G-Quadruplex nucleic acids or G-quadruplexes (G4s) are four-stranded DNA or RNA secondary structures that are formed in guanine-rich sequences. They are widely distributed in functional regions of the human genome, such as telomeres, ribosomal DNA (rDNA), transcription start sites, promoter regions and untranslated regions of mRNA, suggesting that G-quadruplex structures may play a pivotal role in the control of a variety of cellular processes. In addition, G4s are enriched and conserved in the regulatory regions of microbes, including bacteria, fungi, and viruses.
The irregular formation of G4s on some genes might cause neurodegenerative diseases and cancers. Therefore, G4s in the genome are the therapeutic targets of these diseases. Small molecules, from naturally occurring to synthetic, are exploited to specifically target G-quadruplexes and have proven to be a new class of anticancer agents.
| Cat. No. | Product Name | CAS No. | Purity | Chemical Structure |
|---|---|---|---|---|
| KM6658 |
360A iodide
360A iodide 是一种 G-四联体 (G-quadruplex) 的稳定剂，同时可抑制端粒酶 (telomerase) 的活性，在 TRAP-G4 实验中，IC50 值为 300 nM。 |
737763-37-0 | ≥98% |
|
| KM7316 |
BMVC-8C3O
BMVC-8C3O 是一种 G4 配体，可诱导人端粒 DNA G4s 的非平行型向平行型拓扑转化。 |
1301708-12-2 | 98% |
|
| KM8879 |
Phen-DC3 Trifluoromethanesulfonate
Phen-DC3 Trifluoromethanesulfonate 是一个 G4 特异性配体，可以抑制解旋酶 FANCJ 和 DinG 且 IC50s 值分别为 65±6 和 50±10 nM。 |
929895-45-4 | 98% |
|
| KM5638 |
Pyridostatin hydrochloride
Pyridostatin (RR82) hydrochloride 是一种高选择性的 G-quadruplex DNA 稳定剂 (Kd=490 nM)。Pyridostatin hydrochloride 通过诱导复制和转录依赖的 DNA 损伤促进人类癌细胞生长停滞。Pyridostatin hydrochloride 靶向原癌基因 Src。Pyridostatin hydrochloride 降低人乳腺癌细胞 SRC 蛋白水平和 SRC 依赖的细胞运动。 |
1781882-65-2 | 98% |
|
| KM3947 |
TMPyP4 tosylate
TMPyP4 tosylate (TMP 1363) 是一种四链体 (G-quadruplex) 特异性配体，可抑制 G-四链体和 IGF-1 之间的相互作用。TMPyP4 tosylate (TMP 1363) 是一种端粒酶 (telomerase) 抑制剂，在骨肉瘤细胞系中具有抗肿瘤作用。 |
36951-72-1 | ≥98% |
|
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