| DC44834 |
TC14012 |
TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity. |
|
| DC44835 |
CTCE-9908 |
CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells. |
|
| DC44836 |
(R,R)-CXCR2-IN-2 |
(R,R)-CXCR2-IN-2, diastereoisomer of CXCR2-IN-2 (compound 68), is a brain penetrant CXCR2 antagonist with a pIC50 of 9 and 6.8 in the Tango assay and d in the HWB Gro-α induced CD11b expression assay, respectively. |
|
| DC46240 |
CCR4 antagonist 2 |
CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues.
CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively. |
|
| DC46450 |
CTCE-9908 TFA |
CTCE-9908 TFA is a potent and selective CXCR4 antagonist. CTCE-9908 TFA induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells. |
|
| DC46481 |
TC14012 TFA |
TC14012 TFA, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 TFA is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity. |
|
| DC46942 |
CCR4 antagonist 3 hydrochloride |
CCR4 antagonist 3 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity. |
|
| DC48039 |
BMS-753426 |
BMS-753426 is a potent and orally bioavailable antagonist of CCR2. |
|
| DC48046 |
AZD-5672
Featured
|
AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis. |
|
| DC48389 |
CCR2 antagonist 5 |
CCR2 antagonist 5 is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). CCR2 antagonist 5 displays a Ki of 9.6 µM for mCCR2 binding. CCR2 antagonist 5 can be used in the research of inflammatory disease. |
|
| DC48395 |
ACT-1004-1239
Featured
|
ACT-1004-1239 is a potent, selective, orally available CXCR7 antagonist with an IC50 value of 3.2 nM. |
|
| DC48396 |
CXCR2 antagonist 2 |
CXCR2 antagonist 2 is a potent CXCR2 antagonist for cancer immunotherapy with an IC50 value of 95 nM. |
|
| DC48397 |
AZD4721 |
AZD4721 (RIST4721) is the potent and orally active antagonist of acidic CXC chemokine receptor 2 (CXCR2). AZD4721 has the potential for the research of inflammatory disease. |
|
| DC48688 |
CXCR2 antagonist 3 |
CXCR2 antagonist 3 (compound 11h) is a potent antagonist of CXC chemokine receptor 2 (CXCR2). CXCR2 antagonist 3 demonstrates double-digit nanomolar potencies against CXCR2 and significantly inhibited neutrophil infiltration into the air pouch. CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs and enhance the infiltration of CD3+ T lymphocytes into the Pan02 tumor tissues. |
|
| DC48823 |
SB-328437
Featured
|
SB-328437 is a potent, selective non-peptide CCR3 antagonist with an IC50 of 4.5 nM. |
|
| DC49414 |
CKLF1-C27 |
CKLF1-C27, a C-terminal peptide of CKLF1, binds to CCR4 receptor and activates ERK1/2 pathway. CKLF1-C27 can abrogate the effect of CKLF1 on cells by competing for CCR4 receptor. CKLF1-C27 shows great effect on promoting proliferation on HUVECs. CKLF1-C27 has the potential for psoriasis research. |
|
| DC49415 |
CKLF1-C27 TFA |
CKLF1-C27, a C-terminal peptide of CKLF1, binds to CCR4 receptor and activates ERK1/2 pathway. CKLF1-C27 can abrogate the effect of CKLF1 on cells by competing for CCR4 receptor. CKLF1-C27 shows great effect on promoting proliferation on HUVECs. CKLF1-C27 has the potential for psoriasis research. |
|
| DC50168 |
BMS-639623 |
BMS-639623 is a potent and orally activeCCR3 antagonist with an IC50 of 0.3 nM. BMS-639623 picomolar inhibition potency against eosinophil chemotaxis (IC50=38 pM). BMS-639623 can be used for the research of asthma. |
|
| DC50169 |
CCR8 antagonist 1 |
CCR8 antagonist 1 (compound 15) is a potente human CCR8 antagonist with a Ki of 1.6 nM. |
|
| DC50170 |
Fuscin |
Fuscin, a fungal metabolite, CCR5 receptor antagonist with anti-HIV effects. Fuscin is a respiration and oxidative phosphorylation inhibitor, and also a mitochondrial SH-dependent transport-linked functions inhibitor. |
|
| DC50201 |
CXCR4 antagonist 3 |
CXCR4 antagonist 3 (compound 12a) is a potent antagonist of CXCR4 with an IC50 of 11 nM. CXCR4 antagonist 3 is a congener of TIQ15. CXCR4 antagonist 3 demonstrates the best overall properties including CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. CXCR4 antagonist 3 has the potential for the research of human immunodeficiency virus. |
|
| DC50202 |
HF51116 |
HF51116 is a potent antagonist of CXCR4. HF51116 strongly antagonizes SDF-1α-induced cell migration, calcium mobilization, and CXCR4 internalization. HF51116 inhibits HIV-1 infection via CXCR4. HF51116 has the potential for the research of HIV-1 infection, hematopoietic stem cell mobilization, and cancer metastasis. |
|
| DC50203 |
CXCR4 antagonist 4 |
CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM). |
|
| DC70088 |
VUF11207 fumarate |
VUF11207 fumarate is a potent CXCR7 (ACKR3) agonist with EC50 of 1.6 nM, inducse recruitment of β-arrestin2 and subsequent internalization of CXCR7 in cells. |
|
| DC70128 |
ALT-1188 |
A novel potent, nonpeptide CXCR4 antagonist with IC50 of 0.93 nM; induces increased and prolonged mobilization of murine HSPC compared to AMD3100. |
|
| DC70129 |
PRX-177561 |
A novel potent, selective, brain-penetrating, orally active CXCR4 antagonist with Ki of 3 nM; inhibits tumor growth alone, increases the antitumor effects of bevacizumab and sunitinib in preclinical models of human glioblastoma; reduces the expression of Nestin in vivo, reduces tumor cell proliferation and accelerates cancer stem cell differentiation in glioblastoma preclinical models. |
|
| DC70140 |
GSK 163929 |
A potent, selective CCR5 antagonist and HIV-1 entry inhibitor with pIC50 of 8.37 and 8.46 in HOS and PBL assays, respectively. |
|
| DC70141 |
GSK 214096 |
A potent, selective CCR5 antagonist and HIV-1 entry inhibitor. |
|
| DC70149 |
AZ 13381758 |
A potent, small molecule CXCR2 inhibitor with IC50 of 26 nM and 30 nM for mCXCR2 and hCXCR2, respectively; inhibits the growth and metastatic potential pancreatic ductal adenocarcinoma, enhances sensitivity to anti-PD1 immunotherapy in vivo; chemical analog of AZD 5069. |
|
| DC70190 |
AMD3451 |
AMD3451 is a specific, dual CXCR5/CXCR4 antagonist with antiviral activity against a wide variety of HIV-1 and HIV-2 (IC50=1.2 to 26.5 uM) in vitro.AMD3451 has antiviral activity against a wide variety of R5, R5/X4, and X4 strains if HIV-1 and HIV-2 in various T-cell lines, CCR5- or CXCR4-transfected cells, PBMCs, and monocytes/macrophages.AMD3451 inhibited R5, R5/X4, and X4 HIV-1 primary clinical isolates in PBMCs (IC50, 1.8 to 7.3 uM), AMD3451 blocks R5 and X4 HIV-1 infection at the virus entry stage.AMD3451 dose-dependently inhibited the intracellular Ca2+ signaling induced by the CXCR4 ligand CXCL12 in T-lymphocytic cells and in CXCR4-transfected cells, as well as the Ca2+ flux induced by the CCR5 ligands CCL5, CCL3, and CCL4 in CCR5-transfected cells.AMD3451 did not interfere with chemokine-induced Ca2+ signaling through CCR1, CCR2, CCR3, CCR4, CCR6, CCR9, or CXCR3 and did not induce intracellular Ca2+ signaling by itself at 400 uM.AMD3451 inhibited CXCL12- and CCL3L1-induced endocytosis in CXCR4- and CCR5-transfected cells.AMD3451 does not inhibit the binding of CXCR4- or CCR5-specific MAbs. |
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