1. Cell Cycle/DNA Damage
    Antibody-drug Conjugate/ADC Related
  2. Telomerase
    ADC Cytotoxin
  3. Telomestatin


目录号: HY-15225

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。

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Telomestatin Chemical Structure

Telomestatin Chemical Structure

CAS No. : 265114-54-3

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Telomestatin is a very potent telomerase inhibitor and can be isolated from Streptomyces anulatus 3533-SV4. Telomestatin selectively facilitates the formation of intramolecular G-quadruplexes, in particular, that produced from the human telomeric sequence d[T2AG3]4. Telomestatin is an ADC cytotoxin and can be used for cancer research[1].

IC50 & Target

Traditional Cytotoxic Agents


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 µM, EC50 values of 0.03 µM and 0.53 µM 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[1].
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[2].
Telomestatin (2-5 μM; short-time or long trem) has less effect on normal diploid human fibroblasts and ALT-positive cells[2].
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[2].
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[2].

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[2].

Animal Model: Mice model with U937 xenografts[2]
Dosage: 3-15 mg/kg
Administration: Intraperitoneal injection; 3-15 mg/kg; two times a week; 4 weeks
Result: Treated with PBS for 21 days had a mean tumor volume of 1395 mm3 compared with telomestatin treated with a mean tumor volume of 291 mm3.
Exhibited no adverse effects (body weight loss, clinical signs or survival).
Reduced U937 cells in bone marrow and recovered the normal hematopoiesis in mice.
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TelomestatinTelomeraseADC CytotoxintelomeraseG-quadruplexesADC cytotoxinU937 cellstelomeric sequencecancerADCInhibitorinhibitorinhibit


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