2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. MS479

MS479 是一种 BRD4 PROTAC 降解剂。MS479 与 BRD4-BD2 和 GLP 具有高亲和力结合 (BRD4-BD2：Kd = 200 nM；GLP：Kd = 306 nM)。MS479 可以降低 BRD4 短异构体的蛋白水平。MS479 通过直接结合其底物 GLP 作为桥接蛋白来募集 E3 连接酶 SPOP。MS479 可用于抑制结直肠癌细胞的增殖。(粉色：BRD4 配体 (HY-78695)；蓝色：GLP 配体 (HY-176036)；黑色：连接子 (HY-176037)；GLP 配体+连接子：HY-176038)。

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MS479 Chemical Structure

MS479 Chemical Structure

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MS479 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MS479 is a BRD4 PROTAC degrader. MS479 binds BRD4-BD2 and GLP with high affinities (BRD4-BD2: Kd = 200 nM; GLP: Kd = 306 nM). MS479 can reduce the protein level of BRD4 short isoform. MS479 recruits the E3 ligase SPOP by directly binding its substrate GLP as a bridge protein. MS479 can be used to inhibit the proliferation of colorectal cancer cells. (Pink: BRD4 ligand (HY-78695); Blue: GLP ligand (HY-176036); Black: linker (HY-176037); GLP ligand+linker: HY-176038)[1].

体外研究
(In Vitro)

MS479 (Compound 9) (0.5-5 μM，24 小时) 在 HT29 细胞系中表现出最佳的 BRD4 (S) 降解效果 (5 μM 时降解率 >50%)[1]。
MS479 (0.156-10 μM，24 小时) 对 BRD4 (L) 蛋白水平的影响相对较弱 (DC50 = 13.2 μM)，在 HT29 细胞系中 10 μM 时降解率约为 50%[1]。
MS479 (1-10 μM，24 小时) 通过翻译后机制调节 HT29 细胞系中的 BRD4 蛋白水平[1]。
MS479 (5 μM，24 小时) 表明，在 HT29 细胞系中，BRD4 (S) 的降解依赖于 BRD4、GLP、SPOP 和 UPS 的参与[1]。
MS479 (0.021-10 μM，72 小时) 在 HT29 细胞中表现出浓度依赖性的显著抗增殖作用(GI50 = 4.5 μM)，但对正常细胞无细胞毒性[1]。

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

MS479 相关抗体:

Western Blot Analysis[1]

Cell Line: HT29
Concentration: 1-10 μM
Incubation Time: 2-72 h
Result: Observed degradation of BRD4 (S) at 16 h and persisted up to 72 h.
Required longer time (48 h or longer) to degrade BRD4 (L), BRD3, and BRD2 effectively.
Reduced c-Myc protein level sharply after 2 h and completely abolished at 16 h.

Western Blot Analysis[1]

Cell Line: Biotin-MS479 (20 or 100 μM), parent BRD4 ligand (JQ1 (HY-13030), 1 μM), parent GLP ligand (MS1262, 1 μM) or a neddylation inhibitor (MLN4924 (HY-70062), 1 μM) pre-treated HT29 cell lines
Concentration: 5 μM
Incubation Time: 24 h
Result: Rescued BRD4 (S) degradation by pretreatment of HT29 cells.
Induced BRD4 degradation in HT29 cells, but the negative controls (MS479N1 and MS479N2) did not.
Showed BRD4 (S), BRD4 (L), and GLP all coeluted with SPOP in the presence of Biotin MS479, suggesting MS479 indeed induces the interaction between BRD4 and the GLP-SPOP complex.
分子量

1092.87

Formula

C59H82ClN11O5S
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

MS479 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

MS479MS 479MS-479PROTACsEpigenetic Reader DomainBRD4degraderPROTACGLPcolorectal cancer cellscancerInhibitorinhibitorinhibit

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