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 8HCl (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
S9665 Motixafortide (BL-8040) 100 mg/mL -1 mg/mL ''''-1 mg/mL
S8506 SCH-527123 <1 mg/mL 79 mg/mL 79 mg/mL
S6617 MSX-122 <1 mg/mL 3 mg/mL <1 mg/mL
S6620 Danirixin (GSK1325756) <1 mg/mL 88 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
S8813 LIT-927 <1 mg/mL 66 mg/mL <1 mg/mL
S4785 Nicotinamide N-oxide -1 mg/mL 8 mg/mL '-1 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 inhibitor of human CXCR1/R2 and rat CXCR2 receptor activation. It also inhibits human CXCL8 receptor activation.

S3013

Plerixafor 8HCl (AMD3100 8HCl)

Plerixafor 8HCl (AMD3100, JM 3100) 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.

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.

S8506

SCH-527123

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

S6617

MSX-122

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

S6620

Danirixin (GSK1325756)

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

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.

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.

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.

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 inhibitor of human CXCR1/R2 and rat CXCR2 receptor activation. It also inhibits human CXCL8 receptor activation.

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 8HCl (AMD3100 8HCl)

Plerixafor 8HCl (AMD3100, JM 3100) 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, 14(4):779-794

2019, 101(1):102-111

2018, 155(3):880-891.e8

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, 10.1016/j.chembiol.2020.01.010

2020, 14(4):779-794

2020, 1 pii: jbc

S2912

WZ811

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

2018, 315(3):L404-L421

2018, 9(6):929-940

2018, 59(6):1451-1460

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.

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.

S8506

SCH-527123

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

S6617

MSX-122

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

S6620

Danirixin (GSK1325756)

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

2019, 9(18):5332-5346

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.

2020, 27;15(4):e0232230

2020, 10.1038/s41416-020-1026-0

2020, 53(1):114-123

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.

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.

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).