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Submit ReviewMS 41 is a potent and selective degrader of Eleven-Nineteen Leukemia (ENL), a histone acylation reader crucial in sustaining oncogenic gene expression, especially in MLL-r (Mixed Lineage Leukemia-rearranged) leukemia. DC50 = 2.84 nM, 3.03 nM, 3.50 nM and 26.58 nM in SEMK2, Jurkat, MV4;11 and KASUMI1 cells, respectively.
Comprises an ENL-binding moiety (PFI-6) joined by a linker to VHL1-Me as the ligand for von Hippel-Lindau E3 ubiquitin ligase.
MS41 effectively inhibits leukemia cell proliferation and clonogenic ability in vitro and suppresses leukemia progression in a xenograft mouse model of MLL-r leukemia in vivo.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license
| M. Wt | 1031.28 |
| Formula | C56H70N8O9S |
| Storage | Store at -20°C |
| Purity | ≥97% |
| CAS Number | 2768610-97-3 |
| PubChem ID | 172407974 |
| InChI Key | XPICNVKPGAOVBF-VCNVHFLLSA-N |
| Smiles | O=C(N[C@H]1C2=CC(C(NCCCCCCCCCC(N[C@H](C(N3[C@H](C(N[C@@H](C)C4=CC=C(C=C4)C5=C(C)N=CS5)=O)C[C@@H](O)C3)=O)C(C)(C)C)=O)=O)=CC=C2CC1)C6=NOC(C7=CC(O)=C(C(N(C)C)=O)C=C7)=C6 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 103.13 | 100 |
The following data is based on the product molecular weight 1031.28. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.97 mL | 4.85 mL | 9.7 mL |
| 5 mM | 0.19 mL | 0.97 mL | 1.94 mL |
| 10 mM | 0.1 mL | 0.48 mL | 0.97 mL |
| 50 mM | 0.02 mL | 0.1 mL | 0.19 mL |
References are publications that support the biological activity of the product.
Xue et al (2024) A potent and selective ENL degrader suppresses oncogenic gene expression and leukemia progression. Sci.Adv. 10
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Keywords: MS 41, MS 41 supplier, MS41, potent, selective, degrader, ENL, eleven, nineteen, leukemia, oncogenesis, VHL, PROTAC, PROTACS, in, vivo, Other, Degraders, 8919, Tocris Bioscience
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This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia