CXCR
Inhibitory Selectivity
Isoform-specific Inhibitors
CXCR Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S8947 |
SX-682SX-682 is an orally bioavailable small-molecule allosteric inhibitor of CXCR1 and CXCR2 that blocks tumor MDSC recruitment and enhances T cell activation and antitumor immunity. |
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| S2912 |
WZ811WZ811 is a highly potent competitive CXCR4 antagonist with EC50 of 0.3 nM. |
Gelatin degradation by COR-L23 (f) cells treated with 1 μM PF-573228 and 1 μM WZ811. Histograms showing percentages of degraded gelatin areas relative to the cell volume for each cell line are presented together with representative images. Merged channels show fluorescent gelatin (green), actin (red) and nuclei (blue) staining; dark areas represent spots of degraded gelatin. Scale bar = 100 μm. |
|
| S8505 |
LY2510924LY2510924 is a potent and selective CXCR4 antagonist that specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nmol/L and inhibits SDF-1-induced GTP binding with Kb value of 0.38 nmol/L. |
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| S6645 |
AZD5069AZD5069 is a novel antagonist of CXCR2, which is shown to inhibit binding of CXCL8 to CXCR2 with a pIC50 value of 8.8 and inhibit CXCL8 binding to CXCR1 with pIC50 values of 6.5. |
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| S0292 |
MSX-127MSX-127 (NSC-23026) is a C-X-C chemokine receptor type 4 (CXCR4) receptor antagonist. |
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| S0293 |
MSX-130MSX-130 is an antagonist of C-X-C chemokine receptor type 4 (CXCR4). |
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| S9516New |
SB 265610SB265610, a competitive antagonist at the human CXCR2 receptor, can displace [125I]-IL-8 and [125I]-GROα with pIC50 values of 8.41 and 8.47 respectively, preventing receptor activation by binding to a region distinct from the agonist binding site. |
||
| S8682 |
AMG 487AMG 487 is an orally active and selective CXC chemokine receptor 3 (CXCR3) antagonist that inhibits the binding of IP-10 (CXCL10) and ITAC (CXCL11) to CXCR3 with IC50 of 8.0 nM and 8.2 nM, respectively. |
||
| S7651 |
SB225002SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested. |
SB225002 could inhibited h-JBMMSCs chemotaxis in both the co-culture and the monoculture transwell systems (n = 3; *P < 0.05). |
|
| S9665 |
Motixafortide (BL-8040)Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ～1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression. |
||
| S8813 |
LIT-927LIT-927 is a novel neutraligand of CXCL12 with Ki value of 267 nM for inhibition of Texas red-labeled CXCL12 (CXCL12-TR) binding. It shows high selectivity toward CXCL12 vs other chemokines also involved in asthma. |
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| S6617 |
MSX-122MSX-122 is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM). |
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| S9725 |
Balixafortide (POL6326)Balixafortide (POL6326) is an orally bioavailable peptidic CXC chemokine receptor 4 (CXCR4) antagonist. |
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| S4785 |
Nicotinamide N-oxideNicotinamide N-oxide (Nicotinamide 1-oxide, 1-oxynicotinamide) is recognized as an in vivo metabolite of nicotinamide which is a precurser of nicotinamide-adenine dinucleotide (NAD+) in animals. Nicotinamide N-oxide is novel, potent, and selective antagonists of the CXCR2 receptor. |
||
| S8309 |
ATI-2341ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. |
||
| S8869 |
UNBS5162UNBS5162 is a pan-antagonist of CXCL chemokine expression with in vitro cytotoxic activity (IC50 range of 0.5-5 µM) against a range of human cancer cell lines including glioblastoma (Hs683 and U373MG), colorectal (HCT-15 and LoVo), non-small-cell lung (A549) and breast (MCF-7). |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S8947 |
SX-682SX-682 is an orally bioavailable small-molecule allosteric inhibitor of CXCR1 and CXCR2 that blocks tumor MDSC recruitment and enhances T cell activation and antitumor immunity. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S2912 |
WZ811WZ811 is a highly potent competitive CXCR4 antagonist with EC50 of 0.3 nM. |
Gelatin degradation by COR-L23 (f) cells treated with 1 μM PF-573228 and 1 μM WZ811. Histograms showing percentages of degraded gelatin areas relative to the cell volume for each cell line are presented together with representative images. Merged channels show fluorescent gelatin (green), actin (red) and nuclei (blue) staining; dark areas represent spots of degraded gelatin. Scale bar = 100 μm. |
|
| S8505 |
LY2510924LY2510924 is a potent and selective CXCR4 antagonist that specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nmol/L and inhibits SDF-1-induced GTP binding with Kb value of 0.38 nmol/L. |
||
| S6645 |
AZD5069AZD5069 is a novel antagonist of CXCR2, which is shown to inhibit binding of CXCL8 to CXCR2 with a pIC50 value of 8.8 and inhibit CXCL8 binding to CXCR1 with pIC50 values of 6.5. |
||
| S0292 |
MSX-127MSX-127 (NSC-23026) is a C-X-C chemokine receptor type 4 (CXCR4) receptor antagonist. |
||
| S0293 |
MSX-130MSX-130 is an antagonist of C-X-C chemokine receptor type 4 (CXCR4). |
||
| S9516New |
SB 265610SB265610, a competitive antagonist at the human CXCR2 receptor, can displace [125I]-IL-8 and [125I]-GROα with pIC50 values of 8.41 and 8.47 respectively, preventing receptor activation by binding to a region distinct from the agonist binding site. |
||
| S8682 |
AMG 487AMG 487 is an orally active and selective CXC chemokine receptor 3 (CXCR3) antagonist that inhibits the binding of IP-10 (CXCL10) and ITAC (CXCL11) to CXCR3 with IC50 of 8.0 nM and 8.2 nM, respectively. |
||
| S7651 |
SB225002SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested. |
SB225002 could inhibited h-JBMMSCs chemotaxis in both the co-culture and the monoculture transwell systems (n = 3; *P < 0.05). |
|
| S9665 |
Motixafortide (BL-8040)Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ～1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression. |
||
| S8813 |
LIT-927LIT-927 is a novel neutraligand of CXCL12 with Ki value of 267 nM for inhibition of Texas red-labeled CXCL12 (CXCL12-TR) binding. It shows high selectivity toward CXCL12 vs other chemokines also involved in asthma. |
||
| S6617 |
MSX-122MSX-122 is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM). |
||
| S9725 |
Balixafortide (POL6326)Balixafortide (POL6326) is an orally bioavailable peptidic CXC chemokine receptor 4 (CXCR4) antagonist. |
||
| S4785 |
Nicotinamide N-oxideNicotinamide N-oxide (Nicotinamide 1-oxide, 1-oxynicotinamide) is recognized as an in vivo metabolite of nicotinamide which is a precurser of nicotinamide-adenine dinucleotide (NAD+) in animals. Nicotinamide N-oxide is novel, potent, and selective antagonists of the CXCR2 receptor. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S8309 |
ATI-2341ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S8869 |
UNBS5162UNBS5162 is a pan-antagonist of CXCL chemokine expression with in vitro cytotoxic activity (IC50 range of 0.5-5 µM) against a range of human cancer cell lines including glioblastoma (Hs683 and U373MG), colorectal (HCT-15 and LoVo), non-small-cell lung (A549) and breast (MCF-7). |
