SGC 0946
Tocris Bioscience, part of Bio-Techne | Catalog # 4541
Highly potent and selective DOT1L inhibitor; cell permeable
Key Product Details
Description
Highly potent and selective DOT1L inhibitor; cell permeable
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
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.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Scheer A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 2019 PMID: 30604761
- Yu Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat.Commun. 2012 PMID: 23250418
Product Specific Notices for SGC 0946
For research use only
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