2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. PROTAC BRD4 Degrader-39

PROTAC BRD4 Degrader-39 是一种选择性靶向 BRD4 的降解剂，其 DC50 值为 24.66 nM。PROTAC BRD4 Degrader-39 将 BRD PROTAC (ARV-771) (HY-100972) 与碳水化合物结合。PROTAC BRD4 Degrader-39 可选择性递送至高 GLUT1 表达的肿瘤细胞，随后在谷胱甘肽的触发下释放 ARV-771 并降解 BRD4。PROTAC BRD4 Degrader-39 能够抑制肿瘤生长，且无明显毒性。PROTAC BRD4 Degrader-39 可用于癌症研究，例如乳腺癌。(结构：粉色：BRD4 配体 (HY-78695)；蓝色：VHL 连接酶配体 (HY-112078)；黑色：连接子 (HY-42427)；BRD4 配体-Linker (HY-42429))

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PROTAC BRD4 Degrader-39

PROTAC BRD4 Degrader-39 Chemical Structure

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PROTAC BRD4 Degrader-39 相关抗体

Top Publications Citing Use of Products

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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

PROTAC BRD4 Degrader-39 is a selective targeting Bromodomain protein 4 (BRD4) degrader with an DC50 value of 24.66 nM. PROTAC BRD4 Degrader-39 conjugates BRD PROTAC (ARV-771) (HY-100972) with carbohydrate. PROTAC BRD4 Degrader-39 selectively delivers to tumor cells with high GLUT1 expression, followed by GSH-triggered release of ARV-771 and degrades BRD4. PROTAC BRD4 Degrader-39 can inhibit tumor growth and show no significant toxicity. PROTAC BRD4 Degrader-39 can be used for the research of cancer, such as breast cancer[1]. (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: VHL ligand (HY-112078); Black: (HY-42427); BRD4 ligand-Linker: (HY-42429))

IC50 & Target[1]

BRD4

24.66 nM (DC50)

VHL

 

体外研究
(In Vitro)

PROTAC BRD4 Degrader-39 (Compound NG-2) (0.01-10 μM, 3-48 h) 在 MDA-MB-231 细胞中以浓度和时间依赖性方式降解 BRD4[1]。
PROTAC BRD4 Degrader-39 在 MDA-MB-231 细胞中依赖葡萄糖转运蛋白和蛋白酶体降解 BRD4[1]。
PROTAC BRD4 Degrader-39 (5-5000 nM, 3 h) 在 MDA-MB-157、MCF-7、T-47D 和 BEAS-2B 细胞中降解 BRD4[1]。
PROTAC BRD4 Degrader-39 难以被 P-糖蛋白识别，因此在 Caco-2 细胞中能有效规避外排作用[1]。

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

PROTAC BRD4 Degrader-39 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.01, 0.1, 1 and 10 μM
Incubation Time: 3, 6, 12, 24 and 48 h
Result: Degraded BRD4 in a concentration- and time-dependent manner.
体内研究
(In Vivo)

PROTAC BRD4 Degrader-39 (Compound NG-2) (2.5 mg/kg，腹腔注射，每隔一天一次，共 14 次) 在 MDA-MB-231 肿瘤小鼠模型中可抑制肿瘤生长[1]。

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

Animal Model: MDA-MB-231 tumor mice models[1]
Dosage: 2.5 mg/kg
Administration: Intraperitoneally injection, every other day for 14 times
Result: Reduced tumor volume and weight.
Reduced BRD4 levles and Ki67-positive cells.
Had no changes of body weight, AST/ALT and BUN/Scr.
分子量

1410.10

Formula

C63H81ClN12O15S4
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

PROTAC BRD4 Degrader-39 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 *
= × ×

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:

PROTAC BRD4 Degrader-39PROTACsEpigenetic Reader DomainPROTACBRD4GLUT1Breast cancerMDA-MB-231MDA-MB-157MCF-7T-47DBEAS-2BInhibitorinhibitorinhibit

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目录号：
HY-175767
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