2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. 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)).

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MS108

MS108 Chemical Structure

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MS108 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

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[1]. (Pink: ENL ligand (HY-169094); Blue: VHL ligand (HY-170348); Black: linker (HY-W895436)).

IC50 & Target[1]

VHL

 

ENL

 

AF9

 

In Vitro

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.

MS108 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV4;11 human MLL-r leukemia cells, Jurkat cells
Concentration: 0.049, 0.098, 0.19, 0.39, 0.78, 1.56, 3.13, 6.25, 12.5, 25, 50 nM
Incubation Time: 24 h
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%.

Western Blot Analysis[1]

Cell Line: MV4;11 human MLL-r leukemia cells
Concentration: 1, 10, 100, 1000 nM
Incubation Time: 24 h
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).
Molecular Weight

1041.27

Formula

C56H68N10O8S
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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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MS108 Related Classifications

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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:

MS108MS 108MS-108PROTACsEpigenetic Reader DomainYEATS domainAF9acute myeloid leukemiavon Hippel-LindauENLJurkat cellsRS4;11 cellsVHL E3 ligaseubiquitin-proteasome systemMV4;11 cellsInhibitorinhibitorinhibit

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