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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C29H31N5O4 |
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分子量 | 513.59 | CAS No. | 331771-20-1 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (194.7 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc. |
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in vitro | In vitro, ZM-447439 selectively inhibits recombinant human Aurora A and B with IC50 values of 110 and 130 nM, respectively, while other protein kinases of diverse structural types including the mitotic kinases CDK1 and PLK1 are inhibited with IC50 values >10 μM. [1] Aurora kinase inhibitor, ZM-447439 time- and dose-dependently inhibits the growth of all three cell lines with IC50 values of 3 μM (BON), 0.9 μM (QGP-1) and 3 μM (MIP-101) after 72 hours of continuous exposure. In addition, ZM-447439 potently induces cell apoptosis by promoting DNA fragmentation and caspase 3 and 7 activation, and arrests GEP-NET cells in the G0 /G1and G2/M phase of the cell cycle. [2] In mouse embryo, inhibition of Aurora kinase activity by ZM-447439 results in abnormalities during mitosis by regulating the phosphorylation of histone H3 serine 10 (H3S10Ph) from G2 to metaphase with different perturbations in each embryonic cycle. [3] A recent study shows that ZM-447439 exhibits growth inhibitory and proapoptotic effect on cervical cancer SiHa cells, and enhances the chemosensitivity to cisplatin. [4] |
特徴 | An Aurora selective ATP-competitive inhibitor. |
キナーゼアッセイ | In vitro kinase assays | |
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Recombinant Aurora A and B are expressed as NH2-terminal His6-tagged fusion proteins using a baculovirus expression system. Aurora A is purified by affinity chromatography using Ni-NTA agarose, and Aurora B is purified by ion exchange chromatography using CM Sepharose Fast Flow. 1 ng purified recombinant enzyme is added to a reaction cocktail containing 25 mM Tris-HCl, pH 7.5, 12.5 mM KCl, 2.5 mM NaF, 0.6 mM DTT, 6.25 mM MnCl2, 10 μM peptide substrate, 10 μM for Aurora A or 5 μM ATP for Aurora B, and 0.2 μCi γ-[33P]ATP (specific activity ≥2,500 Ci/mmol), and is then incubated at RT for 60 minutes. Reactions are stopped by addition of 20% phosphoric acid, and the products are captured on P30 nitrocellulose filters and assayed for incorporation of 33P with a BetaplateTM counter. No enzyme and no compound control values are used to determine the concentration of ZM447439, which gave 50% inhibition of enzyme activity. Further details are available on request from Nicholas Keen. | ||
細胞アッセイ | 細胞株 | BON, QGP-1 and MIP-101 cells |
濃度 | 0-5 μM | |
反応時間 | 72 hours | |
実験の流れ | Cell number is evaluated by crystal violet staining. In brief, cells in 96-well plates are fixed with 1% glutaraldehyde. Then cells are stained with 0.1% crystal violet. The unbound dye is removed by washing with water. Bound crystal violet is solubilized with 0.2% Triton X-100. Light extinction which increases linearly with the cell number is analyzed at 570 nm using an ELISA reader. |
Data from [Mol Biol Cell, 2011, 22, 4227-35]
, , Dr. Yuanhong Chen of University of Nebraska
, , Dr. Zhang of Tianjin Medical University
Detection of senescence using machine learning algorithms based on nuclear features [ Nat Commun, 2024, 15(1):1041] | PubMed: 38310113 |
Human Endonuclease ANKLE1 Localizes at the Midbody and Processes Chromatin Bridges to Prevent DNA Damage and cGAS-STING Activation [ Adv Sci (Weinh), 2023, 10(12):e2204388] | PubMed: 36825683 |
Extra centrosomes induce PIDD1-mediated inflammation and immunosurveillance [ EMBO J, 2023, e113510.] | PubMed: 37530438 |
RIF1 suppresses the formation of single-stranded ultrafine anaphase bridges via protein phosphatase 1 [ Cell Rep, 2023, 42(2):112032] | PubMed: 36719798 |
Aberrant metabolite trafficking and fuel sensitivity in human pluripotent stem cell-derived islets [ Cell Rep, 2023, 42(8):112970] | PubMed: 37556323 |
DELs enable the development of BRET probes for target engagement studies in cells [ Cell Chem Biol, 2023, 30(8):987-998.e24] | PubMed: 37490918 |
PLK1 promotes the mitotic surveillance pathway by controlling cytosolic 53BP1 availability [ EMBO Rep, 2023, e57234.] | PubMed: 37888778 |
Mitotic DNA damage promotes chromokinesin-mediated missegregation of polar chromosomes in cancer cells [ Mol Biol Cell, 2023, 34(5):ar47] | PubMed: 36989031 |
Nuclear chromosome locations dictate segregation error frequencies [ Nature, 2022, 607(7919):604-609] | PubMed: 35831506 |
Pancreas agenesis mutations disrupt a lead enhancer controlling a developmental enhancer cluster [ Dev Cell, 2022, 57(16):1922-1936.e9] | PubMed: 35998583 |
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人間や獣医の診断であるか治療的な使用のためにでない。
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