SGC 0946

Catalog No.S7079

For research use only.

SGC 0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM in a cell-free assay, is inactive against a panel of 12 PMTs and DNMT1.

SGC 0946 Chemical Structure

CAS No. 1561178-17-3

Selleck's SGC 0946 has been cited by 13 publications

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description SGC 0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM in a cell-free assay, is inactive against a panel of 12 PMTs and DNMT1.
Features Cell-active DOT1L-selective chemical probe.
Targets
DOT1L [1]
(Cell-free assay)
0.3 nM
In vitro

SGC 0946 is over 100-fold selective for other histone methyltransferases/HMTs. SGC 0946 potently reduces H3K79 dimethylation with IC50 of 2.6 nM in A431 cells, and 8.8 nM in MCF10A cells, which potently and selectively kills cells containing an MLL translocation. SGC 0946 is much more potent than its close analog EPZ004777, and serves as an excellent chemical probe for investigating DOT1L and further development of DOT1L inhibitors for cancer therapy. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MCF10A cells NEjuUmZHfW6ldHnvckBie3OjeR?= M4j0UGlvcGmkaYTpc44hd2ZiRF;UNWwhcW5iaIXtZY4hVUOIMUDBJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iCKM1u3PUBt\X[nbDygTWM2OD1yLkCwPFgh|ryP MX2yOVQxPjh3Mx?=
Assay
Methods Test Index PMID
Western blot DOT1L / H3K79me2 / CDK6 / Cyclin D3 28114995

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(161.66 mM)
Ethanol 100 mg/mL
(161.66 mM)
Water Insoluble

Chemical Information

Molecular Weight 618.57
Formula

C28H40BrN7O4

CAS No. 1561178-17-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)N(CCCNC(=O)NC1=CC=C(C=C1)C(C)(C)C)CC2C(C(C(O2)N3C=C(C4=C(N=CN=C43)N)Br)O)O

In vivo Formulation Calculator (Clear solution)

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% DMSO % % Tween 80 % ddH2O
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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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