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Highly potent DOT1L methyltransferase inhibitor (Kd = 0.06 nM, IC50 = 0.3 nM in a radioactive assay); blocks H3K79 methylation in A431 cells and MCF10A cells. Inactive at 12 histone methyltransferases and DNMT1. Selectively kills cells transformed with the MLL-AF9 fusion oncogene in an in vitro model of leukemia; lowers levels of MLL target genes HOXA9 and Meis1.
To request the negative control for SGC0946, please fill out the SGC0649 request form on the SGC website.
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the SGC 0946 probe summary on the SGC website.
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of SGC 0946 is reviewed on the chemical probes website.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 618.57. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.62 mL||8.08 mL||16.17 mL|
|5 mM||0.32 mL||1.62 mL||3.23 mL|
|10 mM||0.16 mL||0.81 mL||1.62 mL|
|50 mM||0.03 mL||0.16 mL||0.32 mL|
References are publications that support the biological activity of the product.
Yu et al (2012) Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat.Commun. 3 1288 PMID: 23250418
Scheer et al (2019) A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 10 19 PMID: 30604761
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Keywords: SGC 0946, SGC 0946 supplier, SGC0946, epigenetics, DOT1L, histone, protein, methyltransferase, PKMTs, H3K79me, potent, selective, inhibitors, inhibits, leukemia, MLL, target, genes, Lysine, Methyltransferases, Other, 4541, Tocris Bioscience
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