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UNC 0631

Catalog No. T2354Cas No. 1320288-19-4
Alias UNC0631

UNC 0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).

UNC 0631

UNC 0631

Purity: 98.76%
Catalog No. T2354Alias UNC0631Cas No. 1320288-19-4
UNC 0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).
Pack SizePriceAvailabilityQuantity
1 mg$42In Stock
5 mg$98In Stock
10 mg$156In Stock
25 mg$313In Stock
50 mg$493In Stock
100 mg$718In Stock
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Purity:98.76%
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Product Introduction

Bioactivity
Description
UNC 0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).
Targets&IC50
G9a:4 nM
Kinase Assay
SAHH-coupled assays: This assay utilizes SAHH to hydrolyze the methyltransfer product SAH to homocysteine and adenosine in the presence of adenosine deaminase which converts adenosine to inosine. The homocysteine concentration is then determined through conjugation of its free sulfhydryl moiety to a thiol-sensitive fluorophore, ThioGlo. For IC50 determinations, assay mixtures are prepared in 25 mM potassium phosphate buffer pH 7.5, 1 mM EDTA, 2 mM MgCl2, 0.01% Triton X-100 with 5 μM SAHH, 0.3 U/mL of adenosine deaminase, 25 μM SAM, and 15 μM ThioGlo. G9a, GLP, SETD7, SETD8, PRMT3 and SUV39H2 are assayed at 25 nM, 100 nM, 200 nM, 250 nM, 500 nM and 100 nM, respectively. Inhibitors are added at concentrations ranging from 4 nM to 16 μM. After 2 min incubation, reactions are initiated by addition of the histone peptides: 10 μM H3(1–25) for G9a, 20 μM H3(1–25) for GLP, 100 μM H3(1–25) for SETD7, 500 μM H4(1–24) for SETD8, 10 μM H4(1–24) for PRMT3 and 200 μM H3K9Me1 (1–15) for SUV39H2. The methylation reaction is followed by monitoring the increase in fluorescence using Biotek Synergy2 plate reader with 360/40 nm excitation filter and 528/20 nm emission filter for 20 min in 384 well-plate format. Activity values are corrected by subtracting background caused by the peptide or the protein. IC50 values are calculated using Sigmaplot. Standard deviations are calculated from two independent experiments.
Cell Research
MDA-MB-231, PC3, HCT116 cells are cultured in RPMI with 10% FBS, 22RV1 cells in alphaMEM and 10% FBS, MCF7 and IMR90 cells in DMEM with 10% FBS. Cells are treated with inhibitors for 48 h. The media is removed and replaced with DMEM 10% FBS without phenol red supplemented with 1 mg/mL of MTT and incubated for 1–2 h. Live cells reduce yellow MTT to purple formazan. The resulting formazanis solubilized in acidified isopropanol and 1% Triton. Formazan signal absorbance is measured at 570 nm and corrected for the 650 nm background. IC50s are calculated using GraphPad Prizm statistical package with sigmoidal variable slope dose response curve fit.(Only for Reference)
AliasUNC0631
Chemical Properties
Molecular Weight635.93
FormulaC37H61N7O2
Cas No.1320288-19-4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
Ethanol: 5 mg/mL (7.86 mM), Heating is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 100 mg/mL (157.25 mM), Heating is recommended.
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.5725 mL7.8625 mL15.7250 mL78.6250 mL
5 mM0.3145 mL1.5725 mL3.1450 mL15.7250 mL
DMSO
1mg5mg10mg50mg
10 mM0.1573 mL0.7863 mL1.5725 mL7.8625 mL
20 mM0.0786 mL0.3931 mL0.7863 mL3.9313 mL
50 mM0.0315 mL0.1573 mL0.3145 mL1.5725 mL
100 mM0.0157 mL0.0786 mL0.1573 mL0.7863 mL

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