SGC 0946

Pricing Availability Delivery Time Qty
Cat.No. 4541 - SGC 0946 | C28H40BrN7O4
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% (HPLC)
Datasheet
Citations
Literature

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.

Licensing Information

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.

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.

Compound Libraries

SGC 0946 is also offered as part of the Tocriscreen Plus and Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 618.57
Formula C28H40BrN7O4
Storage Store at -20°C
Purity ≥99% (HPLC)
PubChem ID 56962337
InChI Key IQCKJUKAQJINMK-HUBRGWSESA-N
Smiles O[C@H]([C@H](O)[C@@H](CN(C(C)C)CCCNC(NC4=CC=C(C(C)(C)C)C=C4)=O)O3)[C@@H]3N1C2=C(C(N)=NC=N2)C(Br)=C1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 61.86 100
ethanol 61.86 100

Preparing Stock Solutions

The following data is based on the product molecular weight 618.57. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.62 mL 8.08 mL 16.17 mL
5 mM 0.32 mL 1.62 mL 3.23 mL
10 mM 0.16 mL 0.81 mL 1.62 mL
50 mM 0.03 mL 0.16 mL 0.32 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Yu et al (2012) Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat.Commun. 3 1288 PMID: 23250418


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View all Lysine Methyltransferase Inhibitors

Keywords: SGC0946 epigenetics DOT1L histone protein methyltransferase PKMTs H3K79me potent selective inhibitors inhibits leukemia MLL target genes Lysine Methyltransferases

Citations for SGC 0946

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Epigenetics

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Pathways for SGC 0946

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