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

MS8847 is a PROTAC degrader and antiproliferative agent targeting EZH2 (DC50=34.4 nM in EOL-1 MLL-rAML cells). MS8847 recruits the E3 ligase von Hippel-Lindau (VHL) to mediate the degradation of EZH2 via the ubiquitin-proteasome system. MS8847 induces antiproliferative effects in MLL-rearranged acute myeloid leukemia cells and inhibits the growth of triple-negative breast cancer cell lines or 3D triple-negative breast cancer models. MS8847 is applicable to research related to MLL-rearranged acute myeloid leukemia and triple-negative breast cancer.
(Pink: EZH2 ligand (HY-185582); Blue: VHL ligand (HY-125845); Black: linker (HY-W014831)).

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

MS8847

MS8847 Chemical Structure

CAS No. : 3050872-59-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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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 ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MS8847 is a PROTAC degrader and antiproliferative agent targeting EZH2 (DC50=34.4 nM in EOL-1 MLL-rAML cells). MS8847 recruits the E3 ligase von Hippel-Lindau (VHL) to mediate the degradation of EZH2 via the ubiquitin-proteasome system. MS8847 induces antiproliferative effects in MLL-rearranged acute myeloid leukemia cells and inhibits the growth of triple-negative breast cancer cell lines or 3D triple-negative breast cancer models. MS8847 is applicable to research related to MLL-rearranged acute myeloid leukemia and triple-negative breast cancer[1]. (Pink: EZH2 ligand (HY-185582); Blue: VHL ligand (HY-125845); Black: linker (HY-W014831)).

IC50 & Target

VHL

 

EZH2

 

Cellular Effect
Cell Line Type Value Description References
BT-549 IC50
1.45 μM
Compound: 8; MS8847
Anti-proliferative activity against human BT-549 cells assessed as cell growth inhibition measured after 5 days incubation by CCK-8 assay
Anti-proliferative activity against human BT-549 cells assessed as cell growth inhibition measured after 5 days incubation by CCK-8 assay
[PMID: 38295690]
EOL1 IC50
0.11 μM
Compound: 8; MS8847
Anti-proliferative activity against human EOL1 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay
Anti-proliferative activity against human EOL1 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay
[PMID: 38295690]
MDA-MB-468 IC50
0.45 μM
Compound: 8; MS8847
Anti-proliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 5 days incubation by CCK-8 assay
Anti-proliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 5 days incubation by CCK-8 assay
[PMID: 38295690]
MV4-11 IC50
0.17 μM
Compound: 8; MS8847
Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay
Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay
[PMID: 38295690]
RS4-11 IC50
0.41 μM
Compound: 8; MS8847
Anti-proliferative activity against human RS4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay
Anti-proliferative activity against human RS4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay
[PMID: 38295690]
In Vitro

MS8847 selectively targets EZH2-dependent cell growth and inhibits the proliferation of triple-negative breast cancer (TNBC) cells, with 5-day IC50 values of 1.45 μM (BT549) and 0.45 μM (MDA-MB-468), respectively. It also inhibits the proliferation of MLL-r AML cell lines, with 5-day IC50 values of 0.11 μM (EOL-1), 0.17 μM (MV4;11) and 0.41 μM (RS4;11), respectively[1].
MS8847 (0.1-1 μM; 24 h) completely degrades EZH2 protein in EOL-1 MLL-r AML cells[1].
MS8847 (1 nM-0.3 μM; 24 h) potently degrades EZH2 in a concentration-dependent manner in EOL-1 MLL-rAML cells, with a DC50 of 34.4 nM, and also degrades EED and SUZ12[1].
MS8847 (2.5-20 μM; 5 d) significantly inhibits cell growth and reduces spheroid size in a 3D in vitro BT549 TNBC model[1].

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

MS8847 Related Antibodies

Western Blot Analysis[1]

Cell Line: EOL-1 (MLL-r AML cell line)
Concentration: 1-1000 nM; 0.03-0.3 μM
Incubation Time: 24 h
Result: Achieved a half-maximal degradation concentration (DC50) of 34.4 nM for EZH2.
Potently degraded PRC2 core component EED, and degraded SUZ12 to a lesser extent.
Reduced the H3K27me3 mark.

Western Blot Analysis[1]

Cell Line: EOL-1 (MLL-r AML cell line)
Concentration: 300 nM
Incubation Time: 2 h; 4 h; 8 h; 12 h; 24 h; 48 h
Result: Initiated EZH2 degradation at 8 h and reached maximum degradation by 24 h.
Reduced the H3K27me3 mark over time.

Western Blot Analysis[1]

Cell Line: EOL-1 (MLL-r AML cell line)
Concentration: 0.03-0.3 μM (direct treatment); 0.5 μM (post 2 h pre-incubation with inhibitors/ligands)
Incubation Time: 24 h (direct treatment); 24 h (post 2 h pre-incubation with inhibitors/ligands)
Result: Effectively induced EZH2 degradation at 0.03, 0.1, 0.3 μM.
Rescued EZH2 degradation induction via pre-treatment with MLN4942, EPZ-6438, or VHL-1.
Failed to induce EZH2 degradation with negative controls MS8847N1 and MS8847N2.

Western Blot Analysis[1]

Cell Line: EOL-1, MV4;11, RS4;11 (MLL-r AML cell lines)
Concentration: 0.03-0.3 μM
Incubation Time: 24 h
Result: Induced complete EZH2 degradation at 0.1 and 0.3 μM in EOL-1 cells.
Induced near-complete EZH2 degradation at 0.03, 0.1, 0.3 μM in MV4;11 cells.
Induced EZH2 degradation at 0.1 and 0.3 μM in RS4;11 cells.

Western Blot Analysis[1]

Cell Line: BT549, MDA-MB-468 (TNBC cell lines)
Concentration: 0.1-3 μM
Incubation Time: 48 h
Result: Induced potent EZH2 degradation in both BT549 and MDA-MB-468 cells following 48 h treatment.
Parmacokinetics
Species Dose Route Cmax Plasma Concentration
Mice[1] 50 mg/kg i.p. 3.9 μM >1 μM
In Vivo

MS8847 (50 mg/kg; i.p.; single dose) achieves sustained plasma concentrations in male Swiss Albino mice and is well tolerated following a single 50 mg/kg intraperitoneal injection[1].

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

Animal Model: Swiss Albino (male)[1]
Dosage: 50 mg/kg
Administration: i.p.; single dose
Result: Observed a maximum plasma concentration (Cmax) of 3.9 μM at 4 hours.
Retained over 1 μM in plasma at 9 hours.
Exhibited no obvious clinical signs of toxicity at the tested dose.
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.

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In Vivo Dissolution Calculator
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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 MethyltransferaseBT549von Hippel-LindauRS4;11MLL-rearranged acute myeloid leukemiaEZH2EOL-1 MLL-r AML cellsMDA-MB-468triple-negative breast cancerubiquitin-proteasome systemMV4;11Inhibitorinhibitorinhibit

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