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)
カタログ番号	製品カタログ	水	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

All (18) CXCR阻害剤(3) CXCR拮抗剤(13) CXCR作動薬(1) CXCRモジュレータ(1)

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^新	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.	Nat Protoc, 2020, 15(2):421-449 Biomed Pharmacother, 2020, 122:109693 J Exp Clin Cancer Res, 2019, 38(1):461
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.	Mol Oncol, 2020, 14(4):779-794 Biol Reprod, 2019, 101(1):102-111 Gastroenterology, 2018, 155(3):880-891.e8	BLI of NSG mice engrafted with BV173, treated with no therapy (control), plerixafor: 1 mg/kg IP daily, ESKM 100 ug twice weekly, and a combination of ESKM and plerixafor. (A) Logarithmic plot of BLI of leukemia growth measured weekly. Error bars are 5-95% confidence intervals. There was a small but not significant difference between ESKM and combination treated group. (B) End of therapy (day 34) BLI.
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.	Cell Chem Biol, 2020, 10.1016/j.chembiol.2020.01.010 Mol Oncol, 2020, 14(4):779-794 J Biol Chem, 2020, 1 pii: jbc	BLI of NSG mice engrafted with BV173, treated with no therapy (control), plerixafor: 1 mg/kg IP daily, ESKM 100 ug twice weekly, and a combination of ESKM and plerixafor. (A) Logarithmic plot of BLI of leukemia growth measured weekly. Error bars are 5-95% confidence intervals. There was a small but not significant difference between ESKM and combination treated group. (B) End of therapy (day 34) BLI.
S2912	WZ811 WZ811 is a highly potent competitive CXCR4 antagonist with EC50 of 0.3 nM.	Am J Physiol Lung Cell Mol Physiol, 2018, 315(3):L404-L421 J Cancer, 2018, 9(6):929-940 Leuk Lymphoma, 2018, 59(6):1451-1460	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	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^新	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^新	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^新	SCH-527123 SCH-527123 is a potent, orally bioavailable CXCR2/CXCR1 antagonist with IC50 values of 2.6 nM and 36 nM, respectively.
S6617^新	MSX-122 MSX-122 is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM).
S6620^新	Danirixin (GSK1325756) Danirixin (GSK1325756) is a small molecule, non-peptide, high affinity (IC50 for CXCL8 binding = 12.5 nM), selective, and reversible CXCR2 antagonist.	Theranostics, 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.	PLoS One, 2020, 27;15(4):e0232230 Br J Cancer, 2020, 10.1038/s41416-020-1026-0 Shock, 2020, 53(1):114-123	SB225002 could inhibited h-JBMMSCs chemotaxis in both the co-culture and the monoculture transwell systems (n = 3; *P < 0.05).
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^新

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.

Nat Protoc, 2020, 15(2):421-449

Biomed Pharmacother, 2020, 122:109693

J Exp Clin Cancer Res, 2019, 38(1):461

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.	Mol Oncol, 2020, 14(4):779-794 Biol Reprod, 2019, 101(1):102-111 Gastroenterology, 2018, 155(3):880-891.e8	BLI of NSG mice engrafted with BV173, treated with no therapy (control), plerixafor: 1 mg/kg IP daily, ESKM 100 ug twice weekly, and a combination of ESKM and plerixafor. (A) Logarithmic plot of BLI of leukemia growth measured weekly. Error bars are 5-95% confidence intervals. There was a small but not significant difference between ESKM and combination treated group. (B) End of therapy (day 34) BLI.
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.	Cell Chem Biol, 2020, 10.1016/j.chembiol.2020.01.010 Mol Oncol, 2020, 14(4):779-794 J Biol Chem, 2020, 1 pii: jbc	BLI of NSG mice engrafted with BV173, treated with no therapy (control), plerixafor: 1 mg/kg IP daily, ESKM 100 ug twice weekly, and a combination of ESKM and plerixafor. (A) Logarithmic plot of BLI of leukemia growth measured weekly. Error bars are 5-95% confidence intervals. There was a small but not significant difference between ESKM and combination treated group. (B) End of therapy (day 34) BLI.
S2912	WZ811 WZ811 is a highly potent competitive CXCR4 antagonist with EC50 of 0.3 nM.	Am J Physiol Lung Cell Mol Physiol, 2018, 315(3):L404-L421 J Cancer, 2018, 9(6):929-940 Leuk Lymphoma, 2018, 59(6):1451-1460	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	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^新	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^新	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^新	SCH-527123 SCH-527123 is a potent, orally bioavailable CXCR2/CXCR1 antagonist with IC50 values of 2.6 nM and 36 nM, respectively.
S6617^新	MSX-122 MSX-122 is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM).
S6620^新	Danirixin (GSK1325756) Danirixin (GSK1325756) is a small molecule, non-peptide, high affinity (IC50 for CXCL8 binding = 12.5 nM), selective, and reversible CXCR2 antagonist.	Theranostics, 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.	PLoS One, 2020, 27;15(4):e0232230 Br J Cancer, 2020, 10.1038/s41416-020-1026-0 Shock, 2020, 53(1):114-123	SB225002 could inhibited h-JBMMSCs chemotaxis in both the co-culture and the monoculture transwell systems (n = 3; *P < 0.05).
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

S8309

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).

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).

研究分野別

製品類型

CXCR

シグナル伝達経路

研究分野

阻害剤の選択性比較

亜型選択性的な製品

CXCR製品