1. Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  2. Mitochondrial Metabolism DNA/RNA Synthesis Oxidative Phosphorylation
  3. POLRMT-IN-4

POLRMT-IN-4 是一种光激活的线粒体 RNA 聚合酶 (POLRMT) 抑制剂。POLRMT-IN-4 在光照下可从光活化前药中释放,实现时空精准抑制和局部组织选择性。POLRMT-IN-4 扰乱线粒体转录,损害氧化磷酸化,并抑制癌细胞增殖。POLRMT-IN-4 可用于多种癌症的研究,例如胰腺癌。

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POLRMT-IN-4

POLRMT-IN-4 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

POLRMT-IN-4 is a photoactivated mitochondrial RNA polymerase (POLRMT) inhibitor. POLRMT-IN-4 can be liberated from the photoactivatable prodrug upon irradiation, enables spatiotemporally precise inhibition and localized tissue selectivity. POLRMT-IN-4 disrupts mitochondrial transcription, impairs oxidative phosphorylation, and suppresses cancer cell proliferation. POLRMT-IN-4 can be used in research on various cancers, such as pancreatic cancer[1].

体外研究
(In Vitro)

POLRMT-IN-4 (LJ03) (作用 168 h) 可抑制 MIA PaCa-2 胰腺癌细胞及 HEK293T 正常细胞的增殖,对前者的 IC50 为 0.127 μM,对后者的 IC50 为 0.327 μM[1]
POLRMT-IN-4 (LJ03) (500 nM;12 h) 可将 MIA PaCa-2 细胞中线粒体 ND1 转录本水平降至对照组的 22.2%,将 HEK293T 细胞中的该水平降至对照组的 39.9%[1]
POLRMT-IN-4 (LJ03) (25-100 nM;14 天) 可显著抑制 MIA PaCa-2 细胞的集落形成[1]
POLRMT-IN-4 (LJ03) (500 nM;作用 96 小时) 不会干扰 MIA PaCa-2 细胞的细胞周期进程[1]
POLRMT-IN-4 (LJ03) (500 nM; 96 h) 不会在 MIA PaCa-2 细胞中激活凋亡通路[1]
POLRMT-IN-4 (LJ03) (作用 168 h) 对多种癌细胞系 (A2780、HeLa、A431、MDA-MB-468、HepG2) 表现出广谱抗增殖活性,且其活性不受辐照影响[1]

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

Cell Cycle Analysis[1]

Cell Line: MIA PaCa-2 cells
Concentration: 500 nM
Incubation Time: 96 h
Result: Did not cause significant changes in the distribution of MIA PaCa-2 cells across G1, S, and G2 phases after 96 h of incubation in the dark or upon light irradiation.

Apoptosis Analysis[1]

Cell Line: MIA PaCa-2 cells
Concentration: 500 nM
Incubation Time: 96 h
Result: Did not induce significant early or late apoptotic markers in MIA PaCa-2 cells after 96 h of incubation in the dark or upon light irradiation.
体内研究
(In Vivo)

POLRMT-IN-4 (LJ03) (500 nM; 水体暴露;3 天) 在黑暗条件下的斑马鱼胰腺癌异种移植模型中表现出显著的肿瘤生长抑制作用[1]

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

Animal Model: Zebrafish (Danio rerio, AB strain) bearing MIA PaCa-2 cells.[1]
Dosage: 500 nM
Administration: Aqueous exposure; 3 days
Result: Significantly suppressed tumor-associated fluorescence intensity.
分子量

410.44

Formula

C23H23FN2O4

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 *
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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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产品名称:
POLRMT-IN-4
目录号:
HY-181072
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