2. PROTAC Immunology/Inflammation Apoptosis NF-κB Metabolic Enzyme/Protease
  3. PROTACs Pyroptosis Reactive Oxygen Species (ROS) Caspase
  4. DeFer-2

DeFer-2 是一种铁蛋白 PROTAC 降解剂 (Kd = 17.1 μM)。DeFer-2 诱导铁蛋白降解，通过游离铁离子积累和 ROS 升高在癌细胞中启动半胱天冬酶 3 (caspase 3)-GSDME 介导的细胞焦亡 (pyroptosis)。DeFer-2 显著抑制肿瘤生长，延长 B16F10 皮下肿瘤小鼠的生存期。DeFer-2 可用于研究黑色素瘤。(粉色：Oleic acid：HY-N1446 ，蓝色：(S,R,S)-AHPC：HY-125845，黑色：γ-Aminobutyric acid：HY-N0067，蓝色 + 黑色：(S,R,S)-AHPC-C3-NH2：HY-130711)。

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DeFer-2

DeFer-2 Chemical Structure

CAS No. : 3058911-16-0

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DeFer-2 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DeFer-2 is a ferritin PROTAC degrader (Kd = 17.1 μM). DeFer-2 induces ferritin degradation, triggering caspase 3-GSDME-mediated pyroptosis in cancer cells through free iron accumulation and elevated ROS. DeFer-2 significantly inhibits tumor growth and prolongs survival in mice bearing B16F10 subcutaneous tumors. DeFer-2 can be used to study melanoma. (Pink: Oleic acid: HY-N1446, Blue: (S,R,S)-AHPC: HY-125845, Black: γ-Aminobutyric acid: HY-N0067, Blue + Black: (S,R,S)-AHPC-C3-NH2: HY-130711)[1].

IC50 & Target[1]

VHL

 

Caspase 3

 

体外研究
(In Vitro)

DeFer-2 (0-5 μM，0-24 小时) 通过与铁蛋白和 VHL 形成三元复合物来降低铁蛋白的表达，从而诱导 B16F10 细胞中氧化还原和线粒体稳态的破坏[1]。
DeFer-2 (5 μM，8-24 小时) 在 B16F10 细胞中通过游离铁的积累和 ROS 升高来引发 caspase 3-GSDME 介导的细胞焦亡[1]。
DeFer-2 (24-48 小时) 对 B16F10 细胞造成严重的细胞毒性，24 和 48 小时内的 IC50 分别为 3.1 和 1.5 μM[1]。

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

DeFer-2 相关抗体:

Western Blot Analysis[1]

Cell Line: B16F10 cells
Concentration: 0, 0.008, 0.04, 0.2, 0.5, 1, 5 μM
Incubation Time: 0 h, 4 h , 8 h, 12 h, 16 h, 24 h
Result: Reduced the ferritin expression.
Reduced the ferritin expression when as a nanoparticle albumin-DeFer-2.

Immunofluorescence[1]

Cell Line: B16F10 cells
Concentration: 5 μM
Incubation Time: 16 h
Result: Increased ROS levels.
体内研究
(In Vivo)

DeFer-2 (纳米颗粒白蛋白-DeFer-2，10 mg/kg，静脉注射，每隔一天一次，共 8 天) 可抑制 B16F10 肿瘤小鼠模型中的肿瘤生长并延长其生存时间[1]。

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

Animal Model: B16F10 tumor (1 × 106) mice (8-week-old, C57BL/6, male) model[1]
Dosage: 10 mg/kg; in the form of nanoparticle albumin-DeFer-2
Administration: i.v., every other day, 8 days
Result: Inhibited tumor growth and prolonged survival time.
Did not cause systemic toxicity.
分子量

780.11

Formula

C44H69N5O5S
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

DeFer-2 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

DeFer-23058911-16-0DeFer2DeFer 2PROTACsPyroptosisReactive Oxygen Species (ROS)CaspaseDegradermelanomaB16F10 cellspyroptosisB16F10 tumor miceInhibitorinhibitorinhibit

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