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Table 1 Summary of results

From: Inhibition of HIV-1 replication by P-TEFb inhibitors DRB, seliciclib and flavopiridol correlates with release of free P-TEFb from the large, inactive form of the complex

Assay DRB (μM) Seliciclib (μM) Flavopiridol (nM)
IC50 of kinase inhibition: 0.9* 2.7 22
IC50 of loss of large form from HeLa cells:    
Cyclin T1 5 +/- 3 2.7 +/- 1 12 +/- 4
Cdk9 4.2 +/- 1.6 3.2 +/- 1.4 26 +/- 6
IC50 of inhibition of HIV in HeLa 37 cells: 2.6 3 9.5
Hela37 cell cytotoxicity (LD50): 20 12.5 225
Hela37 therapeutic index: 7.7 4.2 23.7
PBL therapeutic index: N/D N/D 2.7
MDM therapeutic index: N/D N/D 1.7
  1. * as described in Peng et al (1998) Genes and Dev. 12: 755–762.
  2. N/D = not determined