SGC 0946

Catalog # Availability Size / Price Qty
4541/10
4541/50
Cat.No. 4541 - SGC 0946 | C28H40BrN7O4
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Description: Highly potent and selective DOT1L inhibitor; cell permeable

Chemical Name: 1-[3-[[[(2R,3S,4R,5R)-5-(4-Amino-5-bromo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl]methyl](isopropyl)amino]propyl]-3-[4-(2,2-dimethylethyl)phenyl]urea

Purity: ≥99%

Product Details
Reviews

Biological Activity

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.

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.

Technical Data

M.Wt:
618.57
Formula:
C28H40BrN7O4
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥99%
Storage:
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.

Additional Information

Licensing Caveats:
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.

Background References

  1. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
    Yu et al.
    Nat.Commun., 2012;3:1288

Product Datasheets

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