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SR-0813

Name: SR-0813
Brand: TargetMol
SKU: T40229
Price: 35 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T40229Cas No. 2597186-19-9

SR-0813 is a potent and selective inhibitor of the YEATS domain in ENL/AF9, with an IC50 of 25 nM and EC50 of 205 nM for the ENL YEATS domain, and an IC50 of 311 nM and EC50 of 76 nM (CETSA) for the AF9 YEATS domain. It shows over 100-fold lower affinity for MAP3K19 (Kd = 3.5 μM) compared to ENL YEATS (Kd = 30 nM). SR-0813 can be utilized in acute leukemia research.

SR-0813

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Purity: 98.81%

Catalog No. T40229Cas No. 2597186-19-9

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$35	In Stock	In Stock
5 mg	$83	In Stock	In Stock
10 mg	$133	In Stock	In Stock
25 mg	$281	In Stock	In Stock
50 mg	$427	In Stock	In Stock
100 mg	$592	-	In Stock
200 mg	$783	-	In Stock
1 mL x 10 mM (in DMSO)	$91	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:98.81%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	SR-0813 is a potent and selective inhibitor of the YEATS domain in ENL/AF9, with an IC50 of 25 nM and EC50 of 205 nM for the ENL YEATS domain, and an IC50 of 311 nM and EC50 of 76 nM (CETSA) for the AF9 YEATS domain. It shows over 100-fold lower affinity for MAP3K19 (Kd = 3.5 μM) compared to ENL YEATS (Kd = 30 nM). SR-0813 can be utilized in acute leukemia research.
Targets&IC50	MAP3K19:3.5 μM (Kd), ENL YEATS domain:205 nM (EC50), ENL YEATS domain:25 nM (IC50), ENL YEATS domain:30 nM (Kd), AF9 YEATS domain:311 nM (IC50), AF9 YEATS domain:76 nM (EC50)
In vitro	SR-0813, also identified as compound 10, demonstrates a dose-dependent activity in expelling ENL from its known binding sites, including the HOXA10 gene body and MYB promoter within MV4;11 cells at concentrations of 0, 1, and 10 μM over 4 hours. Furthermore, it modulates gene expression in these cells by decreasing the levels of HOXA9, MEIS1, and MYC, while augmenting ITGAM transcript abundance across various time points of 0, 24, 48, and 72 hours at the same concentrations. Notably, at 1 μM for 4 hours, SR-0813 specifically suppresses ENL target genes without broadly altering global gene expression in MV4;11 cells. Over approximately two weeks, SR-0813 shows a marked ability to hinder the proliferation of multiple lineage leukemia (MLL)-fusion leukemia cell lines, including MV4;11, MOLM-13, and OCI/AML-2, in addition to HB11;19 cells, all of which exhibit sensitivity to ENL genetic loss, at concentrations of 0, 1, and 10 μM. This is evidenced in the Cell Proliferation Assay, highlighting SR-0813's potential in targeting MLL-fusion leukemias that harbor ENL dependencies.

Chemical Properties

Molecular Weight	496.62
Formula	C₂₅H₃₂N₆O₃S
Cas No.	2597186-19-9
Smiles	C(NC1CCC1)(=O)C2=CN3C(=NC(=C3)C4=CC(NS(NCCN5CCCCC5)(=O)=O)=CC=C4)C=C2
Relative Density.	1.41 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (100.68 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.03 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0136 mL	10.0681 mL	20.1361 mL	100.6806 mL
5 mM	0.4027 mL	2.0136 mL	4.0272 mL	20.1361 mL
10 mM	0.2014 mL	1.0068 mL	2.0136 mL	10.0681 mL
20 mM	0.1007 mL	0.5034 mL	1.0068 mL	5.0340 mL
50 mM	0.0403 mL	0.2014 mL	0.4027 mL	2.0136 mL
100 mM	0.0201 mL	0.1007 mL	0.2014 mL	1.0068 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc