ML364

製品コードS6748 バッチS674802

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₄H₁₈F₃N₃O₃S₂

分子量

517.54

CAS No.

1991986-30-1

Solubility (25°C)*

体外

DMSO

60 mg/mL (115.93 mM)

Ethanol

15 mg/mL (28.98 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

5%DMSO 1 Corn oil

3.0mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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	ML364 is a small molecule inhibitor of the deubiquitinase USP2 with an IC50 of 1.1 μM in a biochemical assay using an internally quenched fluorescent di-ubiquitin substrate.
in vitro	ML364 induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest in Mino and HCT116 cancer cell lines. ML364 is antiproliferative in cancer cell lines. ML364 also causes a decrease in homologous recombination-mediated DNA repair. It is inactive against caspase 6, caspase 7, MMP1, MMP9, and USP15, but does inhibit USP8 with an IC50 of 0.95 μM. In a panel of 102 kinases that included regulators of the cell cycle there is no binding observed to any of the enzymes tested using 10 μM ML364^[1].

製品説明

ML364 is a small molecule inhibitor of the deubiquitinase USP2 with an IC50 of 1.1 μM in a biochemical assay using an internally quenched fluorescent di-ubiquitin substrate.

in vitro

ML364 induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest in Mino and HCT116 cancer cell lines. ML364 is antiproliferative in cancer cell lines. ML364 also causes a decrease in homologous recombination-mediated DNA repair. It is inactive against caspase 6, caspase 7, MMP1, MMP9, and USP15, but does inhibit USP8 with an IC50 of 0.95 μM. In a panel of 102 kinases that included regulators of the cell cycle there is no binding observed to any of the enzymes tested using 10 μM ML364^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	LnCAP cells and MCF7 cells
	濃度	0-20 μM
	反応時間	24 h
	実験の流れ	ML364 promotes degradation of cyclin D1 in LnCAP cells and MCF7 cells. Cells are treated with ML364 for 24 h, and cyclin D1 protein levels are assessed by Western blotting using a tubulin control.

参考

[1] Davis MI, et al. J Biol Chem. 2016, 291(47):24628-24640.

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：

USP2 promotes experimental colitis and bacterial infections by inhibiting the proliferation of myeloid cells and remodeling the extracellular matrix network [ Cell Insight, 2022, 1(4):100047]	PubMed: 37192862
Epstein-Barr virus-encoded latent membrane protein 1 and B-cell growth transformation induces lipogenesis through fatty acid synthase [ J Virol, 2020, JVI.01857-20]	PubMed: 33208446

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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