Cat. No. 4541
Chemical Name: 1-[3-[[[(2R,3S,4R,5R)-5-(4-Amino-5-
Biological ActivityPotent 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.
Structural Genomics Consortium (SGC) CollaborationThis 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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
Yu et al (2012) Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat.Commun. 3 1288. PMID: 23250418.
If you know of a relevant citation for this product please let us know.
Keywords: SGC 0946, supplier, SGC0946, epigenetics, DOT1L, histone, protein, methyltransferase, PKMTs, H3K79me, potent, selective, inhibitors, inhibits, leukemia, MLL, target, genes
Find multiple products by catalog number
New Products in this Area
Potent and selective G9a and GLP histone lysine methyltransferase inhibitor(R)-PFI 2 hydrochloride
Potent and selective SETD7 histone lysine methyltransferase inhibitorGGsTop
Inhibitor of γ-glutamyl transpeptidase (GGT)GPP 78 hydrochloride
NMPRTase inhibitor; also induces autophagyIWP L6
Potent Porcn inhibitor
Tocris Product News
SGC Epigenetic Probes
Introducing our new epigenetics probes provided in collaboration with the Structural Genomics Consortium (SGC).