Skip to main content
. Author manuscript; available in PMC: 2015 Mar 24.
Published in final edited form as: Curr Top Med Chem. 2014;14(13):1574–1589. doi: 10.2174/1568026614666140827143541

Table 1.

Representative CXCR4 Antagonists and Agonists.

Name Chemical Structure Binding Activity
(IC50, nM)b 		Migration
Activity		 Calcium
Mobilization		 Anti-HIV
Activity
(IC50, nM)c 		Type of Modulator
and References
SDF-1α 12G5
SDF-1α KPVSLSYRCPCRFFESHVARANVK
HLKILNTPNCALQIVARLKNNNRQ
VCIDPKLKWIQEYLEKALNK		 4 20 +f + 730 Linear Peptide Modulator
[171-175]
ALX40-4C Ac-NH-RRRRRRRRR-CONH2 NDe 3,200 ND − g 3 Linear Peptide Modulator
[37, 43, 173]
AMD3100 graphic file with name nihms-672483-t0002.jpg 33 37.5 − − 12.4 Orthosteric Modulator
[46, 176, 177]
AMD3465 graphic file with name nihms-672483-t0003.jpg 18 0.75 − − 12.3 Orthosteric Modulator
[46, 177]
AMD070 graphic file with name nihms-672483-t0004.jpg 13 ND ND ND 2 Orthosteric Modulator
[47, 178]
KRH-3955 graphic file with name nihms-672483-t0005.jpg 0.61 2.8 ND − 0.99 Orthosteric Modulator
[48]
GSK812397 graphic file with name nihms-672483-t0006.jpg 0.87 ND − − 4.60 Orthosteric Modulator
[50]
T22 graphic file with name nihms-672483-t0007.jpg ND 48 ND − 5.1 Cyclic/Orthosteric
Modulator [51, 173]
T140 H-Arg-Arg-Nal-Cys-Tyr-Arg-Lys-D-
Lys-Pro-Tyr-Arg-Cit-Cys-Arg-NH2a 		2.4 2.5 − − 0.43 Cyclic/Orthosteric
Modulator
[121, 130, 173, 179]
TC14012 H-Arg-Arg-Nal-Cys-Tyr-Cit-Lys-D-
Cit-Pro-Tyr-Arg-Cit-Cys-Arg-NH2a 		2.9 ND − ND 37 Cyclic/Orthosteric
Modulator [130, 179]
FC131 graphic file with name nihms-672483-t0008.jpg 4 ND ND ND 14 Cyclic/Orthosteric
Modulator
[54, 55, 180-182]
CGP64222 graphic file with name nihms-672483-t0009.jpg ND ND ND − 1,386
1.8 (μg/ml)		 Orthosteric Modulator
[57, 58]
R3G graphic file with name nihms-672483-t0010.jpg ND 7,700 ND − 15,000 Orthosteric Modulator
[183]
NeoR graphic file with name nihms-672483-t0011.jpg ND ND ND ND 800 Orthosteric Modulator
[184, 185]
vMIP-II LGASWHRPDKCCLGYQKRPLPQVL
LSSWYPTSQLCSKPGVIFLTKRGR
QVCADKSKDWVKKLMQQLPVTAR		 14.8 3.0 ND − ND Linear Peptide Modu-
lator [38, 66, 67]
V1 LGASWHRPDKCCLGTQKRPLP 190 640 − − ND Linear Peptide Modu-
lator [38, 39, 62]
DV1 LGASWHRPDKCCLGYQKRPLP d 13 32 − − 12,100 Linear Peptide Modu-
lator [39, 78]
RCP168 LGASWHRPDKCCLGYQKRPLPQVL
LSSWYPTSQLCSKPGVIFLTKRGRQ
VCADKSKDWVKKLMQQLPVTAR		 5 5 − − 50 Dimerized/Bivalent/
Orthosteric Modulator
[68-70]
RSVM RSVMLSYRCPCRFFESH ND ND + + ND Allosteric Modulator
[42, 186]
ASLW ASLWLSYRCPCRFFESH ND ND + + ND Allosteric Modulator
[42, 186]
DV1 Dimer graphic file with name nihms-672483-t0012.jpg ND 3 ND − 4,400 Dimerized/Bivalent/
Orthosteric Modulator
[78]
FC131 Analog graphic file with name nihms-672483-t0013.jpg 9.9 ND ND ND ND Dimerized/Bivalent/
Orthosteric Modulator
[187]
CTCE-9908 graphic file with name nihms-672483-t0014.jpg ND ND − ND ND Dimerized/Bivalent/
Orthosteric Modulator
[188-190]
CXCL122 graphic file with name nihms-672483-t0015.jpg 166 ND − + ND Dimerized/Bivalent/
Orthosteric Modulator
[104, 174, 191]
TN14003 H-Arg-Arg-Nal-Cys-Tyr-Cit-Lys-D-Lys
-Pro-Tyr-Arg-Cit-Cys-Arg-NH2a 		ND ND − ND 140 Cyclic/Orthosteric
Modulator [179, 192]
BKT140 (4F-
benzoyl
-TN14003)		 4-fluorobenzoyl-Arg-Arg-Nal-Cys-Tyr-Cit-
Lys-D-Lys-Pro-Tyr-Arg-Cit-Cys-Arg-NH2a 		0.99 ND − − ND Cyclic/Orthosteric
Modulator [130, 193]
ATI-2341 Palmitic acid-MGYQKKLRSMTDKYRL ND ND + + ND Linear Peptide Modu-
lator [168, 194]
a

Each peptide has a disulfide linkage between Cys4 and Cys13.

b

Competition binding assays utilized a single concentration of radioiodinated SDF-1α or monoclonal antibody 12G5 in the presence of various concentrations of unlabeled chemokines.

c

Infectious virus and/or single-cycle focal infective assays were performed to test the antiviral activities of CXCR4 inhibitors.

d

The D-amino acids are italicized.

e

ND: Not determined

f

+: Promotion

g

−: Inhibition