1. Metabolic Enzyme/Protease Stem Cell/Wnt
  2. E1/E2/E3 Enzyme YAP
  3. DDO-4033

DDO-4033 是一种 SPOP 抑制剂 (IC50 = 16.9 μM, Kd = 15.1 μM)。DDO-4033 阻碍透明细胞肾细胞癌 (ccRCC) 细胞系的恶性迁移、侵袭和增殖。DDO-4033 破坏 SPOP 对底物 LATS1 的募集,抑制其多泛素化和随后的降解,上调 LATS1 的表达。DDO-4033 具有良好的抗肿瘤活性,可用于肾细胞癌研究。

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DDO-4033

DDO-4033 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DDO-4033 is a SPOP inhibitor (IC50 = 16.9 μM, Kd = 15.1 μM). DDO-4033 impairs the malignant migration, invasion, and proliferation of clear cell renal cell carcinoma (ccRCC) cell lines. DDO-4033 disrupts SPOP recruitment to its substrate LATS1, inhibits its polyubiquitination and subsequent degradation, and upregulates LATS1 expression. DDO-4033 has promising antitumor activity and is promising for renal cell carcinoma research[1].

体外研究
(In Vitro)

DDO-4033 对 786-O、A498、A549 和 HK-2 细胞表现出抗增殖活性,IC50 分别为 1.1、0.68、19.96 和 18.78 μM,但对 HepG2 细胞的抗增殖活性较弱,IC50 > 50 μM[1]
DDO-4033 (0-3 μM,0-32 小时) 可抑制 SPOP 介导的 LATS1 泛素化和降解,下调 A498 细胞中 CTGF 和 CYR61 基因的 mRNA 水平[1]
DDO-4033 (0-5 μM,24 小时) 可抑制 A498 细胞的集落形成并削弱细胞迁移能力[1]
DDO-4033 在 MST、BLI 和 ITC 检测下表现出对 SPOP 的亲和力,Kd 值分别为 15.1、4.96、4.94 μM[1]

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

Western Blot Analysis[1]

Cell Line: A498 cells
Concentration: 0 μM, 0.12 μM, 0.25 μM, 0.5 μM, 1 μM
Incubation Time: 0 h, 1 h, 2 h, 4 h,8 h, 12 h, 16 h, 32 h
Result: Inhibited LATS1 ubiquitination, prolongs the half-life of LATS1, and accumulates LATS1.

Cell Migration Assay [1]

Cell Line: A498 cells
Concentration: 0 μM, 0.5 μM, 1 μM
Incubation Time: 24 h
Result: Inhibited the colony formation and impaired the cell migratory capacity.
体内研究
(In Vivo)

DDO-4033 (10-50 mg/kg,肿瘤内 (i.t.) 和肿瘤周围 (PTI),每天一次, 3 周) 在 A498-Luc 异种移植 BALB/c 裸鼠模型中可抑制肿瘤生长,上调 LATS1 并激活 Hippo 通路[1]

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

Animal Model: A498-Luc (1 × 107 cells containing 25% Matrigel, s.c.) xenograft BALB/c nude mice (female, 18-20 g, 4-6 weeks of age) model[1]
Dosage: 10 mg/kg, 50 mg/kg
Administration: i.t. and PTI, once daily, 3 weeks
Result: Inhibited tumor growth, upregulated LATS1 and activated the Hippo pathway, was low in toxicity and did not change organ tissues.
分子量

406.39

Formula

C20H18N6O4

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

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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.

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产品名称:
DDO-4033
目录号:
HY-175247
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