Home Epigenetics Histone Methyltransferase inhibitor - DOT1 inhibitor SGC 0946 For research use only.

SGC 0946

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

SGC 0946 Chemical Structure

CAS No. 1561178-17-3

Purity & Quality Control

SGC 0946 Related Products

Signaling Pathway

Histone Methyltransferase Signaling Pathways

Histone Methyltransferase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MCF10A cells Function assay Inhibition of DOT1L in human MCF10A cells assessed as reduction of H3K79 level, IC50=0.0088 μM 25406853
Click to View More Cell Line Experimental Data

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
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 Research Cell lines Molm13 cell
Concentrations 1 µM
Incubation Time 4 days
Method

Cells were treated with indicated concentration of drug for 4 days.
Experimental Result Images Methods Biomarkers Images PMID
Western blot DOT1L / H3K79me2 / CDK6 / Cyclin D3 28114995
In Vivo
In vivo

SGC0946, a highly potent and selective DOT1L methyltransferase inhibitor, resulted in significant inhibition of tumor progression in the ovarian orthotopic xenograft mice model.

Chemical Information & Solubility

Molecular Weight 618.57 Formula

C28H40BrN7O4
CAS No. 1561178-17-3 SDF --
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (161.66 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

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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