SGC 0946

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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)
Citations (1)
Protocols (1)

Biological Activity for SGC 0946

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.

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 for SGC 0946 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 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.

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
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 Data for SGC 0946

Solvent Max Conc. mg/mL Max Conc. mM
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.

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 for SGC 0946

Certificate of Analysis / Product Datasheet
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References for SGC 0946

References are publications that support the biological activity of the product.

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

Scheer et al (2019) A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 10 19 PMID: 30604761

If you know of a relevant reference for SGC 0946, please let us know.

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Keywords: SGC 0946, SGC 0946 supplier, SGC0946, epigenetics, DOT1L, histone, protein, methyltransferase, PKMTs, H3K79me, potent, selective, inhibitors, inhibits, leukemia, MLL, target, genes, Lysine, Methyltransferases, Other, 4541, Tocris Bioscience

1 Citation for SGC 0946

Citations are publications that use Tocris products. Selected citations for SGC 0946 include:

Christopher J et al (2022) Pharmacologic Targeting of TFIIH Suppresses KRAS-Mutant Pancreatic Ductal Adenocarcinoma and Synergizes with TRAIL. Cancer Res 82 3375-3393 PMID: 35819261

Do you know of a great paper that uses SGC 0946 from Tocris? Please let us know.

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Protocols for SGC 0946

The following protocol features additional information for the use of SGC 0946 (Cat. No. 4541).