2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. TKP-5

TKP-5 是一款靶向 BRD4 的 PROTAC 蛋白降解剂。TKP-5 可结合 BRD2、BRD3、BRD4 与 BRDT，其中前三者的 Ka 值分别为 150 nM、100 nM 和 150 nM。TKP-5 可抑制胸腺基质淋巴细胞生成素的产生，并下调 IL-33 mRNA 的表达。TKP-5 适用于胶带剥离诱导的皮肤损伤相关研究。
(粉色: Epigenetic Reader Domain 配体 (HY-182371)；蓝色: Cereblon 配体 (HY-10984)；黑色: 连接子)。

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TKP-5

TKP-5 Chemical Structure

CAS No. : 3076612-97-7

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TKP-5 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

TKP-5 is a PROTAC protein degrader targeting BRD4. TKP-5 can binds to BRD2, BRD3, BRD4 and BRDT, with Ka values of 150 nM, 100 nM and 150 nM for the first three proteins respectively. TKP-5 inhibits the production of thymic stromal lymphopoietin and suppresses the expression of IL-33 mRNA. TKP-5 is applicable to studies related to tape-stripping induced skin injury[1]. (Pink: Epigenetic Reader Domain ligand (HY-182371); Blue: Cereblon ligand (HY-10984); Black: linker).

体外研究
(In Vitro)

TKP-5 (0.1-10 μM; 2-24 h) 可强效降解 KCMH-1 细胞中的 BRD4，其 DC50 为 16.78 nM；在浓度低至 0.1 μM 时即可抑制 KCMH-1 细胞中 TSLP 的产生；在 1 μM 浓度下可选择性结合 BRD2、BRD3、BRD4 及 BRDT 的 BD1 结构域；并通过其三唑基团与 BRD4 的 Trp81 之间的相互作用，与 CRBN 和 BRD4-BD1 形成稳定的三元复合物[1]。
TKP-5 (处理 5 小时) 可在低于 100 nM 的浓度下诱导 KCMH-1 细胞中 BRD2、BRD3 和 BRD4 的降解[1]。

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

TKP-5 相关抗体:
体内研究
(In Vivo)

TKP-5 (1% (w/w)；局部给药；单次给药；6 小时) 可完全抑制 8 周龄雄性 ICR 小鼠中由胶带剥离诱导的皮肤损伤相关 IL-33 mRNA 表达[1]。

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

Animal Model: ICR (male, 8 weeks old, skin barrier disruption model via 10x tape-stripping)[1]
Dosage: 1% (w/w) (80 mg total)
Administration: topical; single application; 6 hours
Result: Completely suppressed skin injury-induced IL-33 mRNA expression, with levels reduced to near baseline values and significantly lower than both vehicle control and 1.2% TK-351 ointment groups.
分子量

833.88

Formula

C44H47N7O10
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

TKP-5 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

TKP-53076612-97-7TKP5TKP 5PROTACsEpigenetic Reader DomainBRD3ICR miceIL-33BRDTKCMH-1 cellsBRD4BRD2thymic stromal lymphopoietincereblonubiquitin-proteasome systemInhibitorinhibitorinhibit

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目录号：
HY-182370
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