PhpC 

PhpC is a G-quadruplex (G4)-DNA/RNA disruptor. PhpC disrupts DNA and RNA G4 structures and promotes G4 helicase activity. PhpC effectively enhancing the activity of Taq polymerase. PhpC modulates G-quadruplexs (G4s) both in vitro and in cells^[1][2][3].

PhpC 增强含 rMYC G4 的 RNA 的逆转录，同时显著抑制 rhTELO、r5YEY 和 rTBA 的逆转录^[3]。
PhpC 促进含 G4 RNA 的体外翻译^[3]。
PhpC 抑制 HEK293FT 细胞活力，IC₅₀ 值为 25.7 μM^[3]。
PhpC (5-20 μM；24 小时) 诱导 DNA 损伤标志物 γH2AX 增加，表明其可诱导 DNA 损伤^[3]。
PhpC (25-100 μM；24 小时) 导致 A549 细胞中成熟 miR-3196 的转录水平逐渐升高^[4]。
PhpC 能够识别并结合形成 G4s (rG4)-3196 序列的区域，破坏其天然 G4 构象并导致结构转变^[4]。
在 HeLa 细胞中，免疫荧光 (IF) 分析表明，100 µM PhpC 显著降低 G4 水平，但对代谢活性没有影响^[5]。
PhpC (90 µM，48 小时) 显著降低 MCF7 细胞中 NRAS G4 的丰度^[6]。
PhpC (90 μM；72 小时) 对 LINC01589 和 MELTF-AS1 无显著影响，而 PhpC 导致 HT-29 细胞中 UXT-AS1 和 NRAS 的含量显著降低^[7]。
PhpC 以有针对性的方式调节 G4 蛋白质组学，仅改变星形胶质细胞中的翻译活性，其中 295 种蛋白质的表达上调，其中大多数蛋白质参与 RNA 交易^[8]。

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

356.38

C₁₈H₂₀N₄O₄

固体

Light yellow to yellow

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

• [1]. Mitteaux, J. et al. Identifying G-Quadruplex-DNA-Disrupting Small Molecules. J. Am. Chem. Soc. 143, 12567-12577 (2021).  [Content Brief]

  [2]. Liu X, et al. Unveiling a Potent Small Molecule Disruptor for RNA G-Quadruplexes Tougher Than DNA G-Quadruplex Disruption. ACS Chem Biol. 2024 Sep 20;19(9):2032-2040.  [Content Brief]

  [3]. Teng X, et al. Discovery of A G-Quadruplex Unwinder That Unleashes the Translation of G-Quadruplex-Containing mRNA without Inducing DNA Damage. Angew Chem Int Ed Engl. 2024 Sep 16;63(38):e202407353.  [Content Brief]

  [4]. Alexandre D, et al. Cellular modulation of a G-quadruplex structure found in the lung cancer-related microRNA-3196. Int J Biol Macromol. 2025 Jul;318(Pt 4):145263.  [Content Brief]

  [5]. De Magis, A. et al. UV-induced G4 DNA structures recruit ZRF1 which prevents UV-induced senescence. Nat. Commun. 14, 6705 (2023).   [Content Brief]

  [6]. Mitteaux J, et al. PhpC modulates G-quadruplex-RNA landscapes in human cells. Chem Commun (Camb). 2024 Jan 4;60(4):424-427.  [Content Brief]

  [7]. Sharma S, et al. Pharmacomodulation of G-quadruplexes in long non-coding RNAs dysregulated in colorectal cancer. BMC Biol. 2025 Aug 8;23(1):249.  [Content Brief]

  [8]. M J VK, et al. Small molecule-based regulation of gene expression in human astrocytes switching on and off the G-quadruplex control systems. J Biol Chem. 2025 Jan;301(1):108040.  [Content Brief]