2. PROTAC Metabolic Enzyme/Protease
  3. PROTACs E1/E2/E3 Enzyme
  4. MS181

MS181 (compound 1) is a potent cereblon (CRBN)-recruiting and EED-binding polycomb repressive complex 1 (PRC1) PROTAC degrader. MS181 decreases the expression of EED, EZH2, SUZ12, BMI1 and RING1B. MS181 shows antiproliferative activity (Strtucture Note: Red, EED binder (HY-158771); Blue, CRBN ligand (HY-41547); Black, Linker HY-131717).

For research use only. We do not sell to patients.

MS181 Chemical Structure

MS181 Chemical Structure

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MS181 Related Antibodies

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Description

MS181 (compound 1) is a potent cereblon (CRBN)-recruiting and EED-binding polycomb repressive complex 1 (PRC1) PROTAC degrader. MS181 decreases the expression of EED, EZH2, SUZ12, BMI1 and RING1B. MS181 shows antiproliferative activity (Strtucture Note: Red, EED binder (HY-158771); Blue, CRBN ligand (HY-41547); Black, Linker HY-131717)[1].

In Vitro

MS181 (compound 1) (0, 0.1, 0.3, 1, 3, 10 µM; 24 h) decreases the expression of EED, EZH2, SUZ12, BMI1 and RING1B in a dose dependent manner[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MS181 Related Antibodies

Western Blot Analysis[1]

Cell Line: K562 cells
Concentration: 0, 0.1, 0.3, 1, 3, 10 µM
Incubation Time: 24 h
Result: Decreassed the expression of EED, EZH2, SUZ12, BMI1 and RING1B, H3K27me3 in a dose dependent manner, showed no changes in the histone H3 lysine 27 trimethylation (H3K27me3) mark catalyzed by the PRC2 complex.
In Vivo

MS181 (50 mg/kg; i.p.; once) shows bioavailable in mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male swiss albino mice[1]
Dosage: 50 mg/kg
Administration: I.p.; once
Result: Showed above 1 μM for the first 2 h and maintained above 0.50 μM for 8 h post in the plasma concentration.
Molecular Weight

759.81

Formula

C39H41N11O6
SMILES

O=C(NCCCCN1CCN(C2=CC=C(C3=CN=C(N4C3=NN=C4)NCC5=CC=CO5)C=C2)CC1)CNC6=CC=CC(C(N7C8C(NC(CC8)=O)=O)=O)=C6C7=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MS181 Related Classifications

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The dilution calculator equation

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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:

MS181MS 181MS-181PROTACsE1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseMS181 was dissolved in 10% v/v NMP10% Solutol HS-1520% v/v PEG400and 60% normal saline[1].Inhibitorinhibitorinhibit

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MS181
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HY-158239
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