2. Epigenetics
  3. Histone Methyltransferase
  4. UNC3866

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.

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Custom Peptide Synthesis

UNC3866 Chemical Structure

UNC3866 Chemical Structure

CAS No. : 1872382-47-2

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Based on 2 publication(s) in Google Scholar

Other Forms of UNC3866:

UNC3866 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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]
Cellular Effect
Cell Line Type Value Description References
PC-3 GI50
7.6 μM
Compound: UNC3866
Antiproliferative activity against human PC3 cells after 3 days by DAPI staining-based microscopic analysis
Antiproliferative activity against human PC3 cells after 3 days by DAPI staining-based microscopic analysis
[PMID: 28478342]
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].

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

UNC3866 Related Antibodies
Molecular Weight

795.02

Formula

C43H66N6O8
CAS No.
Appearance

Solid

Color

White to off-white

Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 27 mg/mL (33.96 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (3.14 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (3.14 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
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.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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UNC3866 Related Classifications

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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