Home Epigenetics Histone Methyltransferase inhibitor - SETD inhibitor UNC0379 For research use only.

UNC0379

UNC0379 is a selective, substrate competitive inhibitor of N-lysine methyltransferase SETD8 with IC50 of 7.3 μM, high selectivity over 15 other methyltransferases.

UNC0379 Chemical Structure

UNC0379 Chemical Structure

CAS No. 1620401-82-2

Purity & Quality Control

UNC0379 Related Products

Signaling Pathway

Histone Methyltransferase Signaling Pathways

Histone Methyltransferase Signaling Pathway

Biological Activity

Description UNC0379 is a selective, substrate competitive inhibitor of N-lysine methyltransferase SETD8 with IC50 of 7.3 μM, high selectivity over 15 other methyltransferases.
Targets
SETD8 [1]
(Cell-free assay)
7.3 μM
In vitro
In vitro

UNC0379 is competitive with the peptide substrate and noncompetitive with the cofactor SAM. [1]
Kinase Assay Microfluidic Capillary Electrophoresis Assay
Inhibition of SETD8 methyltransferase activity is analyzed by monitoring decrease in methylation of the labeled peptide, TW21. The test compounds are solubilized in 100% DMSO to 10 mM and then plated in Greiner 384-well polypropylene plates using 3-fold dilution scheme over 10 points spanning the concentration range from 3 mM to 0.15 μM using TECAN Genesis liquid handler. Then 1 μL of the serial dilution is transferred into compound dilution plate using Nanoscreen MultiMek liquid handling robot. Prior to performing the assay the compounds are diluted 10-fold in 1× assay buffer (20 mM Tris, pH 8.0, 25 mM NaCl, 2 mM DTT, and 0.05% Tween-20), and an amount of 2.5 μL of the resulting dilution is transferred into assay plate by Nanoscreen MultiMek liquid handling robot. To this plate 20 μL of 50 nM SETD8 and 2 μM TW21 peptide cocktail in 1× assay buffer are added using multidrop liquid dispenser. Following a 10 min incubation of the compounds with the enzyme/peptide mix, the reaction is initiated by adding 2.5 μL of 150 μM SAM in 1× buffer. For 100% inhibition controls 1× buffer is added instead of SAM. The reaction is allowed to proceed at room temperature for 120 min, and then the reaction is terminated by adding 35 μL of 0.08 ng/μL Endo-LysC protease solution. Following an additional 1 h incubation the plate is read on a Caliper Life Sciences EZ reader II using upstream voltage −500 V, downstream voltage −1800 V, and pressure of −1.5 psi. The IC50 values are determined using Screenable Solutions software.
Cell Research Cell lines HEK293T cells
Concentrations 10 μM
Incubation Time 24 h
Method

Cells were treated with indicated concentration of drug for 24 h.
In Vivo
In vivo

UNC0379, a specific inhibitor of SET8 (a histone H4 lysine 20 (H4K20) , resulted in myofibroblast dedifferentiation may partly mitigate lung fibrosis without affecting the inflammatory responses.
Animal Research Animal Models Mice
Dosages 1 mg/kg
Administration i.t.

Chemical Information & Solubility

Molecular Weight 413.56 Formula

C23H35N5O2
CAS No. 1620401-82-2 SDF Download UNC0379 SDF
Smiles COC1=C(C=C2C(=C1)C(=NC(=N2)N3CCCC3)NCCCCCN4CCCC4)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 83 mg/mL ( (200.69 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 30 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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