2. PI3K/Akt/mTOR
  3. PIN1
  4. PIN1 degrader-3

PIN1 degrader-3 是一种 Pin1 (肽基脯氨酰异构酶蛋白) 降解剂 (IC50 = 4.65 nM)。PIN1 degrader-3 与 Pin1 共价结合。PIN1 degrader-3 可在体外使 Pin1 不稳定，从而导致其在细胞内降解。PIN1 degrader-3 可用于胰腺癌的研究。

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PIN1 degrader-3

PIN1 degrader-3 Chemical Structure

CAS No. : 3101950-55-1

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PIN1 degrader-3 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

PIN1 degrader-3 is a Pin1 (peptidyl-prolyl isomerase protein) (IC50 = 4.65 nM) degrader. PIN1 degrader-3 bound covalently to Pin1. PIN1 degrader-3-induced Pin1 degradation reduced cell viability, with EC50 values after 72 h of 8.4 μM in MIA PaCa-2 cells and 5.3 μM in KPC cell lines.PIN1 degrader-3 can destabilize Pin1 in vitro, causing its degradation in cells. PIN1 degrader-3 can be used for the study of pancreatic cancer[1].

IC50 & Target

Pin1

4.65 nM (IC50)

体外研究
(In Vitro)

PIN1 degrader-3 (Compound 164B8; Compound H-3-V) (250 μM，3 小时) 与 Pin1 结合，引起构象变化，影响 FG 环和 D 螺旋区域[1]。
PIN1 degrader-3 (0-15 μM，24 小时) 可有效诱导人胰腺癌细胞系 BxPC3 和小鼠胰腺癌细胞系 KPC 中 MIA PaCa-2 和 Pin1 的剂量依赖性降解[1]。
PIN1 degrader-3 (5 μM，24 小时) 诱导的 BxPC3 和 KPC 细胞系中 Pin1 的降解是可逆的[1]。
PIN1 degrader-3 (0.5-10 μM，24 小时) 可诱导所有癌相关成纤维细胞 (CAFs) (胆管癌的 CAF-BTG、阑尾癌的 CAF-APP 和结直肠癌的 CAF-COL) 中 Pin1 的剂量依赖性降解[1]。
PIN1 degrader-3 (72小时) 诱导的 Pin1 降解降低了细胞活力，在 MIA PaCa-2 细胞中 EC50 值为 8.4 μM，在 KPC 细胞系中EC50值为 5.3 μM[1][1]。

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

PIN1 degrader-3 相关抗体:

Western Blot Analysis[1]

Cell Line: BxPC3 cells, MIA PaCa-2 cells, KPC cells
Concentration: 0 μM, 0.5 μM, 1 μM, 3 μM, 5 μM, 10 μM, 15 μM
Incubation Time: 24 h
Result: Pin1 protein levels decreased in a dose-dependent manner in all three cell lines.
体内研究
(In Vivo)

PIN1 degrader-3 (Compound 164B8; Compound H-3-V) (30-60 mg/kg，腹腔注射，每天一次，每周 5 天，持续 2 周) 可有效抑制 KPC 细胞同种移植肿瘤生长，并直接导致肿瘤组织中 Pin1 的降解，但高剂量可能引起血液毒性[1]。

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

Animal Model: Male NSG mice were used to establish a peritoneal metastasis model by intraperitoneal injection of KPC pancreatic cancer cells expressing GFP and luciferase[1].
Dosage: 30 mg/kg, 60 mg/kg
Administration: I.p., once a day, 5 days a week, for 2 weeks
Result: Tumor burden decreased significantly in a dose-dependent manner.
Mild anemia and moderate thrombocytopenia occurred in the 60 mg/kg group.
分子量

625.55

Formula

C31H34Cl2N6O4
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

PIN1 degrader-3 相关分类

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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:

PIN1 degrader-33101950-55-1PIN1peptidylprolyl cis/trans isomerase, NIMA-interacting 1Pin1Pancreatic cancerCancer-associated fibroblastsCAFsInhibitorinhibitorinhibit

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