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Item № 13967
CAS № 1561178-17-3
Purity ≥98%
product image
                (CAS 1561178-17-3)
     5 mg $123.00 0.00
     10 mg $204.00 0.00
     50 mg $763.00 0.00

Pricing updated 2019-07-17. Prices are subject to change without notice.


DOT1L is a protein methyltransferase (PMT). It is the only enzyme known to methylate histone 3 at lysine 79 (H3K79), where it catalyzes mono-, di-, and trimethylation.1 Proper DOT1L function is necessary for transcriptional activation of many genes, DNA damage repair, and cell cycle regulation.2 SGC0946 is a potent inhibitor of DOT1L (IC50 = 0.3 nM) developed by the Structural Genomics Consortium (SGC). It is over 100-fold selective over other PMTs. It is active in cells, reducing H3K79 dimethylation in A431 and MCF10A cells (IC50s = 2.6 and 8.8 nM, respectively). SGC0946 is a brominated analog of EPZ004777, an S-adenosylmethionine-competitive inhibitor of DOT1L.3 Both SGC0946 and EPZ004777 selectively kill mixed lineage leukemia (MLL) cells, in which DOT1L is aberrantly localized via interaction with an oncogenic MLL fusion protein.3 The negative control, SGC0649, for SGC0956 is also available exclusively through the SGC. You can submit a request to receive the negative control here.

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Technical Information
Formal Name
CAS Number
Molecular Formula
Formula Weight
A crystalline solid
242, 280 nm
InChI Code
InChI Key

Warning - this product is not for human or veterinary use.

Shipping & Storage
Room temperature in continental US; may vary elsewhere
≥ 2 years
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Additional Information

View the Cayman Structure Database for chemical structure definitions for many Cayman products

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Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data pack, and GC-MS data.

References & Product Citations
Product Description References

1. Bernt, K.M., and Armstrong, S.A. A role for DOT1L in MLL-rearranged leukemias Epigenomics 3(6), 667-670 (2011).

2. Nguyen, A.T., He, J., Taranova, O., et al. Essential role of DOT1L in maintaining normal adult hematopoiesis Cell Research 21(9), 1370-1373 (2011).

3. Yu, W., Chory, E.J., Wernimont, A.K., et al. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors Nat.Commun. 3, 1-12 (2012).

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