2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase
  4. CHNQD-03301

CHNQD-03301 是一种具有口服活性的缺氧诱导因子 hypoxia-inducible factor-1α (HIF-1α) 抑制剂 (IC50 = 10.97 nM)。CHNQD-03301 可促进 HIF-1α 蛋白的蛋白酶体降解，从而显著抑制其表达。在斑马鱼模型中，CHNQD-03301 可逆转 HIF 积累诱导的血管生成，并减轻 HIF 诱导的红细胞增多症表型。CHNQD-03301 可用于结肠癌的研究。

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CHNQD-03301

CHNQD-03301 Chemical Structure

CAS No. : 3104302-65-7

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CHNQD-03301 相关抗体

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HIF-1α HIF

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CHNQD-03301 is an orally active hypoxia-inducible factor-1α (HIF-1α) inhibitor (IC50 = 10.97 nM). CHNQD-03301 promotes the proteasomal degradation of HIF-1α protein, leading to its significant suppression. CHNQD-03301 can reverse HIF accumulation-induced angiogenesis and mitigate the HIF-induced erythrocytosis phenotype in zebrafish models. CHNQD-03301 can be used for the study of colon cancer[1].

IC50 & Target[1]

HIF-1α

10.97 nM (IC50)

体外研究
(In Vitro)

CHNQD-03301 (Compound 20) (0.01-1.0 μM，24 小时) 呈剂量依赖性地降低 HCT116 细胞中 HIF-1α 蛋白水平，并降低下游靶蛋白 CA9、REDD1 和 PDK1 的表达，同时 CA9、VEGF 和 REDD1 等下游基因的 mRNA 表达水平也显著降低[1]。
CHNQD-03301 (0.4-1.6 μM) 显著降低 EPO mRNA 水平，抑制 HCT116 细胞中缺氧诱导的血管生成[1]。
CHNQD-03301 在常氧条件下对 HCT116 细胞的 IC50 值为 2.31 μM，在缺氧条件下为 0.83 μM[1]。
CHNQD-03301 (0.4-1.6 μM) 在缺氧条件下诱导 HCT116 细胞周期阻滞于 G2 期[1]。
CHNQD-03301 (0.4-1.6 μM) 对 HCT116 细胞增殖无显著影响，但可显著抑制 von Hippel-Lindau (VHL) 缺陷型 RCC4 细胞的增殖[1]。
CHNQD-03301 (1-4 μM，7-14 天) 呈剂量依赖性地抑制 HCT116 细胞的球状体形成[1]。
CHNQD-03301 (0.4-2.0 μM，24 小时) 可显著抑制缺氧条件下 HCT116 细胞和 VHL 缺陷型 RCC4 细胞的迁移能力[1]。

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

CHNQD-03301 相关抗体:

Western Blot Analysis[1]

Cell Line: HCT116 cells, RCC4 cells
Concentration: 0.01 μM, 0.1 μM, 1.0 μM
Incubation Time: 24 h
Result: In HCT116 cells, CHNQD-03301 dose-dependently reduced HIF-1α protein levels and decreased the expression of downstream target proteins (CA9, REDD1, PDK1).
In HCT116 cells exogenously overexpressing HIF-1α, CHNQD-03301 also reduced HIF-1α protein levels.
In RCC4 cells (VHL-deficient), CHNQD-03301 effectively reduced HIF-1α and CA9 protein levels.
Co-treatment with the proteasome inhibitor MG132 rescued CHNQD-03301-induced HIF-1α degradation.

Cell Migration Assay [1]

Cell Line: HCT116 cells (under hypoxic conditions), VHL-deficient RCC4 cells
Concentration: 0.4 μM, 0.8 μM, 1.6 μM
Incubation Time: 24 h
Result: Significantly inhibited the migration ability of HCT116 cells under hypoxic conditions and VHL-deficient RCC4 cells.
体内研究
(In Vivo)

CHNQD-03301 (Compound 20) (1 mg/kg，口服，每日一次，疗程 13-19 天) 可显著抑制小鼠 MB49 同种异体移植瘤和 HCT116 异种移植瘤的生长，且无明显毒性[1]。
CHNQD-03301 (100 mg/kg，口服，单次) 在小鼠中 100 mg/kg 剂量下未显示急性毒性，且最大耐受剂量 (MTD) 高于 100 mg/kg，表明其具有良好的安全性[1]。

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

Animal Model: A tumor model was established in female C57BL/6J (8-week-old) mice by subcutaneous injection of MB49 mouse bladder cancer cells (1×105 cells/mouse)[1].
Dosage: 1 mg/kg
Administration: P.o., once daily for 13 days
Result: Low-dose oral administration effectively inhibited MB49 tumor growth (TGI = 52.0%) and showed no significant change in mouse body weight.
Animal Model: A tumor model was also established in female C57BL/6J (8-week-old) mice by subcutaneous injection of HCT116 human colon cancer cells (2×106 cells/mouse)[1].
Dosage: 1 mg/kg
Administration: P.o., once daily for 19 days
Result: Low-dose oral administration effectively inhibited MB49 tumor growth (TGI = 51.0%) and showed no significant change in mouse body weight.
Animal Model: Healthy female ICR mice[1].
Dosage: 100 mg/kg
Administration: P.o., once
Result: None of the mice died within 7 days.
No apparent difference in blood biochemistry parameters, including ALT, AST, LDH, UREA, CREA, UA, and CK.
Hematoxylin and eosin (H&E) staining results presented no pathological changes in the collected tissues (hearts, livers, spleens, lungs, kidneys, and duodenum).
分子量

392.40

Formula

C23H20O6
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

CHNQD-03301 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

CHNQD-033013104302-65-7CHNQD03301CHNQD 03301HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHHypoxia-Inducible Factor-1αHIF-1αBenzofuranoid p-terphenylsTumor HypoxiaHCT116 XenograftMB49 AllograftInhibitorinhibitorinhibit

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