MS108
MS108 is a selective VHL-based eleven-nineteen leukemia protein (ENL) PROTAC degrader with DC50 of 0.6 nM. MS108 recruits VHL E3 ligase to induce ENL degradation in a VHL- and ubiquitin-proteasome system (UPS)-dependent manner. MS108 degrades the ENL paralog AF9, which shares a highly conserved YEATS domain with ENL. MS108 suppresses proliferation of cancer cells.
(Pink: ENL ligand (HY-169094); Blue: VHL ligand (HY-170348); Black: linker (HY-W895436)).
For research use only. We do not sell to patients.
- Formula: C56H68N10O8S
- Molecular Weight:1041.27
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
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VHL |
ENL |
AF9 |
MS108 (1 nM-10 μM; 24 h) induces near-complete ENL degradation in MV4;11 cells, achieving 99% degradation at 1 μM after 24 h of treatment[1].
MS108 (0.049-50 nM; 24 h) potently induces concentration-dependent ENL degradation in MV4;11 cells (DC50 = 0.60 nM) and Jurkat cells (DC50 = 1.13 nM) with near-maximal degradation (Dmax >97%) after 24 h of treatment[1].
MS108 (30 nM; 10 min-72 h) rapidly induces time-dependent ENL degradation in MV4;11 cells (detectable within 10 min) and Jurkat cells (detectable within 20 min), with sustained degradation for up to 72 h at 30 nM[1].
MS108 degrades ENL in MV4;11 cells in a VHL- and ubiquitin-proteasome system-dependent manner, without affecting ENL transcription[1].
MS108 potently inhibits the proliferation of MV4;11 (GI50 = 1.19 nM), RS4;11 (GI50 = 4.68 nM), KASUMI1 (GI50 = 5.89 nM), and SEMK2 (GI50 = 43.16 nM) leukemia cell lines[1].
MS108 (1-1000 nM; 24 h) is a highly selective degrader that efficiently targets ENL and AF9, but not YEATS2 or GAS41, in MV4;11 cells after 24 h of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4;11 human MLL-r leukemia cells, Jurkat cells
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Concentration:0.049, 0.098, 0.19, 0.39, 0.78, 1.56, 3.13, 6.25, 12.5, 25, 50 nM
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Incubation Time:24 h
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Result:Induced concentration-dependent ENL degradation in MV4;11 cells with a DC50 of 0.60 nM and a Dmax of 97.2%.
Induced concentration-dependent ENL degradation in Jurkat cells with a DC50 of 1.13 nM and a Dmax of 98.4%.
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Cell Line:MV4;11 human MLL-r leukemia cells
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Concentration:1, 10, 100, 1000 nM
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Incubation Time:24 h
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Result:Efficiently degraded both ENL and its paralog AF9 in a concentration-dependent manner.
Left levels of other YEATS domain-containing proteins YEATS2 and GAS41 unchanged.
Did not induce degradation of ENL or AF9 with MS108N and PFI-6 (HY-155412).
Chemical Information
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Molecular Weight 1041.27
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Formula C56H68N10O8S
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SMILES
O=C(N[C@@H]1CCC2=C1C=C(C=C2)C(NCCCCCCCCC3=CN(N=N3)[C@H](C(N4[C@@H](C[C@H](C4)O)C(N[C@@H](C)C5=CC=C(C=C5)C6=C(N=CS6)C)=O)=O)C(C)(C)C)=O)C7=NOC(C8=CC=C(C(O)=C8)C(N(C)C)=O)=C7
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)