Telomestatin


Catalog No. Size PriceQuantity
M12162-2 Contact sales@xcessbio.com for quotation $100
M12162-10 Contact sales@xcessbio.com for quotation $100

Description

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.

Product information

CAS Number: 265114-54-3

Molecular Weight: 582.50

Formula: C26H14N8O7S

Chemical Name: (1R)-4, 8-dimethyl-3, 7, 11, 15, 19, 23, 27-heptaoxa-31-thia-33, 34, 35, 36, 37, 38, 39, 40-octaazanonacyclo[28.2.1.1, .1, .1, .1, .1, .1, .1, ]tetraconta-2(40), 4, 6(39), 8, 10(38), 12, 14(37), 16, 18(36), 20, 22(35), 24, 26(34), 28, 30(33)-pentadecaene

Smiles: CC1OC2=NC=1C1=NC(C3=NC(=CO3)C3=NC(=CO3)C3=NC(=CO3)C3=NC(=CO3)C3=NC(=CO3)C3=N[C@H]2CS3)=C(C)O1

InChiKey: YVSQVYZBDXIXCC-INIZCTEOSA-N

InChi: InChI=1S/C26H14N8O7S/c1-9-17-24-30-14(6-39-24)21-28-12(4-37-21)19-27-11(3-35-19)20-29-13(5-36-20)22-31-15(7-38-22)26-32-16(8-42-26)23-33-18(10(2)40-23)25(34-17)41-9/h3-7,16H,8H2,1-2H3/t16-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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.

References:

  1. Mu-Yong Kim, et al. Telomestatin, a potent telomerase inhibitor that interacts quite specifically with the human telomeric intramolecular g-quadruplex. J Am Chem Soc. 2002 Mar 13;124(10):2098-9.
  2. Keita Amagai, et al. Identification of a gene cluster for telomestatin biosynthesis and heterologous expression using a specific promoter in a clean host. Sci Rep. 2017 Jun 13;7(1):3382.
  3. T Tauchi, et al. Telomerase inhibition with a novel G-quadruplex-interactive agent, telomestatin: in vitro and in vivo studies in acute leukemia. Oncogene. 2006 Sep 21;25(42):5719-25.

Products are for research use only. Not for human use.

Payment & Security

American Express Diners Club Discover JCB Mastercard PayPal Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed