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. 2013 Mar;344(3):589–599. doi: 10.1124/jpet.112.199646

TABLE 1.

DBF-based compounds

Solubility was assessed at 5, 20, 50, and 100 µM compound in 20 mM Kphos buffer, pH 7.0, with 1% TFE, 1% glycerol, 2% NP40, and 150 mM NaCl. Solubilities are reported as >100 µM or <50 µM, depending upon whether a given compound followed Beer’s law up to 100 µM or only up to 50 µM, respectively. Proliferation of endothelial cells is reported in terms of IC50 values (µM) for each compound. Bold letters indicate amino acids in the sequence that have been modified/changed.

Name Sequence Solubility IC50
µM µM
 Anginex ANIKLSVQMKLFKRHLKWKIIVKLND >100 4
 6DBF7 SVQMKL-[DBF]-IIVKLND <50 22
Single alanine substitution of 6DBF7
 DB1 AVQMKL-[DBF]-IIVKLND >100 19
 DB2 SAQMKL-[DBF]-IIVKLND <50 64
 DB3 SVAMKL-[DBF]-IIVKLND <50 28
 DB4 SVQAKL-[DBF]-IIVKLND >100 13
 DB5 SVQMAL-[DBF]-IIVKLND >100 202
 DB6 SVQMKA-[DBF]-IIVKLND >100 27
 DB7 SVQMKL-[DBF]-AIVKLND <50 19
 DB8 SVQMKL-[DBF]-IAVKLND >100 29
 DB9 SVQMKL-[DBF]-IIAKLND >100 31
 DB10 SVQMKL-[DBF]-IIVALND >100 74
 DB11 SVQMKL-[DBF]-IIVKAND <50 28
 DB12 SVQMKL-[DBF]-IIVKLAD <50 22
 DB13 SVQMKL-[DBF]-IIVKLNA <50 10
Double alanine substitution of 6DBF7
 DB14 SVQAKL-[DBF]-IIVKLNA >100 8
 DB15 SVQAKL-[DBF]-AIVKLND <50 9
 DB16 SVQMKL-[DBF]-AIVKLNA >100 5
Triple alanine substitution of 6DBF7
 DB17 SVQAKL-[DBF]-AIVKLNA <50 9
Norleucine substitution for Lys in 6DBF7
 DB18 SVQMNleL-[DBF]-IIVKLNA <50 9
 DB30 SVQMKL-[DBF]- NleIVKLNA <50 3
 DB19 SVQMKL-[DBF]-IIVNleLNA <50 15
 DB29 SVQMNleL-[DBF]-IIVNleLNA <50 20
Norvaline substitution for Val, Met, Leu, or Ile (branched to linear alkyl) in 6DBF7
 DB25 SNvaQMKL-[DBF]-IIVKLNA >100 10
 DB21 SVQNvaKL-[DBF]-IIVKLNA >100 3
 DB22 SVQMKNva-[DBF]-IIVKLNA <50 4
 DB23 SVQMKL-[DBF]- NvaIVKLNA <50 3
 DB26 SVQMKL-[DBF]-IIVKNvaNA <50 5
 DB24 SVQMKL-[DBF]-IINvaKLNA <50 3
 DB27 SVQMKL-[DBF]-IIVKLNNva <50 4
 DB28 SVQNvaKNva-[DBF]- NvaINvaKLNA <50 5