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).

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MS181 Chemical Structure

MS181 Chemical Structure

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Based on 1 publication(s) in Google Scholar

MS181 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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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
Appearance

Solid

Color

Light yellow to yellow

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (131.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3161 mL 6.5806 mL 13.1612 mL
5 mM 0.2632 mL 1.3161 mL 2.6322 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.3161 mL 6.5806 mL 13.1612 mL 32.9030 mL
5 mM 0.2632 mL 1.3161 mL 2.6322 mL 6.5806 mL
10 mM 0.1316 mL 0.6581 mL 1.3161 mL 3.2903 mL
15 mM 0.0877 mL 0.4387 mL 0.8774 mL 2.1935 mL
20 mM 0.0658 mL 0.3290 mL 0.6581 mL 1.6451 mL
25 mM 0.0526 mL 0.2632 mL 0.5264 mL 1.3161 mL
30 mM 0.0439 mL 0.2194 mL 0.4387 mL 1.0968 mL
40 mM 0.0329 mL 0.1645 mL 0.3290 mL 0.8226 mL
50 mM 0.0263 mL 0.1316 mL 0.2632 mL 0.6581 mL
60 mM 0.0219 mL 0.1097 mL 0.2194 mL 0.5484 mL
80 mM 0.0165 mL 0.0823 mL 0.1645 mL 0.4113 mL
100 mM 0.0132 mL 0.0658 mL 0.1316 mL 0.3290 mL
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MS181 Related Classifications

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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