1. PROTAC
  2. PROTACs
  3. DDD2

DDD2 是一种有选择性且高效的由 VHL 介导的 NUDT5 的 PROTAC 靶向降解剂。DDD2 可诱导 NUDT5 大量降解。DDD2 由弹头 TH10184 和 VHL 招募配体 VH032 组成,通过一条饱和脂肪族八碳连接体相连。DDD2 可用于癌症研究,例如淋巴细胞白血病和骨肉瘤。(结构:蓝色:NUDT5 inhibitor (HY-176262);粉色:VHL recruiting ligand (HY-120217);黑色:linker (HY-W001958))

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DDD2 Chemical Structure

DDD2 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

DDD2 is a selective and potent VHL-mediated PROTAC NUDT5 degrader. DDD2 induces robust NUDT5 degradation. DDD2 consists of the warhead TH10184 connected to the VHL recruiting ligand, VH032, through a saturated aliphatic eight carbon linker. DDD2 can be used in cancer research, such as lymphocytic leukemia and osteosarcoma[1]. (Structure Note: Blue: NUDT5 inhibitor (HY-176262); Pink: E3 (HY-125845); Black: linker (HY-W001958))

体外研究
(In Vitro)

DDD2 (2 µM, 24 h) 可在 U-2 OS 细胞中诱导强烈的 NUDT5 降解[1]

DDD2 (0.01-10 µM, 4-96 h) 可在 CCRF-CEM 细胞中诱导内源性的 NUDT5 降解,且呈现浓度和时间依赖性[1]

DDD2 (1 µM, 24 h) 在 U-2 OS 细胞中对 NUDT5 的降解依赖于 VHL (HY-P76124) 而非 CRBN (HY-P702820)[1]

DDD2 具有良好的溶解性和稳定性,动力学溶解度均值为 6.25 µM[1]

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

Western Blot Analysis[1]

Cell Line: U-2 OS cells
Concentration: 2 µM
Incubation Time: 24 h, pretreating with Doxorubicin (HY-15142A) (1 µg/mL) to induce GFP1-10
Result: Induced robust NUDT5 degradation.

Western Blot Analysis[1]

Cell Line: CCRF-CEM cells
Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3, and 10 µM
Incubation Time: 4, 24, and 96 h
Result: Showed concentration- and time-dependent degradation of endogenous NUDT5 and achieved Dmax at 24 h.
分子量

1035.22

Formula

C52H66N12O9S

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)

质量   浓度   体积   分子量 *
= × ×

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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DDD2
目录号:
HY-176261
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