2. Epigenetics
  3. Epigenetic Reader Domain
  4. SR-0813

SR-0813 is a potent and selective ENL/AF9 YEATS domain inhibitor. SR-0813 has IC50 and EC50 values of 25 nM and 205 nM for ENL YEATS domain, respectively. SR-0813 has IC50 and EC50 values of 311 nM and 76 nM (CETSA) for AF9 YEATS domain, respectively. SR-0813 binds MAP3K19 with over 100-fold lower affinity (Kd=3.5 μM) than ENL YEATS (Kd=30 nM). SR-0813 can be used for the research of acute leukemia.

For research use only. We do not sell to patients.

SR-0813 Chemical Structure

SR-0813 Chemical Structure

CAS No. : 2597186-19-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 186 In-stock
Solution
10 mM * 1 mL in DMSO USD 186 In-stock
Solid
5 mg USD 170 In-stock
10 mg USD 270 In-stock
25 mg USD 570 In-stock
50 mg USD 860 In-stock
100 mg USD 1300 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

SR-0813 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SR-0813 is a potent and selective ENL/AF9 YEATS domain inhibitor. SR-0813 has IC50 and EC50 values of 25 nM and 205 nM for ENL YEATS domain, respectively. SR-0813 has IC50 and EC50 values of 311 nM and 76 nM (CETSA) for AF9 YEATS domain, respectively. SR-0813 binds MAP3K19 with over 100-fold lower affinity (Kd=3.5 μM) than ENL YEATS (Kd=30 nM). SR-0813 can be used for the research of acute leukemia[1].

IC50 & Target[1]

ENL YEATS domain

25 nM (IC50)

ENL YEATS domain

205 nM (EC50)

AF9 YEATS domain

311 nM (IC50)

AF9 YEATS domain

76 nM (EC50)

ENL YEATS domain

30 nM (Kd)

MAP3K19

3.5 μM (Kd)

In Vitro

SR-0813 (compound 10; 0, 1, 10 μM; 4 h) dose-dependent evicts ENL from known ENL binding sites, including the HOXA10 gene body and MYB promoter in MV4;11 cells[1].
SR-0813 (0, 1, 10 μM; 0, 24, 48, 72 h) downregulates the transcript levels of HOXA9, MEIS1, and MYC, and increases the abundance of the ITGAM transcript in MV4;11 cells[1].
SR-0813 (0, 1, 10 μM; approximately 2 weeks) inhibits the growth of multiple lineage leukemia (MLL)-fusion leukemia cell lines (MV4;11, MOLM-13, OCI/AML-2) and HB11;19 cells[1].
SR-0813 (1 μM, 4h) does not elicit global changes in gene expression in MV4;11 cells, but produces a strikingly selective suppression of ENL target genes[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SR-0813 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MLL-fusion leukemia cell lines: MV4;11 (MLL-AF4 AML), MOLM-13 (MLL-AF9 AML), and OCI/AML-2 (MLL-AF6 AML), which are sensitive to the genetic loss of ENL.
HB11;19 cells, which harboring an MLL-ENL fusion.
Concentration: 0, 1, 10 μM
Incubation Time: Approximately 2 weeks
Result: Inhibited the growth of cells.
Molecular Weight

496.62

Formula

C25H32N6O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CN2C=C(C3=CC(NS(=O)(NCCN4CCCCC4)=O)=CC=C3)N=C2C=C1)NC5CCC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (201.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0136 mL 10.0681 mL 20.1361 mL
5 mM 0.4027 mL 2.0136 mL 4.0272 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.93%

SDS (252 KB)

COA (245 KB) HNMR (372 KB) LCMS (99 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0136 mL 10.0681 mL 20.1361 mL 50.3403 mL
5 mM 0.4027 mL 2.0136 mL 4.0272 mL 10.0681 mL
10 mM 0.2014 mL 1.0068 mL 2.0136 mL 5.0340 mL
15 mM 0.1342 mL 0.6712 mL 1.3424 mL 3.3560 mL
20 mM 0.1007 mL 0.5034 mL 1.0068 mL 2.5170 mL
25 mM 0.0805 mL 0.4027 mL 0.8054 mL 2.0136 mL
30 mM 0.0671 mL 0.3356 mL 0.6712 mL 1.6780 mL
40 mM 0.0503 mL 0.2517 mL 0.5034 mL 1.2585 mL
50 mM 0.0403 mL 0.2014 mL 0.4027 mL 1.0068 mL
60 mM 0.0336 mL 0.1678 mL 0.3356 mL 0.8390 mL
80 mM 0.0252 mL 0.1259 mL 0.2517 mL 0.6293 mL
100 mM 0.0201 mL 0.1007 mL 0.2014 mL 0.5034 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

SR-0813 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SR-08132597186-19-9SR0813SR 0813Epigenetic Reader DomainMV4;11 cellsMOLM-13 cellsOCI/AML-2 cellsHB11;19 cellsacute leukemiaInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
SR-0813
Cat. No.:
HY-145409
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.