≥98% (HPLC)

5-Bromo-7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-beta-D-7H-Pyrrolo[2,3-d]pyrimidin-4-amine, 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-(tert-butyl)phenyl)urea
Empirical Formula (Hill Notation):
CAS Number:
Molecular Weight:
MDL number:
PubChem Substance ID:

Quality Level


≥98% (HPLC)




white to beige


DMSO: 20 mg/mL, clear

storage temp.


SMILES string




InChI key



5, 25 mg in glass bottle

Biochem/physiol Actions

SGC0946 is a potent and selective inhibitor of Histone H3-lysine79 (H3K79) methyltransferase DOT1L with an IC50 of 0.3 nM in a radioactive enzyme assay, and over 100-fold selectivity for DOT1L over other histone methyltransferases. In cell studies, SGC0946 reduces H3K79 dimethylation with an IC50 of 2.6 nM in A431 cells and 8.8 nM in MCF10A cells. SGC0946 was found to selectively kills cells transformed with the MLL-AF9 fusion oncogene in an in vitro model of leukemia. For full characterization details, please visit the SGC0946 probe summary on the Structural Genomics Consortium (SGC) website.

SGC0649 is the negative control for the active probe, SGC0946. To request a sample of the negative control from the SGC,
click here.

To learn about other SGC chemical probes for epigenetic targets, visit

Features and Benefits

SGC0946 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit

Other Notes

SGC0946 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the SGC0946 probe summary on the Chemical Probes Portal website.


Skull and crossbones

Signal Word


Hazard Statements

Precautionary Statements


UN 2811 6.1 / PGIII

WGK Germany


Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificate of Analysis

Certificate of Origin

Hao Zhang et al.
eLife, 9 (2020-10-02)
Aberrant HOXA9 expression is a hallmark of most aggressive acute leukemias, notably those with KMT2A (MLL) gene rearrangements. HOXA9 overexpression not only predicts poor diagnosis and outcome but also plays a critical role in leukemia transformation and maintenance. However, our...
Julia Gobl et al.
Vaccines, 8(2) (2020-04-05)
Epigenetic mechanisms have not been characterized in ticks despite their importance as vectors of human and animal diseases worldwide. Our investigation identifies and functionally characterizes the orthologue of S-adenosylmethionine (SAM) binding methyltransferase enzyme, disruptor of telomeric silencing 1-like (DOT1L) in...
Giovanni Nassa et al.
Science advances, 5(2), eaav5590-eaav5590 (2019-02-19)
Breast cancer (BC) resistance to endocrine therapy results from constitutively active or aberrant estrogen receptor α (ERα) signaling, and ways to block ERα pathway in these tumors are sought after. We identified the H3K79 methyltransferase DOT1L as a novel cofactor...
Kazuya Ishiguro et al.
Haematologica, 104(1), 155-165 (2018-09-02)
Epigenetic alterations play an important role in the pathogenesis in multiple myeloma, but their biological and clinical relevance is not fully understood. Here, we show that DOT1L, which catalyzes methylation of histone H3 lysine 79, is required for myeloma cell...
Dan Liu et al.
Nature communications, 9(1), 1739-1739 (2018-05-02)
Chemoresistance is a major unmet clinical obstacle in ovarian cancer treatment. Epigenetics plays a pivotal role in regulating the malignant phenotype, and has the potential in developing therapeutically valuable targets that improve the dismal outcome of this disease. Here we...
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