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SGC0946

🥰Excellent
Catalog No. T3082Cas No. 1561178-17-3

SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.

SGC0946

SGC0946

🥰Excellent
Purity: 99.82%
Catalog No. T3082Cas No. 1561178-17-3
SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.
Pack SizePriceAvailabilityQuantity
2 mg$41In Stock
5 mg$63In Stock
10 mg$108In Stock
25 mg$251In Stock
50 mg$450In Stock
1 mL x 10 mM (in DMSO)$85In Stock
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Purity:99.82%
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Product Introduction

Bioactivity
Description
SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.
Targets&IC50
DOT1L:0.3 nM
In vivo
SGC 0946 significantly decreases di-methylation of H3K79 in A431 cells (IC50: 2.6 nM) and MCF10A cells (IC50: 8.8 nM), effectively and selectively killing cells with MLL translocations. Compared to its analogue EPZ004777, SGC 0946 is more potent against DOT1L, making it promising for cancer research. Moreover, SGC 0946 demonstrates over 100-fold higher selectivity for DOT1L than other histone methyltransferases (HMTs).
Kinase Assay
Determination of Inhibitor IC50 Values: EPZ004777 is serially diluted 3-fold in DMSO for a total of ten concentrations, beginning at 1 mM. A 1 μL aliquot of each inhibitor dilution is plated in a 384-well microtiter plate. The 100% inhibition control consisted of 2.5 mM ?nal concentration of the product inhibitor S-adenosyl-L-homocysteine, (SAH). Compound is incubated for 30 min with 40 ml per well of 0.25 nM DOT1L(1-416) in assay buffer (20 mM TRIS [pH 8.0] 10 mM NaCl, 0.002% Tween 20, 0.005% Bovine Skin Gelatin, 100 mM KCl, and 0.5 mM DTT). 10 ml per well of substrate mix comprising assay buffer with 200 nM 3H-SAM (American Radiolabeled Chemicals: 80 Ci/mmol), 600 nM unlabeled SAM, and 20 nM nucleosomes are added to initiate the reaction (both substrates are present in the ?nal reaction mixture at their respective KM values). Reactions are incubated for 120 min and quenched with 10 ml per well of 800 mM SAM. Incorporation of radioactivity into nucleosome substrate is measured in a ?ashplate. IC50 values for enzymes in the histone methyltransferase panel are determined under similar balanced assay conditions with both SAM and protein/peptide substrate present at concentrations equal to their respective KM values.
Chemical Properties
Molecular Weight618.57
FormulaC28H40BrN7O4
Cas No.1561178-17-3
SmilesCC(C)N(CCCNC(=O)Nc1ccc(cc1)C(C)(C)C)C[C@H]1O[C@H]([C@H](O)[C@@H]1O)n1cc(Br)c2c(N)ncnc12
Relative Density.1.48 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 93 mg/mL (150.3 mM)
Ethanol: 93 mg/mL (150.3 mM)
Solution Preparation Table
DMSO/Ethanol
1mg5mg10mg50mg
1 mM1.6166 mL8.0832 mL16.1663 mL80.8316 mL
5 mM0.3233 mL1.6166 mL3.2333 mL16.1663 mL
10 mM0.1617 mL0.8083 mL1.6166 mL8.0832 mL
20 mM0.0808 mL0.4042 mL0.8083 mL4.0416 mL
50 mM0.0323 mL0.1617 mL0.3233 mL1.6166 mL
100 mM0.0162 mL0.0808 mL0.1617 mL0.8083 mL

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