2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. TD-428

TD-428是由Cereblon配体和BRD4配体相连的PROTAC。TD-428 是一种高度特异的 BRD4 降解剂，DC50 为 0.32 nM。TD-428 是一种 BET PROTAC，其中 TD-106 (CRBN 配体) 连接到 JQ1 (BET 抑制剂)，TD-428 可有效诱导 BET 蛋白降解。

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TD-428 Chemical Structure

TD-428 Chemical Structure

CAS No. : 2334525-50-5

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规格 价格 是否有货
1 mg ￥2100
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5 mg ￥5310
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TD-428 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

TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50?of?0.32?nM[1]. TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation[1].

IC50 & Target[1]

BRD4

0.32 nM (DC50)

Cereblon

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CWR22R CC50
20.1 nM
Compound: TD-428; 21b
Antiproliferative activity against human 22Rv1 cells after 72 hrs by CelTiter-Glo reagent-based luminescence assay
Antiproliferative activity against human 22Rv1 cells after 72 hrs by CelTiter-Glo reagent-based luminescence assay
[PMID: 30684871]
体外研究
(In Vitro)

TD-428, which comprises TD-106 linked to a BET inhibitor, JQ1 efficiently induce BET protein degradation in the prostate cancer cell line 22Rv1[1].
TD-428 (0.01-10,000 nM; 72?hours) inhibits the proliferation of 22RV1 cells with a CC50?of??20.1?nM[1].
TD-428 (1 nM-10?μM; 12?hours) induces the degradation of BRD4, IKZF1, and IKZF3 proteins[1].

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

TD-428 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: 22RV1 cells
Concentration: 0.01, 0.1, 1, 10, 100, 1000, and 10000 nM
Incubation Time: 72 hours
Result: Inhibited cell proliferation with a CC50 of 20.1 nM.

Western Blot Analysis[1]

Cell Line: U266 cells
Concentration: 1 nM, 10 nM, 100 nM, 1000 nM, and 10 μM
Incubation Time: 12 hours
Result: Induced the degradation of BRD4, IKZF1, IKZF3 proteins.
分子量

879.38

Formula

C43H43ClN10O7S
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

TD-428 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:

TD-4282334525-50-5TD428TD 428PROTACsEpigenetic Reader DomainInhibitorinhibitorinhibit

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产品名称：
TD-428
目录号：
HY-114407
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