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. 2023 Dec 22;43(12):BSR20230981. doi: 10.1042/BSR20230981

Table 1. Sequences and structures of eleven antagonists.

CXCR4 antagonists Sequence*/structure IC50 (nM)
HC4319 Leu-Gly-Ala-Ser-Trp-His-Arg-Pro-Asp-Lys-Cys-Cys-Leu-Gly-Tyr-Gln-Lys-Arg-Pro-Leu-Pro-Lys 46.0 ± 12.6
                       Leu-Gly-Ala-Ser-Trp-His-Arg-Pro-Asp-Lys
DV1 Leu-Gly-Ala-Ser-Trp-His-Arg-Pro-Asp-Lys-Cys-Cys-Leu-Gly-Tyr-Gln-Lys-Arg-Pro-Leu-Pro 364.7 ± 51.7
DV3 Leu-Gly-Ala-Ser-Trp-His-Arg-Pro-Asp-Lys 2596.6 ± 422.4
DV1 dimer Leu-Gly-Ala-Ser-Trp-His-Arg-Pro-Asp-Lys-Cys-Cys-Leu-Gly-Tyr-Gln-Lys-Arg-Pro-Leu-Pro 60.5 ± 12.8
Leu-Gly-Ala-Ser-Trp-His-Arg-Pro-Asp-Lys-Cys-Cys-Leu-Gly-Tyr-Gln-Lys-Arg-Pro-Leu-Pro
V1 Leu-Gly-Ala-Ser-Trp-His-Arg-Pro-Asp-Lys-Cys-Cys-Leu-Gly-Tyr-Gln-Lys-Arg-Pro-Leu-Pro 2632.1 ± 891.0
vMIP-II LGASWHRPDKCCLGYQKRPLPQVLLSSWYPTSQLCSKPGVIFLTKRGRQVCADKSKDWVKKLMQQLPVTAR 10†
CVX15 graphic file with name bsr-43-bsr20230981-i1.jpg 7.8 ± 2.2
LY2510924 Cyclo[Phe-Tyr-Lys(iPr)-D-Arg-2-Nal-Gly-D-Glu]-Lys(iPr)-NH2 135.4 ± 63.9
IT1t graphic file with name bsr-43-bsr20230981-i2.jpg 29.65 ± 2.8
AMD3100 graphic file with name bsr-43-bsr20230981-i3.jpg 319.6 ± 37.3
AMD11070 graphic file with name bsr-43-bsr20230981-i4.jpg 15.6 ± 7.6
HM60303 Lys-Arg-Leu-Gly-Ala-Ser-Trp-His-Arg-Pro-Asp-Lys >50,000
HM60323 Leu-Gly-Ala-Ser-Trp-His-Arg-Pro-Asp-Lys-Arg 706.6 ± 143.2
HM12 Leu-Gly-Ala-Ser-Trp-His-Arg-Pro-Asp-Lys-Arg-Arg 544.0 ± 75.0
HM13 Leu-Gly-Ala-Ser-Trp-His-Arg-Pro-Asp-Lys-Nal-Arg-Arg 377.4 ± 7.7
HM70116 Leu-Gly-Ala-Ser-Trp-His-Arg-Pro-Nal-Arg-Arg 193.9 ± 37.9
*

Sequences of the D-peptides HC4319, DV1, DV1 dimer, DV3, HM60303, HM60323, HM12, HM13, and HM70116 are composed of D-amino acids. The sequence of vMIP-II is shown by one letter code.

†

The IC50 value of vMIP-II was from the previously published results [42]. The IC50 values of CXCR4 antagonists were averages of at least three independent experiments shown as mean ± standard error of mean (S.E.M.).