2. Metabolic Enzyme/Protease
  3. Prolyl Endopeptidase (PREP)
  4. Y-29794 tosylate

Y-29794 tosylate 是口服有效的非肽脯氨酰内肽酶 (PPCE) 选择性抑制剂，IC50 为 3 nM， Ki 为 0.95 nM。Y-29794 tosylate 增强促甲状腺激素释放激素 (TRH) 对大鼠海马体内 ACh 释放的作用，具有神经保护潜力。Y-29794 tosylate 通过抑制 IRS1-AKT-mTORC1 通路表现出抗癌活性。Y-29794 tosylate 具有血脑屏障 (BBB) 通透性。

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Y-29794 tosylate Chemical Structure

Y-29794 tosylate Chemical Structure

CAS No. : 143984-17-2

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Y-29794 tosylate 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Y-29794 tosylate is a selective, orally active inhibitor for non-peptide prolyl endopeptidase (PPCE), with an IC50 of 3 nM and a Ki of 0.95 nM. Y-29794 tosylate enhances the effect of thyrotropin-releasing hormone (TRH) on the release of ACh in the rat hippocampus, exhibits potential neuroprotective efficacy. Y-29794 tosylate exhibits anticancer activity through inhibition of the IRS1-AKT-mTORC1 pathway. Y-29794 tosylate penetrates the brain-blood barrier (BBB)[1][2].

IC50 & Target

PREP

3 nM (IC50)

体外研究
(In Vitro)

Y-29794 tosylate 抑制 TNBC 癌细胞 BT20、BT549、MDA453、DU4475、MDA 231、MDA468 和 SUM159PT 的增殖 (0-10 μM, 4 days), 在 G1/sub G1 期阻滞细胞周期 (0-10 μM, 48 h)，诱导细胞死亡 (5-10 mM)[1]。

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

Y-29794 tosylate 相关抗体:

Cell Proliferation Assay[1]

Cell Line: TNBC, BT20, BT549, MDA453, DU4475, MDA 231, MDA468, SUM159PT
Concentration: 0-10 μM
Incubation Time: 4 days
Result: Inhibited cell proliferation, induced cell death.

Cell Cycle Analysis[1]

Cell Line: MDA231, MDA468
Concentration: 0-10 μM
Incubation Time: 48 h
Result: Arrested cell cycle at G1 phase at 0-5 μM, arrested cell cycle at sub G1 phase at 5-10 μM.
体内研究
(In Vivo)

Y-29794 tosylate (12.5-50 mg/kg，腹腔注射，每天，每周 5 天，持续 5 周) 在 NOD-SCID 小鼠模型中表现出对三阴性乳腺癌的抗肿瘤活性，且无明显毒性[1]。

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

Animal Model: TNBC xenograft NOD-SCID mice model[1]
Dosage: 12.5-50 mg/kg
Administration: i.p., daily, 5 times a week for 5 weeks
Result: Inhibited tumor growth, maintained body weight.
分子量

590.86

Formula

C30H42N2O4S3
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

Y-29794 tosylate 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:

Y-29794143984-17-2Y29794Y 29794Prolyl Endopeptidase (PREP)prolyl oligopeptidasePOPanti-amnesicAlzheimer’s Diseasetriple-negative breast cancerTNBCBT20BT549MDA453DU4475MDA 231MDA468SUM159PTInhibitorinhibitorinhibit

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