UNC3866

Catalog No.S8359

UNC3866 Chemical Structure

Molecular Weight(MW): 795.02

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.

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Biological Activity

Description 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.
Targets
PRC1 chromodomains [1] CBX4 chromodomains [1] CBX7 chromodomains [1]
94 nM(Kd) 97 nM(Kd)
In vitro

UNC3866 is a potent antagonist of the CBX7-H3 interaction(IC50 = 66±1.2 nM). The affinity of UNC3866 for CBX2, -4, -6 and -8 is also surprisingly well correlated with the percent sequence identity of each chromodomain relative to that of CBX7. 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. UNC3866 antagonizes PRC1 chromodomains in cells. Thought the permeability of UNC3866 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. UNC3866 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 UNC3866 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 UNC3866 at higher doses for in vivo experiments is currently under investigation[1].

Protocol

Cell Research:

[1]

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  • Cell lines: PC3 cells
  • Concentrations: 30 μM
  • Incubation Time: 24 hours
  • Method:

    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.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: swiss albino mice
  • Formulation: --
  • Dosages: 10 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (125.78 mM)
Ethanol 46 mg/mL (57.86 mM)
Water 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.

Chemical Information

Molecular Weight 795.02
Formula

C43H66N6O8

CAS No. 1872382-47-2
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Related Antibodies

Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID