SGC 0946

Catalog #: 4541
1 Citation Datasheet

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SGC 0946 | CAS No. 1561178-17-3 | Lysine Methyltransferase Inhibitors

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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%

View All Products for Lysine Methyltransferase Inhibitors

Product Details

Citations (1)

Reviews

Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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

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

M.Wt:

618.57

Formula:

C₂₈H₄₀BrN₇O₄

Solubility:

Soluble to 100 mM in DMSO and to 100 mM in ethanol

Purity:

≥99%

Storage:

Store at -20°C

CAS No:

1561178-17-3

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.

Additional Information

Licensing Caveats:

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.

Background References

A chemical biology toolbox to study protein methyltransferases and epigenetic signaling.
Scheer et al.
Nat.Commun., 2019;10:19
Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
Yu et al.
Nat.Commun., 2012;3:1288

Product Datasheets

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Citation for SGC 0946

The citations listed below are publications that use Tocris products. Selected citations for SGC 0946 include:

1 Citation: Showing 1 - 1

Pharmacologic Targeting of TFIIH Suppresses KRAS-Mutant Pancreatic Ductal Adenocarcinoma and Synergizes with TRAIL.
Authors: Christopher J Et al.
Cancer Res 2022;82:3375-3393

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