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SGC 0946 is a 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.
For more information about how SGC 0946 may be used, see our protocol: Highly Efficient Generation of CiPSCs from MEFs
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.
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.
SGC 0946 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
|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|
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
If you know of a relevant reference for SGC 0946, please let us know.
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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The following protocol features additional information for the use of SGC 0946 (Cat. No. 4541).