1. PROTAC Apoptosis Membrane Transporter/Ion Channel NF-κB
  2. NF-κB CRM1 PROTACs Apoptosis
  3. PROTAC XPO1 degrader-1

PROTAC XPO1 degrader-1 (Compound 2c) 是一种 XPO1 降解剂。PROTAC XPO1 degrader-1 具有抗细胞增殖作用,还能诱导细胞凋亡 (Apoptosis),抑制 NF-κB 活性,并导致细胞周期阻滞于 G1 期。PROTAC XPO1 degrader-1 可以用于血液系统恶性肿瘤的研究 (粉色: 靶蛋白配体 (HY-170672); 黑色: Linker (HY-W010525); 蓝色: E3 连接酶配体 (HY-170671); E3 连接酶配体-Linker 偶联物 (HY-170673))。

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PROTAC XPO1 degrader-1 Chemical Structure

PROTAC XPO1 degrader-1 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

PROTAC XPO1 degrader-1 (Compound 2c) is an XPO1 degrader. PROTAC XPO1 degrader-1 exhibits anti-proliferative effects, can induce cell apoptosis, inhibit NF-κB activity, and cause cell cycle arrest in the G1 phase. PROTAC XPO1 degrader-1 can be used in research on hematological malignancies (Pink: Target Protein Ligand (HY-170672); Black: Linker (HY-W010525); Blue: E3 Ligase Ligand (HY-170671); E3 Ligase Ligand-Linker Conjugate (HY-170673))[1].

体外研究
(In Vitro)

PROTAC XPO1 degrader-1 (Compound 2c) 在 MV4-11 急性髓系白血病 (AML) 细胞中能有效降解 XPO1 蛋白,其 DC50 为 23.67 nM[1]
PROTAC XPO1 degrader-1 具有显著的抗细胞增殖作用,对 MV4-11 和 MOLM-13 细胞的 IC50 值分别为 0.142 μM 和 0.186 μM[1]
PROTAC XPO1 degrader-1 (100-500 nM; 24 h) 通过 caspase 途径有效诱导 MV4-11 细胞凋亡[1]
PROTAC XPO1 degrader-1 (100-200 nM; 24 h) 可以将 MV4-11 细胞周期阻滞在 G1 期[1]
PROTAC XPO1 degrader-1 (50 nM; 24 h) 在 MV4-11 细胞中可降低细胞迁移[1]

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

Apoptosis Analysis[1]

Cell Line: MV4-11
Concentration: 100, 200, 500 nM
Incubation Time: 24 h
Result: Induced apoptosis in 71.4 % of the cells at a concentration of 200 nM.
Significantly increased the activation of caspase-3/7 in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: MV4-11
Concentration: 5, 10, 25, 50, 100 ,500 nM
Incubation Time: 12 h
Result: Reduced the protein level of XPO1 in cells in a concentration-dependent manner.

Cell Cycle Analysis[1]

Cell Line: MV4-11
Concentration: 100, 200 nM
Incubation Time: 24 h
Result: Caused the proportion of cells arrested in the G1 phase to rise from 39.50% to 60.28% as the concentration increased (from 0 to 200 nM).

Cell Migration Assay [1]

Cell Line: MV4-11
Concentration: 50 nM
Incubation Time: 24 h
Result: Resulted in approximately a 42.6 % reduction in MV4-11 cell migration at 50 nM.
分子量

734.12

Formula

C33H35ClF3N7O7

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)

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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:
PROTAC XPO1 degrader-1
目录号:
HY-170669
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