2597186-19-9
2597186-19-9 structure
- Name: SR-0813
- Chemical Name: SR-0813
- CAS Number: 2597186-19-9
- Molecular Formula: C25H32N6O3S
- Molecular Weight: 496.62
- Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
- Create Date: 2022-03-18 13:25:45
- Modify Date: 2024-01-28 13:18:50
-
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].
| Name | SR-0813 |
|---|
| 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]. |
|---|---|
| Related Catalog | |
| Target |
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]. 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. |
| References |
| Molecular Formula | C25H32N6O3S |
|---|---|
| Molecular Weight | 496.62 |