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CCR Signaling Pathways

CCR Products

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  • New CCR Products
Catalog No. Product Name 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.
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.
S2004 Vicriviroc Malate Vicriviroc 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.
Nature, 2013, 493(7430):51-5
Cancer Res, 2012, 72(15):3839-50
J Antimicrob Chemot, 2011, 66(4):802-12
S2907 Pirfenidone (S-7701) Pirfenidone (S-7701, AMR-69) is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Pirfenidone attenuates chemokine (CC motif) ligand-2 (CCL2) and CCL12 production with anti-fibrotic activity. Phase 3.
Cancer Biol Ther, 2022, 23(1):150-162
Sci Rep, 2022, 12(1):7
Integr Biol (Camb), 2022, 14(1):1-12
S3032 Bindarit (AF 2838) Bindarit (AF 2838) exhibits selective inhibition against monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 34(6):1911-1918
S3205 Perillaldehyde Perillaldehyde (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.
S3479 R243 R243 is an inhibitor of Chemokine (C-C motif) receptor 8 (CCR8) signaling and chemotaxis.
S7604New BX471

BX471 (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.

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.
Biometals, 2022, 1-14
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00191-0
E0395New Vercirnon Vercirnon (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.
E0486New C-021 C-021 is a potent CCR4 antagonist with IC50 values are 0.14 μM and 39 nM for inhibition of chemotaxis in human and mouse respectively.
S0085 BMS-813160 BMS-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-297006 SB-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.
Cell Death Dis, 2022, 13(5):478
S2003 Maraviroc (UK-427857) Maraviroc (UK-427857) is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM in cell-free assays, respectively. Maraviroc is used in the treatment of HIV infection.
J Exp Clin Cancer Res, 2022, 41(1):81
J Ethnopharmacol, 2022, 289:115051
Biol Pharm Bull, 2022, 45(1):34-41
S3383 RS102895 RS 102895 is a small molecule antagonist of CCR2 with an IC50 of 360 nM.
S6555 AZD2098 AZD2098 is a potent and bioavailable CCR4 receptor antagonist with pIC50 of 7.8.
S7538 RS-102895 Hydrochloride RS-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.
S8220New INCB3344 INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
S8361 PF-4136309 PF-4136309 (INCB8761, PF-04136309) is a potent, selective, and orally bioavailable CCR2 antagonist with an IC50 of 5.2 nM for human CCR2.
S8501 Adaptavir (DAPTA) Adaptavir (DAPTA, D-Ala-peptide T-amide, peptide T) is a water soluble potent, selective CCR5 antagonist which potently inhibits specific CD4-dependent binding of gp120 Bal (IC50 = 0.06 nM) and CM235 (IC50 = 0.32 nM) to CCR5.
Cell Death Dis, 2022, 13(5):478
Proc Natl Acad Sci U S A, 2021, 118(9)e2017282118
FEBS J, 2020, 287(11):2367-2385
S9738New RS504393 RS504393, an extremely selective CC chemokine receptor (CCR) 2 antagonist with IC50 of 98 nM, also targets multiple receptors for inhibition of CCR2b and CCR1 receptors when administrated in higher concentration.
S8324 ZK756326 2HCl ZK756326 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.
Cancer Immunol Immunother, 2022, 10.1007/s00262-022-03196-3
J Exp Med, 2019, 216(12):2763-2777
P1137New Thymulin Thymulin (FTS) is a neuroendocrine hormone with immunoregulatory actions, with anti-inflammatory potential by downregulating the release of inflammatory mediators, such as cytokines and chemokines, upregulating anti-inflammatory factors, such as interleukin (IL)-10, exerting molecular control via the regulation of transcription factors and mediators.
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.
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.
S2004 Vicriviroc Malate Vicriviroc 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.
Nature, 2013, 493(7430):51-5
Cancer Res, 2012, 72(15):3839-50
J Antimicrob Chemot, 2011, 66(4):802-12
S2907 Pirfenidone (S-7701) Pirfenidone (S-7701, AMR-69) is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Pirfenidone attenuates chemokine (CC motif) ligand-2 (CCL2) and CCL12 production with anti-fibrotic activity. Phase 3.
Cancer Biol Ther, 2022, 23(1):150-162
Sci Rep, 2022, 12(1):7
Integr Biol (Camb), 2022, 14(1):1-12
S3032 Bindarit (AF 2838) Bindarit (AF 2838) exhibits selective inhibition against monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 34(6):1911-1918
S3205 Perillaldehyde Perillaldehyde (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.
S3479 R243 R243 is an inhibitor of Chemokine (C-C motif) receptor 8 (CCR8) signaling and chemotaxis.
S7604New BX471

BX471 (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.

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.
Biometals, 2022, 1-14
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00191-0
E0395New Vercirnon Vercirnon (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.
E0486New C-021 C-021 is a potent CCR4 antagonist with IC50 values are 0.14 μM and 39 nM for inhibition of chemotaxis in human and mouse respectively.
S0085 BMS-813160 BMS-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-297006 SB-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.
Cell Death Dis, 2022, 13(5):478
S2003 Maraviroc (UK-427857) Maraviroc (UK-427857) is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM in cell-free assays, respectively. Maraviroc is used in the treatment of HIV infection.
J Exp Clin Cancer Res, 2022, 41(1):81
J Ethnopharmacol, 2022, 289:115051
Biol Pharm Bull, 2022, 45(1):34-41
S3383 RS102895 RS 102895 is a small molecule antagonist of CCR2 with an IC50 of 360 nM.
S6555 AZD2098 AZD2098 is a potent and bioavailable CCR4 receptor antagonist with pIC50 of 7.8.
S7538 RS-102895 Hydrochloride RS-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.
S8220New INCB3344 INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
S8361 PF-4136309 PF-4136309 (INCB8761, PF-04136309) is a potent, selective, and orally bioavailable CCR2 antagonist with an IC50 of 5.2 nM for human CCR2.
S8501 Adaptavir (DAPTA) Adaptavir (DAPTA, D-Ala-peptide T-amide, peptide T) is a water soluble potent, selective CCR5 antagonist which potently inhibits specific CD4-dependent binding of gp120 Bal (IC50 = 0.06 nM) and CM235 (IC50 = 0.32 nM) to CCR5.
Cell Death Dis, 2022, 13(5):478
Proc Natl Acad Sci U S A, 2021, 118(9)e2017282118
FEBS J, 2020, 287(11):2367-2385
S9738New RS504393 RS504393, an extremely selective CC chemokine receptor (CCR) 2 antagonist with IC50 of 98 nM, also targets multiple receptors for inhibition of CCR2b and CCR1 receptors when administrated in higher concentration.
S8324 ZK756326 2HCl ZK756326 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.
Cancer Immunol Immunother, 2022, 10.1007/s00262-022-03196-3
J Exp Med, 2019, 216(12):2763-2777
P1137New Thymulin Thymulin (FTS) is a neuroendocrine hormone with immunoregulatory actions, with anti-inflammatory potential by downregulating the release of inflammatory mediators, such as cytokines and chemokines, upregulating anti-inflammatory factors, such as interleukin (IL)-10, exerting molecular control via the regulation of transcription factors and mediators.
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.
S7604New BX471

BX471 (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.

E0395New Vercirnon Vercirnon (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.
E0486New C-021 C-021 is a potent CCR4 antagonist with IC50 values are 0.14 μM and 39 nM for inhibition of chemotaxis in human and mouse respectively.
S8220New INCB3344 INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
S9738New RS504393 RS504393, an extremely selective CC chemokine receptor (CCR) 2 antagonist with IC50 of 98 nM, also targets multiple receptors for inhibition of CCR2b and CCR1 receptors when administrated in higher concentration.
P1137New Thymulin Thymulin (FTS) is a neuroendocrine hormone with immunoregulatory actions, with anti-inflammatory potential by downregulating the release of inflammatory mediators, such as cytokines and chemokines, upregulating anti-inflammatory factors, such as interleukin (IL)-10, exerting molecular control via the regulation of transcription factors and mediators.
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