2. PROTAC Epigenetics Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. PROTACs Epigenetic Reader Domain HSP
  4. Hsp70TAC BRD4 Degrader-1

Hsp70TAC BRD4 Degrader-1 是一种靶向 BRD4 的降解剂，KD 值为 0.22 μM。Hsp70TAC BRD4 Degrader-1 可借助 Hsp70 (KD: 5.13 μM) 形成三元复合物，通过泛素-蛋白酶体途径特异性高效降解胞内 BRD4 。Hsp70TAC BRD4 Degrader-1 具有较强的抗肿瘤增殖活性。Hsp70TAC BRD4 Degrader-1 可用于三阴性乳腺癌、多形性胶质母细胞瘤的相关研究。
(粉色: BRD4 配体 (HY-78695)；蓝色: HSP70 E3 连接酶配体；黑色: 连接子 (HY-B0236))。

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Hsp70TAC BRD4 Degrader-1

Hsp70TAC BRD4 Degrader-1 Chemical Structure

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Hsp70TAC BRD4 Degrader-1 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 HSP 亚型特异性产品:

查看所有亚型
HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Hsp70TAC BRD4 Degrader-1 is a PROTAC degrader targeting BRD4, with a KD value of 0.22 μM. Hsp70TAC BRD4 Degrader-1 forms a ternary complex with Hsp70 (KD: 5.13 μM), and specifically and efficiently degrades intracellular BRD4 via the ubiquitin-proteasome pathway. Hsp70TAC BRD4 Degrader-1 exhibits potent anti-tumor proliferative activity. Hsp70TAC BRD4 Degrader-1 can be used in studies related to triple-negative breast cancer and glioblastoma multiforme[1]. (Pink: BRD4 ligand (HY-78695); Blue: HSP70 E3 ligase ligand; Black: linker (HY-B0236)).

IC50 & Target[1]

BRD4

 

HSP70

 

体外研究
(In Vitro)

Hsp70TAC BRD4 Degrader-1 (compound SB-2) (0.01-10 μM; 8-24 h) 可在 U-87 MG 和 MDA-MB-231 细胞中以时间和剂量依赖、Hsp70 依赖的方式诱导 BRD4 的蛋白酶体降解，两种细胞中的 DC50 值分别为 0.55 μM 和 0.67 μM[1]。
Hsp70TAC BRD4 Degrader-1 (0.1-12 μM; 48 h) 可抑制 U-87 MG 细胞增殖，其 IC50 为 0.32 μM[1]。
Hsp70TAC BRD4 Degrader-1 (1-5 μM; 12 h) 可在 Hsp70 高表达肿瘤细胞中选择性降解 BRD4，但在 Hsp70 低表达细胞中无此作用[1]。

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

Hsp70TAC BRD4 Degrader-1 相关抗体:

Western Blot Analysis[1]

Cell Line: HEK293T, MEF, MDA-MB-231, U-87 MG, TE-1, MCF-7, U937
Concentration: 1, 5 μM
Incubation Time: 12 h
Result: Induced efficient BRD4 degradation in Hsp70-high expression tumor cells (MDA-MB-231, MCF-7, U-87 MG, U937), but caused negligible degradation in Hsp70-low expression cells (HEK293T, MEF, TE-1).
Showed degradation efficiency correlated with cellular Hsp70 expression levels.
分子量

930.62

Formula

C50H56ClN9O3S2
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

Hsp70TAC BRD4 Degrader-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

Hsp70TAC BRD4 Degrader-1PROTACsEpigenetic Reader DomainHSPHeat shock proteinsMycPARPtriple-negative breast cancerHsp70MDA-MB-231 cellsU-87 MG cellsubiquitin-proteasome systemBcl-2glioblastoma multiformeBRD4Inhibitorinhibitorinhibit

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