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SR-0813

Catalog No. T40229 CAS 2597186-19-9

SR-0813 is a potent and selective inhibitor of the YEATS domain in ENL/AF9. It has an IC 50 of 25 nM and EC 50 of 205 nM for the ENL YEATS domain and an IC 50 of 311 nM and EC 50 of 76 nM (CETSA) for the AF9 YEATS domain. SR-0813 exhibits over 100-fold lower affinity (Kd =3.5 μM) for MAP3K19 compared to ENL YEATS (Kd =30 nM). It can be utilized in acute leukemia research.

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SR-0813, CAS 2597186-19-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 116.00
5 mg	In stock	$ 289.00
10 mg	In stock	$ 478.00
25 mg	In stock	$ 913.00
50 mg	In stock	$ 1,260.00
100 mg	In stock	$ 1,680.00
1 mL * 10 mM (in DMSO)	In stock	$ 336.00

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Purity: 99.72%

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Description	SR-0813 is a potent and selective inhibitor of the YEATS domain in ENL/AF9. It has an IC 50 of 25 nM and EC 50 of 205 nM for the ENL YEATS domain and an IC 50 of 311 nM and EC 50 of 76 nM (CETSA) for the AF9 YEATS domain. SR-0813 exhibits over 100-fold lower affinity (Kd =3.5 μM) for MAP3K19 compared to ENL YEATS (Kd =30 nM). It can be utilized in acute leukemia research.
Targets&IC50	AF9 YEATS domain:311 nM (IC50), AF9 YEATS domain:76 nM (EC50), ENL YEATS domain:205 nM (EC50), ENL YEATS domain:25 nM (IC50), ENL YEATS domain:30 nM (Kd), MAP3K19:3.5 μM (Kd)
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.

Molecular Weight	496.62
Formula	C25H32N6O3S
CAS No.	2597186-19-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (100.68 mM)

References and Literature

1. Garnar-Wortzel L, et al. Chemical Inhibition of ENL/AF9 YEATS Domains in Acute Leukemia. ACS Cent Sci. 2021 May 26;7(5):815-830.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Histone Modification Compound Library Bioactive Compound Library Bioactive Compounds Library Max Epigenetics Compound Library

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Keywords

SR-0813 2597186-19-9 Chromatin/Epigenetic Epigenetic Reader Domain SR 0813 SR0813 inhibitor inhibit

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