2. PROTAC Epigenetics
  3. PROTACs Histone Methyltransferase
  4. MS8847

MS8847 is a highly potent EZH2 PROTAC degrader that recruits the E3 ligase von Hippel-Lindau (VHL). MS8847 potently degrades EZH2 in a ubiquitin-proteasome system-dependent manner. MS8847 effectively inhibits the growth of acute myeloid leukemia (AML) and triple-negative breast cancer (TNBC) cells.

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MS8847 Chemical Structure

MS8847 Chemical Structure

CAS No. : 3050872-59-5

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Based on 1 publication(s) in Google Scholar

MS8847 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

MS8847 is a highly potent EZH2 PROTAC degrader that recruits the E3 ligase von Hippel-Lindau (VHL). MS8847 potently degrades EZH2 in a ubiquitin-proteasome system-dependent manner. MS8847 effectively inhibits the growth of acute myeloid leukemia (AML) and triple-negative breast cancer (TNBC) cells[1].

IC50 & Target[1]

VHL

 

EZH2

 

Molecular Weight

1239.65

Formula

C70H98N10O8S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=CC(C)=C(CNC(C2=C(C)C(N(C3CCOCC3)CC)=CC(C4=CC=C(CN5CCN(CCC(NCCCCCCCCCCC(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)C(N1)=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 (80.67 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 0.8067 mL 4.0334 mL 8.0668 mL
5 mM 0.1613 mL 0.8067 mL 1.6134 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.

  • Molarity Calculator

  • 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

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(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 0.8067 mL 4.0334 mL 8.0668 mL 20.1670 mL
5 mM 0.1613 mL 0.8067 mL 1.6134 mL 4.0334 mL
10 mM 0.0807 mL 0.4033 mL 0.8067 mL 2.0167 mL
15 mM 0.0538 mL 0.2689 mL 0.5378 mL 1.3445 mL
20 mM 0.0403 mL 0.2017 mL 0.4033 mL 1.0083 mL
25 mM 0.0323 mL 0.1613 mL 0.3227 mL 0.8067 mL
30 mM 0.0269 mL 0.1344 mL 0.2689 mL 0.6722 mL
40 mM 0.0202 mL 0.1008 mL 0.2017 mL 0.5042 mL
50 mM 0.0161 mL 0.0807 mL 0.1613 mL 0.4033 mL
60 mM 0.0134 mL 0.0672 mL 0.1344 mL 0.3361 mL
80 mM 0.0101 mL 0.0504 mL 0.1008 mL 0.2521 mL
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MS8847 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:

MS88473050872-59-5MS 8847MS-8847PROTACsHistone MethyltransferaseEZH2 PROTAC degradernon-canonical oncogenic functions of EZH2Inhibitorinhibitorinhibit

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