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

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5 mg USD 350 In-stock
10 mg USD 580 In-stock
25 mg USD 1100 In-stock
50 mg USD 1760 In-stock
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Based on 1 publication(s) in Google Scholar

SR-0813 Related Antibodies

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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.

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Purity & Documentation
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
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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

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