Aurora A Inhibitor I - CAS 1158838-45-9
Catalog number: 1158838-45-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Aurora Kinase
Aurora A Inhibitor I is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM. It is 1000-fold more selective for Aurora A than Aurora B.
Publictions citing BOC Sciences Products
  • >> More
TC-S 7010
1.Aurora-A modulates MMP-2 expression via AKT/NF-κB pathway in esophageal squamous cell carcinoma cells.
Wang X1, Li X2, Li C3, He C3, Ren B3, Deng Q3, Gao W4, Wang B5. Acta Biochim Biophys Sin (Shanghai). 2016 Apr 28. [Epub ahead of print]
Esophageal squamous cell carcinoma (ESCC) is one of the most common malignancies. It is necessary to identify new markers for predicting tumor progression and therapeutic molecular targets. It has been reported that overexpressions of Aurora-A and matrix metalloproteinases 2 (MMP-2) may promote the malignant development of tumor. However, the relationship between Aurora-A and MMP-2 expression in tumor patients has not been investigated. In addition, the underlying mechanisms that Aurora-A regulates MMP-2 expression are still not fully elucidated. In this study, we demonstrated that Aurora-A and MMP-2 were overexpressed in ESCC tissues compared with paired normal adjacent tissues (P < 0.0001). Overexpression of Aurora-A was associated with the lymph node metastasis of ESCC (P = 0.01). Significantly, Aurora-A protein expression was positively correlated with MMP-2 protein expression in ESCC tissues (r = 0.66, P < 0.0001) as well as in ESCC cell lines.
2.Activation of Aurora A kinase through the FGF1/FGFR signaling axis sustains the stem cell characteristics of glioblastoma cells.
Hsu YC1, Kao CY2, Chung YF3, Lee DC3, Jen-Wei L4, Chiu IM5. Exp Cell Res. 2016 Apr 29. pii: S0014-4827(16)30087-8. doi: 10.1016/j.yexcr.2016.04.012. [Epub ahead of print]
Fibroblast growth factor 1 (FGF1) binds and activates FGF receptors, thereby regulating cell proliferation and neurogenesis. Human FGF1 gene 1B promoter (-540 to +31)-driven SV40 T antigen has been shown to result in tumorigenesis in the brains of transgenic mice. FGF1B promoter (-540 to +31)-driven green fluorescent protein (F1BGFP) has also been used in isolating neural stem cells (NSCs) with self-renewal and multipotency from developing and adult mouse brains. In this study, we provide six lines of evidence to demonstrate that FGF1/FGFR signaling is implicated in the expression of Aurora A (AurA) and the activation of its kinase domain (Thr288 phosphorylation) in the maintenance of glioblastoma (GBM) cells and NSCs. First, treatment of FGF1 increases AurA expression in human GBM cell lines. Second, using fluorescence-activated cell sorting, we observed that F1BGFP reporter facilitates the isolation of F1BGFP(+) GBM cells with higher expression levels of FGFR and AurA.
3.In vitro Characterization of Derrone as an Aurora Kinase Inhibitor.
Hoang NT1, Phuong TT, Nguyen TT, Tran YT, Nguyen AT, Nguyen TL, Bui KT. Biol Pharm Bull. 2016 Mar 15. [Epub ahead of print]
Among mitotic kinases, Aurora kinases are the most widely studied, since their expression is restricted to mitosis. They play a key role in chromosome segregation and cell polyploidy. Aurora kinases are important therapeutic targets, and several research groups have directed their efforts toward the identification of kinase inhibitors. The aim of this study is to screen and characterize Aurora kinase inhibitors from natural substances extracted from plants that are used in the Vietnamese pharmacopoeia. We have characterized in vitro Derrone, extracted from Erythrina orientalis L. Murr, as a novel Aurora kinase inhibitor. This compound exhibited an ability to inhibit the phosphorylation of histone H3 at serine 10 both in kinase assay and at the cellular level. The compound was more effective against Aurora kinase B, with a lower IC50 value as compared to Aurora A. Moreover, it impaired the mitotic spindle checkpoint and led to endoreduplication in cancer cells, a phenomenon caused by an Aurora B inhibitor.
4.An update on the pharmacokinetics and pharmacodynamics of alisertib, a selective Aurora kinase A inhibitor.
Durlacher CT1, Li ZL2, Chen XW3, He ZX4, Zhou SF1. Clin Exp Pharmacol Physiol. 2016 Jun;43(6):585-601. doi: 10.1111/1440-1681.12571.
Human Aurora kinases, including Aurora kinase A (AURKA), B (AURKB), and C (AURKC), play an essential role in mitotic events such as monitoring of the mitotic checkpoint, creation of bipolar mitotic spindle and alignment of centrosomes on it, also regulating centrosome separation, bio-orientation of chromosomes and cytokinesis. AURKA and AURKB are key regulators of mitosis and centrosome via polymerizing microfilaments and controlling chromatid segregation. In particular, AURKA plays critical roles in the regulation of mitotic entry, centrosome function, bipolar spindle assembly, and chromosome segregation. AURKA has been found to be overexpressed in various solid and haematological cancers and has been linked with poor prognosis. Its important role in cancer initiation, growth, and metastasis has brought the focus to search for potent and selective AURKA inhibitors for cancer treatment. MLN8237, also known as alisertib, is one selective AURKA inhibitor that has shown remarkable anticancer effects in preclinical studies.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Aurora Kinase Products

CAS 656820-32-5 Reversine

(CAS: 656820-32-5)

CAS 942947-93-5 CCT129202

(CAS: 942947-93-5)

CCT129202 is an inhibitor of Aurora kinase activity and displays a favorable antineoplastic effect in preclinical studies. CCT129202 significantly reversed ABCB...

CAS 422513-13-1 Hesperadin

(CAS: 422513-13-1)

Hesperadin is  an inhibitor of human Aurora B, which can prevent the phosphorylation of substrate with IC(50) of 40 nM. Growth of cultured bloodstream forms was...

CAS 869363-13-3 MLN8054

(CAS: 869363-13-3)

MLN8054 is an aurora kinase inhibitor MLN8054, which is an orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase...

CAS 693228-63-6 CYC116

(CAS: 693228-63-6)

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 ...

CAS 722544-51-6 AZD-1152HQPA

(CAS: 722544-51-6)

AZD-1152HQPA is an active metabolite of Barasertib (AZD-1152), which is a novel acetanilide-substituted pyrazole-aminoquinazoline prodrug that is converted rap...

CAS 1028486-01-2 Alisertib

(CAS: 1028486-01-2)

MLN8237 is a second-generation, orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase with pote...

CAS 1095382-05-0 CCT-137690

(CAS: 1095382-05-0)

CCT137690, an aurora kinase inhibitor CCT137690, is a highly selective, orally bioavailable imidazo[4,5-b]pyridine derivative that inhibits Aurora A and B kinas...

CAS 1245907-03-2 TC-A 2317 hydrochloride

TC-A 2317 hydrochloride
(CAS: 1245907-03-2)

TC-A 2317 hydrochloride is a selective and potent Aurora kinase A (ARK-1) inhibitor (Ki = 1.2 nM and 101 nM for inhibition of Aurora kinase A and Aurora kinase ...

CAS 722543-31-9 Barasertib

(CAS: 722543-31-9)

Barasertib is an orally bioavailable, small-molecule, dihydrogen phosphate prodrug of the pyrazoloquinazoline Aurora kinase inhibitor AZD1152–hydroxyquinazolin...

CAS 885325-71-3 MK-8745

(CAS: 885325-71-3)

MK-8745 is a novel Aurora-A specific inhibitor. MK8745 induced apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lin...

CAS 1158838-43-7 Aurora A inhibitor II

Aurora A inhibitor II
(CAS: 1158838-43-7)

Aurora A inhibitor II is a potent and selective inhibitor of Aurora A kinase (AurA; IC50 = 4.3 nM).

CAS 1094067-13-6 SCH1473759 (HCl salt)

SCH1473759 (HCl salt)
(CAS: 1094067-13-6)

The hydrochloride salt form of SCH-1473759, a new sub-nanomolar Aurora A/B inhibitor which could result in cell death by inhibiting Aurora kinases. It is proved...

(CAS: 1256137-14-0)

SAR156497 is a selective Aurora A, B and C inhibitor with in vitro and in vivo efficacy IC50 value is 0.5 nM for Aurora A; 1.0 nM for Aurora B (incenp) and 3.0 ...

CAS 942918-07-2 GSK-1070916A

(CAS: 942918-07-2)

GSK-1070916A is an ATP-competitive inhibitor of the serine/threonine kinases Aurora B and C with potential antineoplastic activity. Aurora B/C kinase inhibitor ...

CAS 898280-07-4 XL228

(CAS: 898280-07-4)

XL228 is a protein kinase inhibitor targeting IGF1R, the Aurora kinases, FGFR1-3, ABL and SRC family kinases.

CAS 1010085-13-8 MK-5198

(CAS: 1010085-13-8)

MK-5108 is a novel small molecule with potent inhibitory activity against Aurora-A kinase. Although most of the Aurora-kinase inhibitors target both Aurora-A an...

CAS 1158838-45-9 Aurora A Inhibitor I

Aurora A Inhibitor I
(CAS: 1158838-45-9)

Aurora A Inhibitor I is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM. It is 1000-fold more selective for Aurora A than Aurora B.

CAS 398493-79-3 PHA-680632

(CAS: 398493-79-3)

PHA-680632 is a is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM. PHA-680632 is also the first representative of a ...

CAS 827318-97-8 Danusertib

(CAS: 827318-97-8)

Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Aurora kinase inhibitor PHA-739358 binds to and inhibits the A...

Chemical Structure

CAS 1158838-45-9 Aurora A Inhibitor I

Quick Inquiry

Verification code

Featured Items