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

Y-29794 是口服有效的非肽脯氨酰内肽酶 (PREP) 选择性抑制剂,IC50 为 3 nM, Ki 为 0.95 nM。Y-29794 可以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 通过抑制 IRS1-AKT-mTORC1 通路表现出抗癌活性。Y-29794 具有血脑屏障 (BBB) 通透性。

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Y-29794 Chemical Structure

Y-29794 Chemical Structure

CAS No. : 129184-48-1

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Other Forms of Y-29794:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

IC50 & Target

PREP

3 nM (IC50)

体外研究
(In Vitro)

Y-29794 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.

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 (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

418.66

Formula

C23H34N2OS2

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
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  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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.

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产品名称:
Y-29794
目录号:
HY-15113
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