2. PROTAC Epigenetics
  3. PROTACs Histone Methyltransferase
  4. MS115

MS115 is a selective PRMT5/MEP50 PROTAC degrader, with DC50 values of 17.4 nM and 11.3 nM for PRMT5 and MEP50, respectively. MS115 promotes PRMT5/MEP50 ubiquitination and degradation. MS115 shows anticancer activity against breast cancer.
(Pink: PRMT5 and MEP50 ligand (HY-173562); Blue: VHL ligand (HY-47070); Black: linker).

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MS115

MS115 Chemical Structure

CAS No. : 3109377-60-5

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Other Forms of MS115:

MS115 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

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Description

MS115 is a selective PRMT5/MEP50 PROTAC degrader, with DC50 values of 17.4 nM and 11.3 nM for PRMT5 and MEP50, respectively. MS115 promotes PRMT5/MEP50 ubiquitination and degradation. MS115 shows anticancer activity against breast cancer[1]. (Pink: PRMT5 and MEP50 ligand (HY-173562); Blue: VHL ligand (HY-47070); Black: linker).

In Vitro

MS115 (2.1 μM; 120 min) inhibits PRMT5 methyltransferase activity in a cell-free assay with an IC50 of 2.1 μM[1].
MS115 (0.01-5 μM; 3-72 h) potently and selectively degrades PRMT5 (DC50: 17.4 nM) and MEP50 (DC50: 11.3 nM) in MDAMB468 cells in concentration- and time-dependent manners, achieving >85% maximum degradation of both proteins[1].
MS115 (0.5-5 μM; 24-72 h, with 1-2 h pretreatment for mechanism assays) mediates PRMT5/MEP50 degradation in MDAMB468 cells that requires binding to both PRMT5 and VHL, and proceeds via the ubiquitin-proteasome system[1].
MS115 (serial dilutions; 7 days) inhibits MDAMB468 cell proliferation with a gIC50 of 5.6 μM[1].
MS115 (serial dilutions; 5 days) inhibits proliferation of MDAMB453, MDAMB231, and MCF7 breast cancer cells, with potency comparable to the PRMT5 inhibitor GSKi[1].
MS115 (0.004-5 μM; 7 h-3 days) potently degrades PRMT5/MEP50 in PC-3 prostate cancer cells, showing greater efficacy than the PRMT5 degrader MS4322[1].
MS115 (0.5-5 μM; 3 days) degrades PRMT5/MEP50 in MCF10A normal breast epithelial cells and PNT2 normal prostate epithelial cells[1].
MS115 (serial dilutions; 5-6 days) degrades PRMT5/MEP50 in normal epithelial cell lines (MCF10A, PNT2) without significant cytotoxicity[1].

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

MS115 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDAMB468 triple negative breast cancer cells
Concentration: 0.01-0.5 μM (72 h degradation assay); 0.5-5 μM (24 h degradation assay); 2 μM (time-dependent degradation assay)
Incubation Time: 3-48 h (2 μM time-dependent assay); 24 h (0.5-5 μM assay); 72 h (0.01-0.5 μM assay)
Result: Degraded PRMT5 with a DC50 of 17.4 nM and a maximum degradation (Dₘₐₓ) of 86.0 % after 72 h of treatment.
Degraded MEP50 with a DC50 of 11.3 nM and a Dₘₐₓ of 91.4 % after 72 h of treatment.
Induced time-dependent degradation, with PRMT5 degradation detectable by 6 h and MEP50 degradation detectable by 12 h of treatment with 2 μM MS115.
Reduced PRMT5 and MEP50 protein levels to near-undetectable levels at 0.5 μM, and eliminated detectable PRMT5 and MEP50 protein at 5 μM after 24 h of treatment.

Western Blot Analysis[1]

Cell Line: MDAMB468 triple negative breast cancer cells (including sgVHL and sgNTC CRISPR-modified cells)
Concentration: 0.5-5 μM (72 h degradation assay); 5 μM (24 h mechanism assay with 2 h GSKi/VHL-1 pretreatment); 5 μM (24 h mechanism assay with 1 h MG132/MLN4924 pretreatment); 0.5-5 μM (24 h sgVHL/sgNTC cell assay)
Incubation Time: 72 h (0.5-5 μM degradation assay); 24 h (5 μM mechanism assays, with 1-2 h pretreatment); 24 h (0.5-5 μM sgVHL/sgNTC cell assay)
Result: Reduced PRMT5 and MEP50 protein levels to near-undetectable levels and inhibited sDMA levels after 72 h of treatment with 5 μM MS115.
Rescued PRMT5 and MEP50 degradation when cells were pretreated with GSKi or VHL-1, confirming dependence on PRMT5 and VHL binding.
Rescued PRMT5 and MEP50 degradation when cells were pretreated with MG132 or MLN4924, confirming the ubiquitin-proteasome system is required for degradation.

Cell Viability Assay[1]

Cell Line: MDAMB468 triple negative breast cancer cells
Concentration: Serial dilutions
Incubation Time: 7 days
Result: Inhibited MDAMB468 cell proliferation with a growth inhibitory IC50 (gIC50) of 5.6 μM.

Western Blot Analysis[1]

Cell Line: PC-3 prostate cancer cells
Concentration: 0.004-2.5 μM (7 h degradation assay); 0.5-5 μM (3 days degradation and sDMA assay)
Incubation Time: 7 h (0.004-2.5 μM assay); 3 days (0.5-5 μM assay)
Result: Degraded PRMT5 and MEP50 at concentrations lower than MS4322, with detectable degradation at 0.004 μM and near-complete degradation at 2.5 μM after 7 h of treatment.
Reduced PRMT5 and MEP50 protein levels to near-undetectable levels and inhibited sDMA levels after 3 days of treatment with 5 μM MS115.

Western Blot Analysis[1]

Cell Line: MCF10A normal breast epithelial cells, PNT2 normal prostate epithelial cells
Concentration: 0.5-5 μM
Incubation Time: 3 days
Result: Completely degraded PRMT5 and MEP50 after 3 days of treatment with 5 μM MS115, and reduced PRMT5 and MEP50 to near-undetectable levels with 0.5 μM MS115 in MCF10A cells.
Significantly reduced PRMT5 and MEP50 protein levels after 3 days of treatment with 5 μM MS115 in PNT2 cells.

Cell Viability Assay[1]

Cell Line: MCF10A normal breast epithelial cells, PNT2 normal prostate epithelial cells
Concentration: Serial dilutions
Incubation Time: 5 days (MCF10A cells); 6 days (PNT2 cells)
Result: Showed no significant toxicity in MCF10A cells at concentrations up to 15 μM, with cell viability remaining >100% of control at all tested concentrations.
Showed minimal toxicity in PNT2 cells, with cell viability remaining >80% of control even at the highest tested concentration.
Molecular Weight

1258.50

Formula

C63H88FN11O13S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC[C@@H](CN1CC2=C(CC1)C=CC=C2)O)C3=NC=NC(NC4CCN(CC4)C(CCOCCOCCOCCOCCOCCNC(C[C@H](NC([C@H]5N(C[C@@H](C5)O)C([C@H](C(C)(C)C)NC(C6(CC6)F)=O)=O)=O)C7=CC=C(C=C7)C8=C(N=CS8)C)=O)=O)=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

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

Purity & Documentation
References
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MS115 Related Classifications

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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:

MS1153109377-60-5MS 115MS-115PROTACsHistone MethyltransferasePRMT5/MEP50 complexprostate cancerPRMT5breast cancerubiquitin-proteasome systemMEP50MDAMB468 cellsVHLbreast cancer cellsprostate cancer cellsInhibitorinhibitorinhibit

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