2. PROTAC Metabolic Enzyme/Protease
  3. PROTACs E1/E2/E3 Enzyme
  4. MS147

MS147 is a VHL-based PROTAC degrader of PRC1 (Polycomb Repressive Complex 1). The dissociation constants (Kd) of MS147 for EED (Embryonic Ectoderm Development) and VHL (Von Hippel-Lindau) are 3.0 μM and 450 nM, respectively. MS147 specifically binds to the EED protein through its EED-binding moiety; EED is a core component of PRC2 (Polycomb Repressive Complex 2) and interacts with the core components of PRC1, BMI1 (B-lymphoma Mo-MLV insertion region 1 homolog) and RING1B (Ring Finger Protein 1B). By this binding, MS147 is able to recruit BMI1 and RING1B near to VHL. Through the degradation of BMI1 and RING1B, MS147 reduces the level of H2AK119ub (histone H2A lysine 119 ubiquitination), affecting the proliferation of cancer cells. (Blue: VHL ligand (HY-125845), Black: linker ; Pink: PRC1 ligand (HY-158771)).

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MS147 Chemical Structure

MS147 Chemical Structure

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Description

MS147 is a VHL-based PROTAC degrader of PRC1 (Polycomb Repressive Complex 1). The dissociation constants (Kd) of MS147 for EED (Embryonic Ectoderm Development) and VHL (Von Hippel-Lindau) are 3.0 μM and 450 nM, respectively. MS147 specifically binds to the EED protein through its EED-binding moiety; EED is a core component of PRC2 (Polycomb Repressive Complex 2) and interacts with the core components of PRC1, BMI1 (B-lymphoma Mo-MLV insertion region 1 homolog) and RING1B (Ring Finger Protein 1B). By this binding, MS147 is able to recruit BMI1 and RING1B near to VHL. Through the degradation of BMI1 and RING1B, MS147 reduces the level of H2AK119ub (histone H2A lysine 119 ubiquitination), affecting the proliferation of cancer cells. (Blue: VHL ligand (HY-125845), Black: linker ; Pink: PRC1 ligand (HY-158771))[1].

Molecular Weight

1015.28

Formula

C54H70N12O6S
SMILES

O=C([C@H]1N(C([C@@H](NC(CCCCCCNC(CCCCN2CCN(C3=CC=C(C4=CN=C(NCC5=CC=CO5)N6C4=NN=C6)C=C3)CC2)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC7=CC=C(C8=C(C)N=CS8)C=C7
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
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References
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MS147 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:

MS147MS 147MS-147PROTACsE1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligasePRC1epigenetic inheritanceubiquitinationantitumor activityInhibitorinhibitorinhibit

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