Aurora Kinase
Aurora kinases are of particular relevance as they play a crucial role in cellular division by controlling chromatids segregation. Mammalian genomes uniquely encode for three Aurora kinases, Aurora A, Aurora B, and Aurora C, while for other metazoans, including the frog, fruitfly and nematode, only Aurora A and B kinases are known. Human Auroras A–C are kinases of a size ranging from 309 to 403 amino acid residues that exhibit a relatively high sequence divergence between species. The maintenance of a functional balance between mitotic checkpoint proteins and Aurora A is essential for the proper progression through mitosis. Moreover, this kinase is a key regulatory component of the p53 pathway as its overexpression leads to increased p53 degradation, which facilitates oncogenic transformation. Aurora B also plays an essential role in chromosome segregation and cytokinesis and its kinase activity is required for bipolar chromosome orientation and condensation. Aurora C is expressed at a moderate level albeit about an order of magnitude lower than Aurora B in diploid human fibroblasts. In contrast, the level of Aurora C is elevated in several human cancer cell types. Auroras C and B protein expression is maximally elevated during the G2/M phase but their expression profiles in synchronized cells reveal differential temporal regulation through the cell cycle.
References
1.Bolanos-Garcia VM. Int J Biochem Cell Biol. 2005 Aug;37(8):1572-7.
References
1.Bolanos-Garcia VM. Int J Biochem Cell Biol. 2005 Aug;37(8):1572-7.
Cell Cycle/DNA Damage
ABC(12)
AChR(104)
Antifolate(12)
ATM/ATR(26)
Aurora Kinase(51)
CLK(15)
c-Myc(22)
DHFR(16)
DNA Alkylator(34)
DNA gyrase(11)
DNA Repair Protein(21)
DNA/RNA Synthesis(187)
DNA-PK(15)
GPR(97)
HDAC(152)
Hec1/Nek2(9)
Integrin(77)
LIM Kinase (LIMK)(7)
Mps1/TTK(2)
Nucleoside Antimetabolite/Analog(48)
Other Targets(4)
PAK(13)
PARP(67)
PLK(26)
Potassium Channel(146)
RAD51(1)
Rho(16)
ROCK(42)
Telomerase(12)
Topoisomerase(88)
Wee1(7)
Aurora Kinase
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CD532
产品货号 : M35289
cas no: 1639009-81-6
CD532 是一种有效的 Aurora A 激酶抑制剂,IC50 值为 45 nM。CD532 具有阻断 Aurora A 激酶活性和驱动 MYCN 降解的双重作用。CD532 还可以直接与 AURKA 相互作用并诱导整体构象转变。CD532 可用于癌症的研究。 -
TAS-119
产品货号 : M34717
cas no: 1453099-83-6
TAS-119 是一种有效的,选择性的,具有口服活性的 Aurora A 抑制剂,IC50 为 1.0 nM。TAS-119 对 Aurora A 的选择性高于其他蛋白激酶,包括 Aurora B (IC50 为 95 nM)。TAS-119 具有有效的抗肿瘤活性。 -
XU1
产品货号 : M34473
cas no: 53439-81-9
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. -
Aurora B inhibitor 1
产品货号 : M33019
cas no: 937276-52-3
Aurora B inhibitor 1 是一种 Aurora B (Aurora-1) 抑制剂,Ki 值 <0.010 uM。详细信息请参考专利文献 WO2007059299A1 中的化合物 1-3。 -
Ilorasertib hydrochloride
产品货号 : M32965
cas no: 1847485-91-9
Ilorasertib (ABT-348) hydrochloride 是一种有效的,具有口服活性和 ATP 竞争性的 aurora 抑制剂,对 aurora A, aurora B, aurora C 的 IC50 值分别为 116, 5, 1 nM。Ilorasertib hydrochloride 也是一种有效的 VEGF 和 PDGF 抑制剂。Ilorasertib hydrochloride 具有用于急性髓系白血病 (AML) 和骨髓增生异常综合征 (MDS) 的研究潜力。