SGC 0946

Name: SGC 0946
Brand: Tocris Bioscience
SKU: 4541

Tocris Bioscience a Bio-Techne Brand

Catalog # 4541

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Key Product Details

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)
Molecular Weight:	618.57

View Full Technical Details for SGC 0946

Biological Activity for SGC 0946

SGC 0946 is a highly potent DOT1L methyltransferase inhibitor (K_d = 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.

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.

Compound Libraries for SGC 0946

SGC 0946 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

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.

Technical Data for SGC 0946

M. Wt	618.57
Formula	C₂₈H₄₀BrN₇O₄
Storage	Store at -20°C
Purity	≥99% (HPLC)
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for SGC 0946

	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 will 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

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References for SGC 0946

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

Citations for SGC 0946

Please visit our Instrument Citation Database to search our collection of scientific articles that feature our instruments.