Hesperadin

製品コードS1529 バッチS152902

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₉H₃₂N₄O₃S

分子量

516.65

CAS No.

422513-13-1

Solubility (25°C)*

体外

DMSO

100 mg/mL (193.55 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	2.500mg/ml (4.84mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Hesperadin potently inhibits Aurora B with IC50 of 250 nM in a cell-free assay. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo.
in vitro	Hesperadin inhibits the ability of immunoprecipitated Aurora B to phosphorylate histone H3 with IC50 of 250 nM and markedly reduces the activity of other kinases (AMPK, Lck, MKK1, MAPKAP-K1, CHK1, and PHK) at a concentration of 1 μM. In contrast, only 20-100 nM of this compound is sufficient to induce the loss of mitotic histone H3-Ser10 phosphorylation in HeLa cells. Its treatment causes defects in mitosis and cytokinesis, leading to stoppage of proliferation of HeLa cells and polyploidization, which can be specifically ascribed to the inhibition of Aurora B function during the process of chromosome attachment. This compound (100 nM) quickly overrides the mitotic arrest induced by taxol or monastrol but not by nocodazole. It and nocodazole treatment in HeLa cells abolishes kinetochore localization of BubR1 and diminishes the intensity of Bub1 at kinetochores, suggesting that Aurora B function is required for efficient kinetochore recruitment of BubR1 and Bub1, which in turn might be necessary for prolonged checkpoint signaling. ^[1] It prevents the phosphorylation of recombinant trypanosome histone H3 by the T. brucei Aurora kinase-1 (TbAUK1) from pathogenic Trypanosoma brucei with IC50 of 40 nM in vitro kinase assays. This chemical significantly inhibits cell growth of cultured infectious bloodstream forms (BF) with IC50 of 48 nM, and only weakly inhibits cell growth of insect stage procyclic forms (PF) with IC50 of 550 nM. ^[2]

製品説明

Hesperadin potently inhibits Aurora B with IC50 of 250 nM in a cell-free assay. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo.

in vitro

Hesperadin inhibits the ability of immunoprecipitated Aurora B to phosphorylate histone H3 with IC50 of 250 nM and markedly reduces the activity of other kinases (AMPK, Lck, MKK1, MAPKAP-K1, CHK1, and PHK) at a concentration of 1 μM. In contrast, only 20-100 nM of this compound is sufficient to induce the loss of mitotic histone H3-Ser10 phosphorylation in HeLa cells. Its treatment causes defects in mitosis and cytokinesis, leading to stoppage of proliferation of HeLa cells and polyploidization, which can be specifically ascribed to the inhibition of Aurora B function during the process of chromosome attachment. This compound (100 nM) quickly overrides the mitotic arrest induced by taxol or monastrol but not by nocodazole. It and nocodazole treatment in HeLa cells abolishes kinetochore localization of BubR1 and diminishes the intensity of Bub1 at kinetochores, suggesting that Aurora B function is required for efficient kinetochore recruitment of BubR1 and Bub1, which in turn might be necessary for prolonged checkpoint signaling. ^[1] It prevents the phosphorylation of recombinant trypanosome histone H3 by the T. brucei Aurora kinase-1 (TbAUK1) from pathogenic Trypanosoma brucei with IC50 of 40 nM in vitro kinase assays. This chemical significantly inhibits cell growth of cultured infectious bloodstream forms (BF) with IC50 of 48 nM, and only weakly inhibits cell growth of insect stage procyclic forms (PF) with IC50 of 550 nM. ^[2]

プロトコル(参考用のみ)

キナーゼアッセイ	The Aurora B kinase assay
キナーゼアッセイ	For the Aurora B kinase assay, HeLa cells are lysed in a buffer containing 50 mM NaCl. The whole cell extract is spun at 13,000 rpm for 20 minutes at 4 °C using a table top centrifuge. The pellet obtained from 200 mg of whole cell extract is extracted again in 15 mL lysis buffer containing 250 mM NaCl in order to obtain active Aurora B kinase from mitotic chromatin. The low speed supernatant of the latter extract is used for immunoprecipitation. Monoclonal mouse anti–AIM-1, or mouse anti-HA, is coupled to GammaBind Plus Sepharose, and beads are rotated over-end in the extract for 90 minutes at 4 °C. Beads are washed, aliquoted, and washed in kinase buffer (20 mM Tris, pH 7.5, 150 mM NaCl, 10 mM MgCl₂, 1 mM DTT, 10 mM NaF). The kinase assay is performed with 10 μL beads in 20 μL kinase buffer containing 5 μg histone H3, 10 μM ATP, 2.5 μCi [γ-³²P]ATP, and different concentrations of this compound for 20 minutes at 37 °C. SDS sample buffer is added, and samples are boiled and resolved by SDS-PAGE. The gel is dried, and the radioactive signal is detected by PhosphorImager analysis. The data is analyzed using ImageQuant software.
細胞アッセイ	細胞株	HeLa cells and PtK1 cells
	濃度	Final concentration ~500 nM
	反応時間	24 and 48 hours
	実験の流れ	Cells are exposed to different concentrations of Hesperadin for 24 and 48 hours. At indicated time points, methanol-fixed cell samples are washed with PBS and subsequently stained in PI buffer (50 μg/mL propidium iodide, 10 mM Tris, pH 7.5, 5 mM MgCl₂, 200 μg/mL RNase A) for 20-40 minutes at 37 °C. The DNA content is determined by flow cytometry.

参考

https://pubmed.ncbi.nlm.nih.gov/12707311/
https://pubmed.ncbi.nlm.nih.gov/19320832/

カスタマーフィードバック

: Data from [Nat Commun, 2011, 2, 316]

: Data from [Nat Commun, 2011, 2, 316 ]

: ,

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Homologous recombination promotes non-immunogenic mitotic cell death upon DNA damage [ Nat Cell Biol, 2025, 27(1):59-72]	PubMed: 39805921
A CPC-shelterin-BTR axis regulates mitotic telomere deprotection [ Nat Commun, 2025, 16(1):2277]	PubMed: 40097392
Identification of chemical inhibitors targeting long noncoding RNA through gene signature-based high throughput screening [ Int J Biol Macromol, 2025, 292:139119]	PubMed: 39722392
Aurora B maintains spherical shape of mitotic cells via simultaneously stabilizing myosin II and vimentin [ J Mol Cell Biol, 2025, mjaf023]	PubMed: 40795355
Dynamic phosphorylation of FOXA1 by Aurora B guides post-mitotic gene reactivation [ Cell Rep, 2024, 43(9):114739]	PubMed: 39276350
Visualization strategies to aid interpretation of high-dimensional genotoxicity data [ Environ Mol Mutagen, 2024, 10.1002/em.22604]	PubMed: 38757760
Histone H3 phospho-regulation by KimH3 in both interphase and mitosis [ iScience, 2023, 26(4):106372]	PubMed: 37013187
Rsk2 and Lrp5 deficiency limit osteosarcoma growth in cFos-transgenic mice by different mechanisms [ ProQuest , 2023, 30683696]	PubMed: None
Hesperadin suppresses pancreatic cancer through ATF4/GADD45A axis at nanomolar concentrations [ Oncogene, 2022, 10.1038/s41388-022-02328-4]	PubMed: 35551503
CDC20-Mediated hnRNPU Ubiquitination Regulates Chromatin Condensation and Anti-Cancer Drug Response [ Cancers (Basel), 2022, 14(15)3732]	PubMed: 35954396

長期の保管のために-20°Cの下で製品を保ってください。

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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