Rev Mol Cell Biol. 2003;4(11):842-854.
- [3]. Carmena M, et al. Making the Auroras glow: regulation of Aurora A and B kinase function by interacting proteins. Curr Opin Cell Biol. 2009 Dec;21(6):796-805. [Content Brief]
- [4]. Wikipedia.
- [5]. Pérez de Castro I, et al. Editorial: Aurora Kinases: Classical Mitotic Roles, Non-Canonical Functions and Translational Views. Front Oncol. 2017;7:48.
- [6]. Kitzen JJ, et al. Aurora kinase inhibitors. Crit Rev Oncol Hematol. 2010 Feb;73(2):99-110. [Content Brief]
-
Aurora A Related Products (112)
Related Products (112)
-
Antibodies (2)
-
SK4454
0 ImagesCat. No.: HY-179640SK4454 is a selective AURKA PROTAC degrader degrading AURKA with IC50 = 8 nM. MYCN levels in MYCN-amplified neuroblastoma cells and limited by MDR1-mediated efflux. SK4454 efficiently reduced AURKA levels in vivo. SK4454 can be used for neuroblastoma research.
-
IBPR002
0 ImagesCat. No.: HY-165369CAS No.: 1192754-38-3IBPR002 is an inhibitor of Aurora kinase A and Aurora kinase B, with IC50 values of 41 nM and 17 nM, respectively. IBPR002 disrupts the nucleation and bundling of kinetochore microtubules, impairs the bipolarity of mitotic spindles, and promotes the binding of non-phosphorylated hepatoma up-regulated protein (HURP) to microtubules derived from the mother centrosome. IBPR002 reduces tumorigenesis levels in a colorectal cancer xenograft model using athymic nude mice. IBPR002 is applicable for research related to colorectal cancer.
-
Aurora kinase/ALK-IN-1
0 ImagesCat. No.: HY-183767Aurora kinase/ALK-IN-1 is a dual Aurora A kinase and ALK inhibitor with IC50 values of 0.296 μM and 0.332 μM, respectively. Aurora kinase/ALK-IN-1 induces G2/M cell cycle arrest, triggers mitochondrial apoptosis, elevates intracellular reactive oxygen species (ROS) levels, and inhibits ALDH1 activity. Aurora kinase/ALK-IN-1 demonstrates cytotoxicity and tumor selectivity. Aurora kinase/ALK-IN-1 can be used for the research of anaplastic large cell lymphoma.
-
PROTAC AURKA degrader-4
0 ImagesCat. No.: HY-187470CAS No.: 3135155-78-8PROTAC AURKA degrader-4 is a AURKA PROTAC degrader with a DC50 of 25.62 nM (Jurkat cells). PROTAC AURKA degrader-4 recruits the CRBN E3 ubiquitin ligase via the ubiquitin-proteasome system. PROTAC AURKA degrader-4 disrupts both the catalytic and non-catalytic functions of AURKA, including its interactions with TPX2 and c-Myc. PROTAC AURKA degrader-4 induces G2/M phase arrest and apoptosis. PROTAC AURKA degrader-4 exhibits enhanced antiproliferative activity and in vivo antitumor efficacy in models with high CRBN and AURKA expression. PROTAC AURKA degrader-4 can be used for the research of acute lymphoblastic leukemia.
-
CDK2-IN-55
0 ImagesCDK2-IN-55 (Compound 12c) is a CDK2 inhibitor with an IC50 value of 4.7 nM. CDK2-IN-55 also has a strong inhibitory effect on CDK1 (IC50 = 26.3 nM), moderate inhibitory effects on Aurora A (IC50 = 92.0 nM) and CDK9 (IC50 = 288 nM), and very weak inhibitory activities on CDK4, CDK6, DYRK1A, and GSK3β (IC50 > 1000 nM). CDK2-IN-55 shows strong anti-proliferative activity against various cancer cell lines, inducing cell cycle arrest and apoptosis. CDK2-IN-55 can be used for research on colorectal cancer, lung cancer, and cervical cancer.
-
RET-IN-19
0 ImagesCat. No.: HY-151377CAS No.: 2484919-71-1RET-IN-19 (compound 59) is a potent RET inhibitor, with IC50 values of 6.8 and 13.51 nM against RET-wt and RET V804M, respectively. RET-IN-19 shows anticancer activity. RET-IN-19 can be used for non-small cell lung cancer (NSCLC) research.
-
SNS-314
0 ImagesCat. No.: HY-108344CAS No.: 1057249-41-8SNS-314 is a potent and selective aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively.
-
Abd141
0 ImagesCat. No.: HY-187195Abd141 is a dual PROTAC degrader of ATR and Aurora kinase A (AURKA), with DC50 values of 97.7 nM and 6.7 nM, respectively. Abd141 inhibits the proliferation of acute lymphoblastic leukemia cells. Abd141 can be used in the research of acute lymphoblastic leukemia.
-
Aurora A/PKC-IN-1
0 ImagesCat. No.: HY-144307CAS No.: 3031505-76-4
-
Aurora kinase-IN-15
0 ImagesCat. No.: HY-184386Aurora kinase-IN-15 is a potent dual Aurora A and Aurora B kinase inhibitor. Aurora kinase-IN-15 has broad-spectrum anticancer activity and low toxicity to normal cells. Aurora kinase-IN-15 induces G2/M phase arrest, apoptosis, and activates the intrinsic apoptotic pathway through upregulation of Caspase 3 and Bax, along with downregulation of Bcl-2. Aurora kinase-IN-15 can be used for the study of breast cancer, hepatocellular carcinoma, colorectal cancer and prostate cancer.
-
XMD-12
0 ImagesXMD-12 (compound 1) is an Aurora kinase (Aurora Kinase) inhibitor with anti-tumor activity that promotes paclitaxel (HY-B0015) induced cell death. XMD-12 exhibits high selectivity and potency against Aurora A, B, and C kinases, with IC50 values of 5.6, 18.4, and 24.6 nM, respectively.
-
AurkA allosteric-IN-1
0 ImagesCat. No.: HY-158038CAS No.: 3035323-39-5AurkA 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.
-
M9101
0 ImagesCat. No.: HY-184193M9101 is a selective Aurora A PROTAC degrader with a DC50 of 2.3 nM. M9101 induces G2/M arrest in triple-negative breast cancer cells and potently inhibits the proliferation of multiple tumor cell lines. M9101 can be used in the research of various cancers including triple-negative breast cancer.
-
Aurora kinase-IN-2
0 ImagesCat. No.: HY-150592CAS No.: 2241914-86-1Aurora kinase-IN-2 (compound 12Aj) is a potent Aurora kinase inhibitor with IC50 values of 90 and 152 nM for Aurora A and Aurora B. Aurora kinase-IN-2 arrests cell cycle at G2/M phase by regulating cyclin B1 and cdc2. Aurora kinase-IN-2 can be used for cancer research.
-
Aurora kinase inhibitor-9
0 ImagesCat. No.: HY-147703CAS No.: 2419107-09-6Aurora 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.
-
CDK1-IN-9
0 ImagesCat. No.: HY-182752CDK1-IN-9 is an orally active and selective CDK1 inhibitor with an IC50 of 5.5 nM. CDK1-IN-9 exhibits broad antiproliferative activity, particularly against HCT116 colon cancer cells. CDK1-IN-9 induces G2/M phase arrest and downregulates CDK1, cyclin B1, and the replication initiation factor CDC45. CDK1-IN-9 induces severe DNA replication stress, subsequently activating the p53 signaling pathway to trigger apoptosis. CDK1-IN-9 can be used for research on colon cancer, liver cancer and gastric cancer.
-
BRD-7880
0 ImagesCat. No.: HY-123610CAS No.: 1456542-69-0BRD-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.
-
LS-Q2
0 ImagesCat. No.: HY-182986LS-Q2 is a highly selective CDK4/9 inhibitor with IC50 values of 1.4 nM and 6.2 nM. LS-Q2 inhibits cancer cells proliferation, induces G2/M phase arrest, apoptosis and reduces pSer2 RNA polymerase II expression. LS-Q2 interacts synergistically with BET and Bcl-2 inhibitors to drive antitumor activity. LS-Q2 can be used for the research of cancer, such as malignant solid tumors.
