2. PROTAC Epigenetics
  3. PROTACs Histone Methyltransferase
  4. MS8815

MS8815 is a selective enhancer of zeste homolog 2 (EZH2) PROTAC degrader. MS8815 has inhibition activity for EZH2 with an IC50 value of 8.6 nM. MS8815 can be used for the research of triple-negative breast cancer (TNBC).

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

MS8815 Chemical Structure

MS8815 Chemical Structure

CAS No. : 2855085-25-3

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 748 In-stock
Solution
10 mM * 1 mL in DMSO USD 748 In-stock
Solid
5 mg USD 680 In-stock
10 mg USD 1100 In-stock
25 mg USD 2250 In-stock
50 mg USD 3500 In-stock
100 mg USD 5600 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

MS8815 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MS8815 is a selective enhancer of zeste homolog 2 (EZH2) PROTAC degrader. MS8815 has inhibition activity for EZH2 with an IC50 value of 8.6 nM. MS8815 can be used for the research of triple-negative breast cancer (TNBC)[1].

IC50 & Target

IC50: 8.6 nM (EZH2); 62 nM (EZH1)[1].
DC50: 140 nM (EZH2 in MDA-MB-453 cells)[1]
In Vitro

MS8815 shows potency in inhibiting the EZH2 and EZH1 methyltransferase activity with IC50 values of 8.6 nM and 62 nM, respectively[1].
MS8815 (0.1-1 μM) degrades EZH2 with a DC50 value of 140 nM in MDA-MB-453 cells[1].
MS8815 (1 μM; 48 h) induces robust EZH2 degradation in a concentration-, time-, and proteasome-dependent manner in TNBC cells[1].
MS8815 (0.1-10 μM; 5 days) effectively suppresses the cell growth in multiple TNBC cell lines and primary patient TNBC cells[1].

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

MS8815 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-453 cells and BT549 cells
Concentration: 0.3, 3 μM; 1μM
Incubation Time: 48 h; 24 h
Result: Induced nearly complete degradation of EZH2 and exhibited the most robust degradation at 0.3 μM.
Induced EZH2 degradation in a time-and concentration-dependent manner.
Induced EZH2 degradation through the UPS.

Cell Proliferation Assay[1]

Cell Line: BT549, MDA-MB-468, SUM159 and MDA-MB-453 cells
Concentration: 0.1-10 μM
Incubation Time: 5 days
Result: Showed superior cellular growth inhibition activity in a panel of TNBC cells.
Molecular Weight

1154.51

Formula

C65H87N9O8S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C=C(C)N1)=C(CNC(C2=C(C)C(N(CC)C3CCOCC3)=CC(C4=CC=C(CN5CCN(C(CCCCCCCC(N[C@@H](C(C)(C)C)C(N6[C@H](C(NCC7=CC=C(C8=C(C)N=CS8)C=C7)=O)C[C@@H](O)C6)=O)=O)=O)CC5)C=C4)=C2)=O)C1=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 120 mg/mL (103.94 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 0.8662 mL 4.3308 mL 8.6617 mL
5 mM 0.1732 mL 0.8662 mL 1.7323 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 3.25 mg/mL (2.82 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  50% PEG300    50% Saline

    Solubility: 2.5 mg/mL (2.17 mM); Suspended solution; Need ultrasonic

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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.79%

COA (246 KB) HNMR (385 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
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 (sealed storage, away from moisture). 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 0.8662 mL 4.3308 mL 8.6617 mL 21.6542 mL
5 mM 0.1732 mL 0.8662 mL 1.7323 mL 4.3308 mL
10 mM 0.0866 mL 0.4331 mL 0.8662 mL 2.1654 mL
15 mM 0.0577 mL 0.2887 mL 0.5774 mL 1.4436 mL
20 mM 0.0433 mL 0.2165 mL 0.4331 mL 1.0827 mL
25 mM 0.0346 mL 0.1732 mL 0.3465 mL 0.8662 mL
30 mM 0.0289 mL 0.1444 mL 0.2887 mL 0.7218 mL
40 mM 0.0217 mL 0.1083 mL 0.2165 mL 0.5414 mL
50 mM 0.0173 mL 0.0866 mL 0.1732 mL 0.4331 mL
60 mM 0.0144 mL 0.0722 mL 0.1444 mL 0.3609 mL
80 mM 0.0108 mL 0.0541 mL 0.1083 mL 0.2707 mL
100 mM 0.0087 mL 0.0433 mL 0.0866 mL 0.2165 mL
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MS8815 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:

MS88152855085-25-3MS 8815MS-8815PROTACsHistone Methyltransferaseenhancer of zeste homolog 2 (EZH2)proteolysis targeting chimera (PROTAC)inhibitionantitumorriple-negative breast cancer (TNBC)Inhibitorinhibitorinhibit

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