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

MS115 TFA 是一种选择性的 PRMT5/MEP50 PROTAC 降解剂，在 MDAMB468 细胞中，24 h 时对 PRMT5 和 MEP50 的 DC50 值分别为 17.4 nM 和 11.3 nM。MS115 TFA 抑制乳腺癌细胞增殖。

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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 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MS115 TFA is a selective PRMT5/MEP50 PROTAC degrader, with DC50 values of 17.4 nM and 11.3 nM for PRMT5 and MEP50 at 24 h in MDAMB468 cells, respectively. MS115 TFA inhibits the proliferation of breast cancer cells[1].

体外研究
(In Vitro)

MS115 (2.1 μM; 120 min) TFA 在无细胞实验中可抑制 PRMT5 甲基转移酶活性，其 IC50 为 2.1 μM[1]。
MS115 (0.01-5 μM; 3-72 h) TFA 可在 MDAMB468 细胞中以浓度和时间依赖的方式强效且选择性地降解 PRMT5 (DC50: 17.4 nM) 和 MEP50 (DC50: 11.3 nM)，对两种蛋白的最大降解率均可达 85%以上[1]。
MS115 (0.5-5 μM; 24-72 h, with 1-2 h pretreatment for mechanism assays) TFA 可介导 MDAMB468 细胞中 PRMT5/MEP50 的降解，该过程需要同时结合 PRMT5 与 VHL，并通过泛素-蛋白酶体系统进行[1]。
MS115 (serial dilutions; 7 days) TFA 可抑制 MDAMB468 细胞增殖，其 gIC50 为 5.6 μM[1]。
MS115 (serial dilutions; 5 days) TFA 可抑制 MDAMB453、MDAMB231 和 MCF7 乳腺癌细胞的增殖，其活性与 PRMT5 抑制剂 GSKi 相当[1]。
MS115 (0.004-5 μM; 7 h-3 days) TFA 可在 PC-3 前列腺癌细胞中强效降解 PRMT5/MEP50，其效力优于 PRMT5 降解剂 MS4322[1]。
MS115 (0.5-5 μM; 3 days) TFA 可在 MCF10A 正常乳腺上皮细胞和 PNT2 正常前列腺上皮细胞中降解 PRMT5/MEP50[1]。
MS115 (serial dilutions; 5-6 days) TFA 可在正常上皮细胞系 (MCF10A、PNT2) 中降解 PRMT5/MEP50，且无显著细胞毒性[1]。

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

MS115 TFA 相关抗体:

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.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Plasma Concentration
Mice[1] 50 mg/kg i.p. 17.5 μM >200 nM
体内研究
(In Vivo)

MS115 TFA (50 mg/kg；腹腔注射；单次) 在小鼠中具有良好的动力学特性，单次腹腔注射 50 mg/kg 后可快速吸收并维持持续的血浆暴露水平[1]。

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.
分子量

1372.53

Formula

C65H89F4N11O15S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MS115 TFA 相关分类

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  • 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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MS115 TFA
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