UNC3866

製品コードS8359 バッチS835902

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

C₄₃H₆₆N₆O₈

分子量

795.02

CAS No.

1872382-47-2

Solubility (25°C)*

体外

DMSO

100 mg/mL (125.78 mM)

Ethanol

100 mg/mL (125.78 mM)

Water

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。	5.000mg/ml (6.29mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 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 clarify; 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.
Clear solution	5% DMSO 1 95% Corn oil 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。	0.830mg/ml (1.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 16.6 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	UNC3866 is a potent antagonist of the methyllysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. UNC3866 binds the chromodomains of CBX4 and CBX7 most potently, with a K(d) of ∼100 nM for each, and is 6- to 18-fold selective as compared to seven other CBX and CDY chromodomains.
in vitro	UNC3866 is a potent antagonist of the CBX7-H3 interaction(IC50 = 66±1.2 nM). The affinity of this compound for CBX2, -4, -6 and -8 is also surprisingly well correlated with the percent sequence identity of each chromodomain relative to that of CBX7. It is equipotent for CBX4, which is most similar to CBX7, while it is 18-, 6- and 12-fold selective for CBX4/7 over CBX2, -6 and -8, respectively. Additionally, this chemical is 65-fold selective for CBX4/7 over CDY1 and 9-fold selective for CBX4/7 over CDYL1b and CDYL2. This compound antagonizes PRC1 chromodomains in cells. Thought the permeability of it is low, it is sufficiently cell permeable and stable to evaluate its ability to engage and antagonize the functions of its chromodomain targets in cells. It inhibits PC3 cell proliferation ^[1].
in vivo	UNC3866 is the predominant species in plasma at all time points tested relative to UNC4007 and shows 25% bioavailability and moderate clearance. While these PK results are promising for a peptidic compound, the use of this compound in vivo may be limited because of the high circulating levels required for intracellular target engagement due to its poor cell permeability. The potential utility of this chemical at higher doses for in vivo experiments is currently under investigation^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	PC3 cells
	濃度	30 μM
	反応時間	24 hours
	実験の流れ	PC3 cells are seeded at 200 cells/well into 24-well plates. Cells are allowed to adhere overnight. The media (DMEM supplemented with 10 % FBS) is then exchanged with fresh media containing DMSO, UNC3866 or UNC4219. On day three, the media are exchanged with fresh media containing DMSO, this compound or this chemical. For dose-response studies, the EC50 is derived from a six-point titration ranging from 100 μM to 0.4 μM of this compound or this chemical. At day 0, 3 or 6, cells are fixed with ice-cold methanol for 30 sec. and rehydrated with PBS. Nuclei of the cells are stained with DAPI (0.05 μg/ml) and numerated using High Content Microscopy. For dose-response studies, the cell count of this compound- or this chemical-treated cells is normalized to the average cell count of DMSO-treated cells. The EC50 is calculated using the "log[inhibitor] vs. the normalized response -- Variable slope" equation in GraphPad Prism 5.
動物実験	動物モデル	swiss albino mice
	投薬量	10 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/26807715/

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：

Asxl1 C-terminal mutation perturbs neutrophil differentiation in zebrafish [ Leukemia, 2021, 10.1038/s41375-021-01121-8]	PubMed: 33483612
Asxl1 C-terminal mutation perturbs neutrophil differentiation in zebrafish [ Leukemia, 2021, 10.1038/s41375-021-01121-8]	PubMed: 33483612
CXCR4 Regulates Temporal Differentiation via PRC1 Complex in Organogenesis of Epithelial Glands [ Int J Mol Sci, 2021, 22(2)E619]	PubMed: 33435128

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。