SGC 0946

Tocris Bioscience | Catalog # 4541

Highly potent and selective DOT1L inhibitor; cell permeable
Tocris Bioscience

Key Product Details

Description

Highly potent and selective DOT1L inhibitor; cell permeable
View all Lysine Methyltransferase Inhibitors »

Product Description

SGC 0946 is a 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. Enables generation of Chemically Induced Pluripotent Stem Cells (CiPSCs) from mouse embryonic fibroblasts (MEFs) (see protocol below).

To request the negative control for SGC0946, please fill out the SGC0649 request form on the SGC website.

For more information about how SGC 0946 may be used, see our protocol: Highly Efficient Generation of CiPSCs from MEFs

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.

Product Specifications for SGC 0946

Molecular Weight

618.57

Formula

C28H40BrN7O4

Storage

Store at -20°C

Purity

≥98% (HPLC)

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

CAS Number

1561178-17-3

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.

Solubility

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

Preparing Stock Solutions for SGC 0946

The following data is based on the product molecular weight 618.57.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all 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

Calculators

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Background References

References are publications that support the biological activity of the product. See our Citations tab to view 5 publications citing the usage of this product.

Product Documents for SGC 0946

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for SGC 0946

For research use only

Related Research Areas

Epigenetics

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