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  3. POLRMT-IN-3

POLRMT-IN-3 是一种光激活线粒体 RNA 聚合酶 (POLRMT) 抑制剂。POLRMT-IN-3 在黑暗中无生物活性,经 405 nm 光照可快速释放活性母药 LJ03,实现时空精准的 POLRMT 抑制。POLRMT-IN-3 具有抗肿瘤的活性,可用于胰腺癌、卵巢癌等肿瘤的研究。

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POLRMT-IN-3

POLRMT-IN-3 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

POLRMT-IN-3 is a photosensitive inhibitor of mitochondrial RNA polymerase (POLRMT). POLRMT-IN-3 is biologically inactive in the dark but rapidly releases the active parent compound LJ03 upon illumination with 405 nm light, enabling spatiotemporally precise inhibition of POLRMT. POLRMT-IN-3 exhibits antitumor activity and can be used in research on tumors such as pancreatic cancer and ovarian cancer[1].

体外研究
(In Vitro)

POLRMT-IN-3 (Compound J5) (168 h) 在黑暗条件下对 MIA PaCa-2 和 HEK293T 细胞的抗增殖活性较低,其 IC50 值分别为 9.900 μM 和 7.358 μM[1]
POLRMT-IN-3 在经 405 nm 光照 3 分钟后可显著抑制 MIA PaCa-2 细胞中 ND1、CytB 和 COX1 的转录水平以及 NDUFB8、UQCRC2 和 MTCO1 的蛋白水平[1]
POLRMT-IN-3 (25-100 nM;14 天) 经 405 nm 辐照 3 分钟后,对 MIA PaCa-2 细胞的集落形成呈现剂量依赖性抑制作用[1]
POLRMT-IN-3 在 A2780、HeLa、A431、MDA-MB-468 和 HepG2 细胞中经 405 nm 光照 3 分钟后表现出光依赖性抗增殖活性[1]

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

体内研究
(In Vivo)

POLRMT-IN-3 (200-500 nM;水溶液暴露; 3 天) 在斑马鱼异种移植模型中对 MIA PaCa-2 肿瘤表现出辐照依赖性、剂量依赖性的抑制作用[1]

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

Animal Model: zebrafish (AB strain) treated CM-DiI labeled MIA PaCa-2 cells[1]
Dosage: 200 nM; 500 nM
Administration: Aqueous exposure; followed by 3 min of 405 nm irradiation; 3 days
Result: Showed no effect on tumor proliferation under dark conditions.
Elicited dose-dependent suppression of tumor growth with no apparent toxicity after 405 nm light irradiation for 3 min.
分子量

635.64

Formula

C36H30FN3O7

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
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  • 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:
POLRMT-IN-3
目录号:
HY-181071
需求量: