CCR
Inhibitory Selectivity
Isoform-specific Inhibitors
CCR Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| A2040New |
Leronlimab (anti-CCR5)Leronlimab (anti-CCR5) （PRO 140; Vyrologix）is a humanized monoclonal antibody to CCR5, blocks breast cancer cellular metastasis and enhances cell death induced by DNA damaging chemotherapy. It is being investigated as a potential therapy in the treatment of HIV infection. |
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| S2004 |
Vicriviroc MalateVicriviroc is a potent CCR5 antagonist with IC50 of 0.91 nM, showing broad-spectrum activity against genetically diverse HIV-1 isolates, and also drug-resistant viruses with RTI, PRI, or MDR phenotypes. Phase 3. |
Effect of CCR5 receptor antagonists/ligands on LukED cytotoxicity and HIV infection. (a) Viability of Jurkat-R5 cells pre-incubated with CCR5 small molecule antagonists maraviroc (MVC), vicriviroc (VVC), or TAK-779 (TAK) (1μg/mL to 2.5 pg/mL) followed by incubation with LukED (5 μg/mL) and quantification of cell viability via FACS scatter. (b) HIV infection of Hut-R5 cells after incubation with the same CCR5 antago-nists as in (a) (1μg/mL to 64 pg/mL) and subsequent incubation with CCR5-tropic HIV-1 virus encoding the mouse heat-stable antigen (HSA) as a reporter (HIV-R5) for 2.5 days. Infection success was determined by FACS analysis after staining cells for the HSA protein encoded by the virus. Mean and s.e.m. of infected cells from duplicate experiments is shown. |
|
| S3479 |
R243R243 is an inhibitor of Chemokine (C-C motif) receptor 8 (CCR8) signaling and chemotaxis. |
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| S7604New |
BX471BX471 (ZK811752, BAY 865047, SH T 04268H) is a potent nonpeptide CC chemokine receptor-1 (CCR1) antagonist with Ki values of 1 nM and 5.5 nM in both MIP-1α and MCP-3 binding to CCR1-transfected HEK293 cells, respectively. |
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| S0777 |
Isuzinaxib (APX-115 free base)Isuzinaxib (APX-115 free base, Ewha-18278 free base) is a potent, orally active inhibitor of pan NADPH oxidase (pan-Nox) with Ki of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 free base (Ewha-18278 free base) significantly suppresses the expression of inflammatory molecules including MCP-1/CCL2, IL-6, and TNFα in the diabetic kidney. |
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| S3205 |
PerillaldehydePerillaldehyde (Perilladehyde, Perillal, PAE, PA), the main component of Perilla frutescens (a traditional medicinal antioxidant herb), inhibits BaP-induced AHR activation and ROS production, inhibits BaP/AHR-mediated release of the CCL2 chemokine, and activats the NRF2/HO1 antioxidant pathway. |
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| S8512 |
Cenicriviroc (TAK-652)Cenicriviroc (CVC, TAK-652, TBR-652) is a potent, orally active dual inhibitor of CC chemokine receptor 2 (CCR2) and CCR5. Cenicriviroc also inhibits HIV-1 and HIV-2 with potent anti-inflammatory and antiinfective activity. |
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| S3383 |
RS102895RS 102895 is a small molecule antagonist of CCR2 with an IC50 of 360 nM. |
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| E0395New |
VercirnonVercirnon (GSK1605786A, CCX-282, Traficet-EN), an orally bioavailable, selective, and potent antagonist of CCR9, is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9. |
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| S7538 |
RS-102895 HydrochlorideRS-102895 hydrochloride (HCl) is a potent antagonist of Chemokine (C-C motif) receptor 2 (CCR2) with IC50 of 360 nM, and shows no effect on CCR1. RS-102895 hydrochloride also inhibits human α1a and α1d receptors, rat brain cortex 5-HT1a receptor in cells with IC50s of 130 nM, 320 nM, 470 nM, respectively. |
||
| S0085 |
BMS-813160BMS-813160 is a potent, well-absorbed dual CCR2 and CCR5 chemokine antagonist. BMS-813160 inhibits inflammatory processes, angiogenesis, tumor cell migration, tumor cell proliferation and invasion. |
||
| S0129 |
SB-297006SB-297006 is an antagonist of C-C chemokine receptor 3 (CCR3) that suppresses antigen-induced accumulation of T(h)2 as well as eosinophils in the lungs. SB-297006 suppressed CCL11-induced Th2 chemotaxis with IC50 of 2.5 μM. |
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| S8361 |
PF-4136309PF-4136309 (INCB8761, PF-04136309) is a potent, selective, and orally bioavailable CCR2 antagonist with an IC50 of 5.2 nM for human CCR2. |
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| S8324 |
ZK756326 2HClZK756326 is a full agonist of CCR8（Chemokine receptor 8） with an IC50 of 1.8 μM, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| A2040New |
Leronlimab (anti-CCR5)Leronlimab (anti-CCR5) （PRO 140; Vyrologix）is a humanized monoclonal antibody to CCR5, blocks breast cancer cellular metastasis and enhances cell death induced by DNA damaging chemotherapy. It is being investigated as a potential therapy in the treatment of HIV infection. |
||
| S2004 |
Vicriviroc MalateVicriviroc is a potent CCR5 antagonist with IC50 of 0.91 nM, showing broad-spectrum activity against genetically diverse HIV-1 isolates, and also drug-resistant viruses with RTI, PRI, or MDR phenotypes. Phase 3. |
Effect of CCR5 receptor antagonists/ligands on LukED cytotoxicity and HIV infection. (a) Viability of Jurkat-R5 cells pre-incubated with CCR5 small molecule antagonists maraviroc (MVC), vicriviroc (VVC), or TAK-779 (TAK) (1μg/mL to 2.5 pg/mL) followed by incubation with LukED (5 μg/mL) and quantification of cell viability via FACS scatter. (b) HIV infection of Hut-R5 cells after incubation with the same CCR5 antago-nists as in (a) (1μg/mL to 64 pg/mL) and subsequent incubation with CCR5-tropic HIV-1 virus encoding the mouse heat-stable antigen (HSA) as a reporter (HIV-R5) for 2.5 days. Infection success was determined by FACS analysis after staining cells for the HSA protein encoded by the virus. Mean and s.e.m. of infected cells from duplicate experiments is shown. |
|
| S3479 |
R243R243 is an inhibitor of Chemokine (C-C motif) receptor 8 (CCR8) signaling and chemotaxis. |
||
| S7604New |
BX471BX471 (ZK811752, BAY 865047, SH T 04268H) is a potent nonpeptide CC chemokine receptor-1 (CCR1) antagonist with Ki values of 1 nM and 5.5 nM in both MIP-1α and MCP-3 binding to CCR1-transfected HEK293 cells, respectively. |
||
| S0777 |
Isuzinaxib (APX-115 free base)Isuzinaxib (APX-115 free base, Ewha-18278 free base) is a potent, orally active inhibitor of pan NADPH oxidase (pan-Nox) with Ki of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 free base (Ewha-18278 free base) significantly suppresses the expression of inflammatory molecules including MCP-1/CCL2, IL-6, and TNFα in the diabetic kidney. |
||
| S3205 |
PerillaldehydePerillaldehyde (Perilladehyde, Perillal, PAE, PA), the main component of Perilla frutescens (a traditional medicinal antioxidant herb), inhibits BaP-induced AHR activation and ROS production, inhibits BaP/AHR-mediated release of the CCL2 chemokine, and activats the NRF2/HO1 antioxidant pathway. |
||
| S8512 |
Cenicriviroc (TAK-652)Cenicriviroc (CVC, TAK-652, TBR-652) is a potent, orally active dual inhibitor of CC chemokine receptor 2 (CCR2) and CCR5. Cenicriviroc also inhibits HIV-1 and HIV-2 with potent anti-inflammatory and antiinfective activity. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S3383 |
RS102895RS 102895 is a small molecule antagonist of CCR2 with an IC50 of 360 nM. |
||
| E0395New |
VercirnonVercirnon (GSK1605786A, CCX-282, Traficet-EN), an orally bioavailable, selective, and potent antagonist of CCR9, is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9. |
||
| S7538 |
RS-102895 HydrochlorideRS-102895 hydrochloride (HCl) is a potent antagonist of Chemokine (C-C motif) receptor 2 (CCR2) with IC50 of 360 nM, and shows no effect on CCR1. RS-102895 hydrochloride also inhibits human α1a and α1d receptors, rat brain cortex 5-HT1a receptor in cells with IC50s of 130 nM, 320 nM, 470 nM, respectively. |
||
| S0085 |
BMS-813160BMS-813160 is a potent, well-absorbed dual CCR2 and CCR5 chemokine antagonist. BMS-813160 inhibits inflammatory processes, angiogenesis, tumor cell migration, tumor cell proliferation and invasion. |
||
| S0129 |
SB-297006SB-297006 is an antagonist of C-C chemokine receptor 3 (CCR3) that suppresses antigen-induced accumulation of T(h)2 as well as eosinophils in the lungs. SB-297006 suppressed CCL11-induced Th2 chemotaxis with IC50 of 2.5 μM. |
||
| S8361 |
PF-4136309PF-4136309 (INCB8761, PF-04136309) is a potent, selective, and orally bioavailable CCR2 antagonist with an IC50 of 5.2 nM for human CCR2. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S8324 |
ZK756326 2HClZK756326 is a full agonist of CCR8（Chemokine receptor 8） with an IC50 of 1.8 μM, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1. |
