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Telomestatin

CAS No. : 265114-54-3

MCE 站：Telomestatin

产品活性：Telomestatin 是一种非常有效的端粒酶 (telomerase) 抑制剂，可从 Streptomyces anulatus?3533-SV4 中分离得到。Telomestatin 选择性地促进分子内 G-quadruplexes 的形成，特别是人类端粒序列 d[T2AG3]4 的形成。Telomestatin 是一种 ADC 细胞毒素，可用于癌症研究。

研究领域：Cell Cycle/DNA Damage  |  Antibody-drug Conjugate/ADC Related

作用靶点：Telomerase  |  ADC Cytotoxin

In Vitro: Telomestatin (0-50 μM) promotes or stabilizes the formation of the intramolecular G-quadruplex. At the DNA concentrations of 0.005 and 0.2 ?M, EC₅₀ values of 0.03 ?M and 0.53 ?M telomestatin are found. In a parallel experiment with the mutated oligonucleotide d[T2AGAG]4, there is no conversion of the mutated sequence to a G-quadruplex structure by telomestatin.
Telomestatin (2-10?μM) effects the expression of DN-hTERT on telomerase activity and telomere length, at 10?μM，the expression of DN-hTERT shows a significant reduction of telomerase activity. Additionally, at 2?μM?, the terminal restriction fragment (TRF) length of U937 cells shortens progressively from 9.5 to 3.8?kb at population doubling (PD) 20 in U937 cells.
Telomestatin (2-5?μM; short-time or long trem) has less effect on normal diploid human fibroblasts and ALT-positive cells.
Telomestatin (5?μM; short-time 3 days) exposure has no affect the viability of normal human fibroblasts BJ or IMR-90; however, 5?μM?of telomestatin reduces the viability of GM847 cells.
Telomestatin (2 μM; long-term 10-50 days) does not significantly change the proliferation rate or viability to that of control cells in BJ or IMR-90 cells and also does not change the proliferation of GM847 cells.

In Vivo: Telomestatin (intraperitoneal injection; 3-15 mg/kg; two times a week; 4 weeks) decreases tumor telomerase activity and inhibits the growth of U937 xenografts. Systemic administrations of 3?mg/kg or 9?mg/kg or 15?mg/kg of telomestatin decreases tumor telomerase activity by 60.2%, 74% and 92.5% compared to control, respectively.

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