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ICRF-193

 

Source: Synthetic

Active Product:

Appearance: White to off-white powder

Brand name(s):
Chemical Name: Meso-4,4'-(3,2-butanediyl)-bis(2,6-piperazinedione) OR 4-[(2S,3R)-3-(3,5-dioxopiperazin-1-yl)butan-2-yl]piperazine-2,6-dione
Molecular Weight: M.W. 282.3
Solubility:  Soluble in DMSO (4 mg/ml).  Aliquot and store at -20 °C
 Storage: −20 °C.  (Store, as supplied, at -20°C for up to 1 year. Store solutions at -20°C for up to 3 months)

Target: Topoisomerase II. The IC50 using  a decatenation assay is 12 and 34 µM for topoisomerase IIa and topoisomerase IIb respectively (van Hille et al. 2000)

  

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Comment

 Structure    

 

ICRF-193, is a bis-dioxopiperazine. As an eukaryotic topoisomerase II inhibitors is a catalytic inhibitors that interfere with ATPase and DNA strand-passage reactions leading to stabilisation of the closed clamp form of the enzyme.

The IC50 for cytotoxicity varies from 0.02 - 10 µM depending on the cell type (van Hille et al. 2000).

 

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Synonym:  ICRF 193, (R*,R*)-(+-)-isomer; ICRF 193, (R*,S*)-isomer;

Molecular Formula: C12N4O4H18

      

 

        

 

 References      

 

- Robinson HM, Bratlie-Thoresen S, Brown R, Gillespie DA. Chk1 is required for G2/M checkpoint response induced by the catalytic topoisomerase II inhibitor ICRF-193. Cell Cycle. 2007 May 15;6(10):1265-7.

- Huang KC, Gao H, Yamasaki EF, Grabowski DR, Liu S, Shen LL, Chan KK, Ganapathi R, Snapka RM. Topoisomerase II poisoning by ICRF-193. J Biol Chem. 2001 Nov 30;276(48):44488-94.

- Morris SK, Baird CL, Lindsley JE. Steady-state and rapid kinetic analysis of topoisomerase II trapped as the closed-clamp intermediate by ICRF-193. J Biol Chem. 2000 Jan 28;275(4):2613-8.

- van Hille B, Etiévant C, Barret JM, Kruczynski A, Hill BT. Characterization of the biological and biochemical activities of F 11782 and the bisdioxopiperazines, ICRF-187 and ICRF-193, two types of topoisomerase II catalytic inhibitors with distinctive mechanisms of action. Anticancer Drugs. 2000 Nov;11(10):829-41.