1. Epigenetics PROTAC
  2. Epigenetic Reader Domain PROTACs
  3. TAT-PiET-PROTAC

TAT-PiET-PROTAC 是一种经蛋白水解靶向嵌合体 (PROTAC) 修饰的 TAT-PiET (HY-P10445),TAT-PiET 是一种靶向 BRD4 的超末端 (ET) 结构域的细胞穿透肽。TAT-PiET-PROTAC 能够降低 BRD4 和 JMJD6 的水平,并抑制细胞增殖。TAT-PiET-PROTAC 还能抵抗 ERα 阳性乳腺癌细胞的内分泌耐药性。TAT-PiET-PROTAC 可用于癌症的研究,如乳腺癌。

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Custom Peptide Synthesis

TAT-PiET-PROTAC

TAT-PiET-PROTAC Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445), which is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET-PROTAC can reduce BRD4 and JMJD6 levels and inhibit cell proliferation. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET-PROTAC can be used for the research of cancer, such as breast cancer[1].

IC50 & Target[1]

BRD4

 

VHL

 

体外研究
(In Vitro)

TAT-PiET-PROTAC (2.5-10 μM, 6-24 h) 可降低 MCF7 细胞中 BRD4 和 JMJD6 的水平[1]
TAT-PiET-PROTAC 能抑制 MCF7、T47D、MDA-MB231 和 BT549 细胞的增殖,其 EC50 值分别为 13.2、6.16、43.88 和 36.3 μM[1]
TAT-PiET-PROTAC (10 μM) 可抑制 MCF7 和 MDA-MB231 细胞的集落形成[1]
TAT-PiET-PROTAC (10 μM) 能抑制 MCF7 和 MDA-MB231 细胞的迁移[1]
TAT-PiET-PROTAC (10 μM, 6 h) 会降低 MCF7 和 MDA-MB-231 细胞中 c-Myc、N-myc 和 CCND1 的表达[1]
TAT-PiET-PROTAC (10 μM) 可提高对 Tamoxifen (HY-13757A) 耐药的 MCF7 和 T47D 细胞的敏感性[1]

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

Western Blot Analysis[1]

Cell Line: MCF7 cells
Concentration: 2.5, 5 and 10 μM
Incubation Time: 6, 12 and 24 h
Result: Reduced BRD4 and JMJD6 levels.

Western Blot Analysis[1]

Cell Line: MCF7 and MDA-MB-231 cells
Concentration: 10 μM
Incubation Time: 6 h
Result: Decreased expression of c-Myc, N-myc, and CCND1.
体内研究
(In Vivo)

TAT-PiET-PROTAC (25 mg/kg,腹腔注射,每 2 天一次) 在 MCF7/MDA-MB231 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: MCF7/MDA-MB231 tumor mice models[1]
Dosage: 25 mg/kg
Administration: Intraperitoneally injection, every 2 days
Result: Reduced tumor volume and weight.
Reduced BRD4 and JMJD6 levels.
Reduced c-Myc, N-myc, and CCND1 levels.
分子量

3316.85

Formula

C145H239N53O35S

Sequence

Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Arg-Asn-Gln-Lys-Phe-Lys-Cys-Gly-Glu-{Ahx}-Tyl-{Hyp}-Tyr-Ile

Sequence Shortening

YGRKKRRQRRRRNQKFKCGE-{Ahx}-Y-{Hyp}-YI

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
  • 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.

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产品名称:
TAT-PiET-PROTAC
目录号:
HY-P10446
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