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SGC0946

Chemical Structure : SGC0946

CAS No.: 1561178-17-3

SGC0946 (SGC-0946)

Catalog No.: PC-49325Not For Human Use, Lab Use Only.

SGC0946 (SGC-0946) is a potent, selective inhibitor of protein methyltransferase DOT1L with KD value of 0.06 nM and IC50 of 0.3 nM, reduces the level of methylation of H3K79 in MCF10A cells with IC50 of 8.8 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

SGC0946 (SGC-0946) is a potent, selective inhibitor of protein methyltransferase DOT1L with KD value of 0.06 nM and IC50 of 0.3 nM, reduces the level of methylation of H3K79 in MCF10A cells with IC50 of 8.8 nM.
SGC0946 is inactive against a panel of 12 protein methyltransferases (PMTs), DNMT1 and PRMT5. SGC0946 is more potent than EPZ004777.
SGC0946 reduced H3K79 methylation and proliferation of MYCN gene-amplified neuroblastoma cells.
SGC0946 displayed selective reduction of cell viability in an experimental leukaemia model derived from human cord blood cells transformed with the MLL-AF9 fusion oncogene, without apparent effect on the viability of cells transformed with an MLL-unrelated translocation (TLS-ERG).
SGC0946 (1 μM) effectively lowered the levels of MLL target genes, HOXA9 and Meis1.

Physicochemical Properties

M.Wt 618.577
Formula C28H40BrN7O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Yu W, et al. Nat Commun. 2012;3:1288.

2. Wong M, et al. Cancer Res. 2017 May 1;77(9):2522-2533.

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