CXCR

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S8947 SX-682 ˂1 mg/mL 93 mg/mL 93 mg/mL
S3951 Tannic acid -1 mg/mL 100 mg/mL -1 mg/mL
S8640 Reparixin (Repertaxin) <1 mg/mL 56 mg/mL '56 mg/mL
S3013 Plerixafor (AMD3100) 8HCl 100 mg/mL <1 mg/mL <1 mg/mL
S8030 Plerixafor (AMD3100) 3 mg/mL <1 mg/mL 100 mg/mL
S2912 WZ811 <1 mg/mL 30 mg/mL <1 mg/mL
S8505 LY2510924 100 mg/mL -1 mg/mL -1 mg/mL
S6645 AZD5069 <1 mg/mL 95 mg/mL 7 mg/mL
S9725 Balixafortide (POL6326) 100 mg/mL -1 mg/mL '-1 mg/mL
S8682 AMG 487 <1 mg/mL 100 mg/mL ''100 mg/mL
S9665 Motixafortide (BL-8040) 100 mg/mL -1 mg/mL '-1 mg/mL
S2879 AMD3465 hexahydrobromide 98 mg/mL 2 mg/mL <1 mg/mL
S7651 SB225002 <1 mg/mL 70 mg/mL 3 mg/mL
S6620 Danirixin (GSK1325756) <1 mg/mL 88 mg/mL ''<1 mg/mL
S8813 LIT-927 <1 mg/mL 66 mg/mL <1 mg/mL
S6617 MSX-122 <1 mg/mL 3 mg/mL <1 mg/mL
S4785 Nicotinamide N-oxide -1 mg/mL 8 mg/mL -1 mg/mL
S8506 SCH-527123 <1 mg/mL 79 mg/mL 79 mg/mL
S8309 ATI-2341 <1 mg/mL 100 mg/mL 2 mg/mL
S8869 UNBS5162 <1 mg/mL 17 mg/mL <1 mg/mL

亜型選択性的な製品

CXCR製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S8947

SX-682

SX-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.

S3951

Tannic acid

Tannic acid (Gallotannic acid), a polyphenolic compound, is a CXCL12/CXCR4 inhibitor with antiangiogenic, anti-inflammatory and antitumor activity.

S8640

Reparixin (Repertaxin)

Reparixin (Repertaxin) is a potent and specific inhibitor of CXCR1 with IC50 of 1 nM. Reparixin (Repertaxin) inhibits PMN migration induced by CXCL8 (IC50 = 1 nM) and rodent PMN chemotaxis induced by CXCL1 and CXCL2. Repertaxin inhibits the response of human PMN to CXCL1, which interacts with CXCR2 (IC50 = 400 nM).

S3013

Plerixafor (AMD3100) 8HCl

Plerixafor (AMD3100, JM 3100) 8HCl is the hydrochloride of Plerixafor, a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively. Plerixafor can be used as an anti-HIV agent.

S8030

Plerixafor (AMD3100)

Plerixafor (AMD3100, JM 3100) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively. Plerixafor inhibits human immunodeficiency virus (HIV) replication.

S2912

WZ811

WZ811 is a highly potent competitive CXCR4 antagonist with EC50 of 0.3 nM.

S8505

LY2510924

LY2510924 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

AZD5069

AZD5069 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.

S9725

Balixafortide (POL6326)

Balixafortide (POL6326) is an orally bioavailable peptidic CXC chemokine receptor 4 (CXCR4) antagonist.

S8682

AMG 487

AMG 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.

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.

S2879

AMD3465 hexahydrobromide

AMD3465 is a monomacrocyclic CXCR4 antagonist.

S7651

SB225002

SB225002 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.

S6620

Danirixin (GSK1325756)

Danirixin (GSK1325756) is a small molecule, non-peptide, high affinity (IC50 for CXCL8 (IL-8) binding = 12.5 nM), selective, and reversible CXCR2 antagonist.

S8813

LIT-927

LIT-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-122

MSX-122 is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM).

S4785

Nicotinamide N-oxide

Nicotinamide 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.

S8506

SCH-527123

SCH-527123 is a potent, orally bioavailable CXCR2/CXCR1 antagonist with IC50 values of 2.6 nM and 36 nM, respectively.

S8309

ATI-2341

ATI-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

UNBS5162

UNBS5162 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).

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S8947

SX-682

SX-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.

S3951

Tannic acid

Tannic acid (Gallotannic acid), a polyphenolic compound, is a CXCL12/CXCR4 inhibitor with antiangiogenic, anti-inflammatory and antitumor activity.

S8640

Reparixin (Repertaxin)

Reparixin (Repertaxin) is a potent and specific inhibitor of CXCR1 with IC50 of 1 nM. Reparixin (Repertaxin) inhibits PMN migration induced by CXCL8 (IC50 = 1 nM) and rodent PMN chemotaxis induced by CXCL1 and CXCL2. Repertaxin inhibits the response of human PMN to CXCL1, which interacts with CXCR2 (IC50 = 400 nM).

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S3013

Plerixafor (AMD3100) 8HCl

Plerixafor (AMD3100, JM 3100) 8HCl is the hydrochloride of Plerixafor, a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively. Plerixafor can be used as an anti-HIV agent.

2020, 18:161-170

2020, 14(4):779-794

2020, 15:5701-5718

S8030

Plerixafor (AMD3100)

Plerixafor (AMD3100, JM 3100) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively. Plerixafor inhibits human immunodeficiency virus (HIV) replication.

2020, 11(1):5400

2020, 33(1):108221

2020, 11(8):707

S2912

WZ811

WZ811 is a highly potent competitive CXCR4 antagonist with EC50 of 0.3 nM.

2021, 12(1):652

2020, 33(1):108221

2019, 10(9):648

S8505

LY2510924

LY2510924 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

AZD5069

AZD5069 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.

S9725

Balixafortide (POL6326)

Balixafortide (POL6326) is an orally bioavailable peptidic CXC chemokine receptor 4 (CXCR4) antagonist.

S8682

AMG 487

AMG 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.

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.

S2879

AMD3465 hexahydrobromide

AMD3465 is a monomacrocyclic CXCR4 antagonist.

S7651

SB225002

SB225002 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.

2021, S1525-0016(21)00019-8

2021, 21(2):163

2020, 11(8):707

S6620

Danirixin (GSK1325756)

Danirixin (GSK1325756) is a small molecule, non-peptide, high affinity (IC50 for CXCL8 (IL-8) binding = 12.5 nM), selective, and reversible CXCR2 antagonist.

2019, 9(18):5332-5346

S8813

LIT-927

LIT-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-122

MSX-122 is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM).

S4785

Nicotinamide N-oxide

Nicotinamide 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.

S8506

SCH-527123

SCH-527123 is a potent, orally bioavailable CXCR2/CXCR1 antagonist with IC50 values of 2.6 nM and 36 nM, respectively.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S8309

ATI-2341

ATI-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.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S8869

UNBS5162

UNBS5162 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).