2. JAK/STAT Signaling Apoptosis
  3. Pim c-Myc Apoptosis
  4. SGI-1776-VHL-02

SGI-1776-VHL-02 是一种立体选择性的 PIM PROTAC 类降解剂。SGI-1776-VHL-02 能促进 PIM1、PIM2、PIM3 的泛素化和降解。SGI-1776-VHL-02 可下调 c-myc 蛋白水平，诱导细胞凋亡 (Apoptosis)，降低前列腺癌细胞的集落形成能力。SGI-1776-VHL-02 可用于前列腺癌的相关研究。
(粉色: Pim 和 Autophagy 和 Apoptosis 配体 (HY-13287)；蓝色: Ligands for E3 Ligase 和 VHL 配体 (HY-112078)；黑色: 连接子 (HY-W015300))。

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SGI-1776-VHL-02

SGI-1776-VHL-02 Chemical Structure

CAS No. : 3013618-84-0

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SGI-1776-VHL-02 相关抗体

Top Publications Citing Use of Products

查看 Pim 亚型特异性产品:

查看所有亚型
PIM1 PIM2 PIM3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SGI-1776-VHL-02 is a stereoselective PIM PROTAC degrader. SGI-1776-VHL-02 promotes the ubiquitination and degradation of PIM1, PIM2 and PIM3. SGI-1776-VHL-02 downregulates c-myc protein levels, induces Apoptosis, and reduces the colony-forming ability of prostate cancer cells. SGI-1776-VHL-02 can be used in studies related to prostate cancer[1]. (Pink: Pim and Autophagy and Apoptosis ligand (HY-13287); Blue: Ligands for E3 Ligase and VHL ligand (HY-112078); Black: linker (HY-W015300)).

IC50 & Target[1]

PIM1

 

PIM2

 

PIM3

 

体外研究
(In Vitro)

SGI-1776-VHL-02 (0.75-10 μM; 24 h) 可剂量依赖性降解 PC3-dox-PIM1 细胞中Doxycycline 诱导的 PIM1，有效降解起始浓度为 0.75 μM[1]。
SGI-1776-VHL-02 (0.75-10 μM; 24 h) 可立体选择性降解 PC3-dox-PIM1 细胞中多西环素诱导的 PIM1，而其无活性差向异构体对照则无法诱导该降解作用[1]。
SGI-1776-VHL-02 (1.5 μM; 24 h) 不会改变 PC3 细胞中的 PIM1 mRNA 水平，证实其对 PIM1 的作用为转录后调控[1]。
SGI-1776-VHL-02 (1.5-3.75 μM; 24 h) 可降解 PC3 细胞中的全部三种 PIM 激酶亚型，其中 PIM3 在 1.5 μM 浓度下发生降解，PIM2 在 3.75 μM 浓度下发生降解[1]。
SGI-1776-VHL-02 (0.75-6.25 μM; 10 天) 可抑制前列腺癌细胞 PC3、LNCaP、C4-2 的克隆形成[1]。
SGI-1776-VHL-02 (3.75 μM; 24 h) 可下调 PC3 和 LNCaP 前列腺癌细胞中的 c-myc 蛋白水平[1]。
SGI-1776-VHL-02 (3.75 μM; 4 h) 可诱导 PC3 细胞发生凋亡[1]。

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

SGI-1776-VHL-02 相关抗体:

Cell Proliferation Assay[1]

Cell Line: PC3, LNCaP, and C4-2 prostate cancer cells
Concentration: 0.75-6.25 μM
Incubation Time: 10 days, with media replacement every 96 h
Result: Showed a more potent inhibitory effect on colony formation in PC3, LNCaP, and C4-2 cells compared to its parent inhibitor SGI-1776.
Efficiently reduced colony formation at tested concentrations.

Western Blot Analysis[1]

Cell Line: PC3 and LNCaP prostate cancer cells
Concentration: 3.75 μM
Incubation Time: 24 h
Result: Downmodulated c-myc after treatment in both PC3 and LNCaP cells.
Showed no c-myc downmodulation effect with the parent inhibitor SGI-1776 or PIM447-VHL-01.

Apoptosis Analysis[1]

Cell Line: PC3 cells
Concentration: 3.75 μM (SGI-1776-VHL-02); 2 nM (docetaxel)
Incubation Time: 4 h (SGI-1776-VHL-02 pre-treatment); 48 h (docetaxel incubation)
Result: Increased apoptosis significantly to 24% of cells as a single agent.
Increased the percentage of apoptotic cells significantly to 40% when co-treated with docetaxel, which was greater than the combination of docetaxel and SGI-1776.
分子量

974.14

Formula

C50H62F3N9O6S
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

SGI-1776-VHL-02 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

SGI-1776-VHL-023013618-84-0Pimc-MycApoptosisPim kinasesMycprostate cancer cellsLNCaP cellsPIM1PC3-dox-PIM1 cellsVHL E3 ubiquitin ligasePIM2PIM3C4-2 cellsPC3 cellsubiquitin-proteasome pathwayInhibitorinhibitorinhibit

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目录号：
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