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 (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
S9516	SB 265610	<1 mg/mL	71 mg/mL	4 mg/mL
S0292	MSX-127	<1 mg/mL	62 mg/mL	'''<1 mg/mL
S0293	MSX-130	<1 mg/mL	3 mg/mL	'''<1 mg/mL
S2879	AMD3465 hexahydrobromide	98 mg/mL	2 mg/mL	<1 mg/mL
S8682	AMG 487	<1 mg/mL	100 mg/mL	''100 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
S9665	Motixafortide (BL-8040)	100 mg/mL	-1 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
S9725	Balixafortide (POL6326)	100 mg/mL	-1 mg/mL	'-1 mg/mL
S4785	Nicotinamide N-oxide	-1 mg/mL	8 mg/mL	-1 mg/mL
S8506	Navarixin (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

All (23) CXCR阻害剤(3) CXCR拮抗剤(18) 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	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, DF 1681Y) 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).	Cell Rep, 2022, 38(10):110490 Cell Death Discov, 2022, 8(1):235 J Exp Clin Cancer Res, 2021, 40(1):87
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.	Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00901-x Kaohsiung J Med Sci, 2022, 10.1002/kjm2.12540 Nat Cell Biol, 2021, 10.1038/s41556-021-00766-y	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, SID791) 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.	ACS Nano, 2022, 10.1021/acsnano.1c07492 Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00901-x Kaohsiung J Med Sci, 2022, 10.1002/kjm2.12540	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.	J Genet Genomics, 2022, S1673-8527(22)00125-4 Nat Commun, 2021, 12(1):652 Cell Rep, 2020, 33(1):108221	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	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.	Cell Rep, 2022, 38(10):110490
S9516^新	SB 265610 SB265610, a competitive antagonist at the human CXCR2 receptor, can displace [125I]-IL-8 and [125I]-GROα with pIC50 values of 8.41 and 8.47 respectively, preventing receptor activation by binding to a region distinct from the agonist binding site.
S0292	MSX-127 MSX-127 (NSC-23026) is a C-X-C chemokine receptor type 4 (CXCR4) receptor antagonist.
S0293	MSX-130 MSX-130 is an antagonist of C-X-C chemokine receptor type 4 (CXCR4).
S2879	AMD3465 hexahydrobromide AMD3465 is a monomacrocyclic 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.
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.	Gut Microbes, 2022, 14(1):2073785 Theranostics, 2022, 12(5):2063-2079 Oncogene, 2022, 10.1038/s41388-021-01920-4	SB225002 could inhibited h-JBMMSCs chemotaxis in both the co-culture and the monoculture transwell systems (n = 3; *P < 0.05).
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.	Theranostics, 2019, 9(18):5332-5346
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.
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.	J Biomed Mater Res B Appl Biomater, 2022, 10.1002/jbm.b.35021
S6617	MSX-122 MSX-122 is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM).
S9725	Balixafortide (POL6326) Balixafortide (POL6326) is an orally bioavailable peptidic CXC chemokine receptor 4 (CXCR4) antagonist.
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	Navarixin (SCH-527123) Navarixin (SCH-527123, MK-7123, PS-291822) 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, DF 1681Y) 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).

Cell Rep, 2022, 38(10):110490

Cell Death Discov, 2022, 8(1):235

J Exp Clin Cancer Res, 2021, 40(1):87

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.	Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00901-x Kaohsiung J Med Sci, 2022, 10.1002/kjm2.12540 Nat Cell Biol, 2021, 10.1038/s41556-021-00766-y	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, SID791) 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.	ACS Nano, 2022, 10.1021/acsnano.1c07492 Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00901-x Kaohsiung J Med Sci, 2022, 10.1002/kjm2.12540	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.	J Genet Genomics, 2022, S1673-8527(22)00125-4 Nat Commun, 2021, 12(1):652 Cell Rep, 2020, 33(1):108221	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	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.	Cell Rep, 2022, 38(10):110490
S9516^新	SB 265610 SB265610, a competitive antagonist at the human CXCR2 receptor, can displace [125I]-IL-8 and [125I]-GROα with pIC50 values of 8.41 and 8.47 respectively, preventing receptor activation by binding to a region distinct from the agonist binding site.
S0292	MSX-127 MSX-127 (NSC-23026) is a C-X-C chemokine receptor type 4 (CXCR4) receptor antagonist.
S0293	MSX-130 MSX-130 is an antagonist of C-X-C chemokine receptor type 4 (CXCR4).
S2879	AMD3465 hexahydrobromide AMD3465 is a monomacrocyclic 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.
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.	Gut Microbes, 2022, 14(1):2073785 Theranostics, 2022, 12(5):2063-2079 Oncogene, 2022, 10.1038/s41388-021-01920-4	SB225002 could inhibited h-JBMMSCs chemotaxis in both the co-culture and the monoculture transwell systems (n = 3; *P < 0.05).
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.	Theranostics, 2019, 9(18):5332-5346
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.
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.	J Biomed Mater Res B Appl Biomater, 2022, 10.1002/jbm.b.35021
S6617	MSX-122 MSX-122 is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM).
S9725	Balixafortide (POL6326) Balixafortide (POL6326) is an orally bioavailable peptidic CXC chemokine receptor 4 (CXCR4) antagonist.
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	Navarixin (SCH-527123) Navarixin (SCH-527123, MK-7123, PS-291822) 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

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).

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