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

MS115 TFA is a selective PRMT5/MEP50 PROTAC degrader, with DC50 values of 17.4 nM and 11.3 nM for PRMT5 and MEP50, respectively. MS115 TFA promotes PRMT5/MEP50 ubiquitination and degradation. MS115 TFA 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 TFA

MS115 TFA Chemical Structure

CAS No. : 3109377-61-6

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Other Forms of MS115 TFA:

MS115 TFA Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All Histone Methyltransferase Isoform Specific Products:

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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

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Description

MS115 TFA is a selective PRMT5/MEP50 PROTAC degrader, with DC50 values of 17.4 nM and 11.3 nM for PRMT5 and MEP50, respectively. MS115 TFA promotes PRMT5/MEP50 ubiquitination and degradation. MS115 TFA 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) TFA 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) TFA 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) TFA 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) TFA inhibits MDAMB468 cell proliferation with a gIC50 of 5.6 μM[1].
MS115 (serial dilutions; 5 days) TFA 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) TFA 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) TFA degrades PRMT5/MEP50 in MCF10A normal breast epithelial cells and PNT2 normal prostate epithelial cells[1].
MS115 (serial dilutions; 5-6 days) TFA 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 TFA 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.
Parmacokinetics
Species Dose Route Cmax Plasma Concentration
Mice[1] 50 mg/kg i.p. 17.5 μM >200 nM
In Vivo

MS115 (TFA) (50 mg/kg; i.p.; single dose) exhibits favorable mouse pharmacokinetic properties with rapid absorption and sustained plasma exposure 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: Achieved a peak plasma concentration (Cmax) of 17.5 μM at 0.5 hours post-administration.
Remained above 200 nM for up to 8 hours post-administration.
Molecular Weight

1372.53

Formula

C65H89F4N11O15S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(C(F)(F)F)=O.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)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (72.86 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 0.7286 mL 3.6429 mL 7.2858 mL
5 mM 0.1457 mL 0.7286 mL 1.4572 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 and light). 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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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 (sealed storage, away from moisture and light). 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 0.7286 mL 3.6429 mL 7.2858 mL 18.2145 mL
5 mM 0.1457 mL 0.7286 mL 1.4572 mL 3.6429 mL
10 mM 0.0729 mL 0.3643 mL 0.7286 mL 1.8215 mL
15 mM 0.0486 mL 0.2429 mL 0.4857 mL 1.2143 mL
20 mM 0.0364 mL 0.1821 mL 0.3643 mL 0.9107 mL
25 mM 0.0291 mL 0.1457 mL 0.2914 mL 0.7286 mL
30 mM 0.0243 mL 0.1214 mL 0.2429 mL 0.6072 mL
40 mM 0.0182 mL 0.0911 mL 0.1821 mL 0.4554 mL
50 mM 0.0146 mL 0.0729 mL 0.1457 mL 0.3643 mL
60 mM 0.0121 mL 0.0607 mL 0.1214 mL 0.3036 mL
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MS115 TFA 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:

MS1153109377-61-6MS 115MS-115PROTACsHistone MethyltransferasePRMT5MDA-MB-468 cellsubiquitin-proteasome systembreast cancerMDA-MB-453 human breast cancer cellsvon Hippel-Lindau (VHL) E3 ubiquitin ligaseprostate cancerMEP50/WDR77PC-3 human prostate cancer cellsInhibitorinhibitorinhibit

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