2. Epigenetics
  3. Histone Methyltransferase
  4. UNC3866

UNC3866 是一种有效的 CBX7-H3 拮抗剂，IC50 为 66±1.2 nM。

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UNC3866 Chemical Structure

UNC3866 Chemical Structure

CAS No. : 1872382-47-2

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规格 价格 是否有货 数量
2 mg ￥800
In-stock
5 mg ￥1000
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10 mg ￥1600
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25 mg ￥2960
In-stock
50 mg ￥4700
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200 mg   询价  

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UNC3866 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 2 篇科研文献

查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

UNC3866 is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen (IC50=66±1.2 nM) and is more than 100-fold selective for CBX7 over the other nine members of this methyl-lysine (Kme) reader panel.

IC50 & Target

IC50: 66±1.2 nM (CBX7)[1]
体外研究
(In Vitro)

UNC3866, a potent antagonist of the methyl-lysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. UNC3866 binds the chromodomains of CBX4 and CBX7 most potently with a Kd of 100 nM for each, and is 6- to 18-fold selective versus seven other CBX and CDY chromodomains while being highly selective versus >250 other protein targets. UNC3866 inhibits PC3 cell proliferation, a known CBX7 phenotype, while UNC4219, a methylated negative control compound, has negligible effects. UNC3866 is a potent and cellularly active antagonist of PRC1 chromodomains. UNC3866 is the most potent ligand reported for CBX7 with a Kd of 97±2.4 nM. UNC3866 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, UNC3866 is 65-fold selective for CBX4/7 over CDY1 and 9-fold selective for CBX4/7 over CDYL1b and CDYL2[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

UNC3866 相关抗体:
分子量

795.02

Formula

C43H66N6O8
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 27 mg/mL (33.96 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2578 mL 6.2891 mL 12.5783 mL
5 mM 0.2516 mL 1.2578 mL 2.5157 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (3.14 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (3.14 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献
Kinase Assay
[1]

The effect of UNC3866 on the methyltransferase activity of G9a, EHMT1, SUV39H1, SUV39H2, SETDB1, SETD8, SUV420H1, SUV420H2, SETD7, MLL1 trimeric complex, MLL3 tetrameric complex, EZH2 trimeric complex, PRMT1, PRMT3, PRMT5-MEP50 complex, PRMT6, PRMT7, PRMT8, PRDM9, SETD2, SMYD2, SMYD3, BCDIN3D and DNMT1 is assessed by monitoring the incorporation of tritium-labeled methyl group to lysine or arginine residues of peptide substrates using Scintillation Proximity Assay (SPA). Assays are performed in a 20 μL reaction mixture containing 3H-SAM at substrate concentrations close to the Km values for each enzyme. Three concentrations (1 μM, 10 μM, and 50 μM) of UNC3866 are used in all selectivity assays. To stop the enzymatic reactions, 7.5 M Guanidine hydrochloride is added, followed by 180 μL of buffer (20 mM Tris, pH 8.0). The reactions are mixed and then transferred to a 96-well FlashPlate. The reaction mixtures in Flash plates are incubated for 1 hour and the CPM are measured using a TopCount plate reader. The CPM counts in the absence of compound for each data set are defined as 100% activity. In the absence of the enzyme, the CPM counts in each data set are defined as background (0%)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

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, UNC3866 or UNC4219. For dose-response studies, the EC50 is derived from a six-point titration ranging from 100 μM to 0.4 μM of UNC3866 or UNC4219. 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 UNC3866- or UNC4219-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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

UNC3866 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2578 mL 6.2891 mL 12.5783 mL 31.4457 mL
5 mM 0.2516 mL 1.2578 mL 2.5157 mL 6.2891 mL
10 mM 0.1258 mL 0.6289 mL 1.2578 mL 3.1446 mL
15 mM 0.0839 mL 0.4193 mL 0.8386 mL 2.0964 mL
20 mM 0.0629 mL 0.3145 mL 0.6289 mL 1.5723 mL
25 mM 0.0503 mL 0.2516 mL 0.5031 mL 1.2578 mL
30 mM 0.0419 mL 0.2096 mL 0.4193 mL 1.0482 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

UNC38661872382-47-2UNC 3866UNC-3866Histone MethyltransferaseInhibitorinhibitorinhibit

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