CXCR
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) | ||
---|---|---|---|---|
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 |
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-682SX-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 acidTannic 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). |
||
S3013 |
Plerixafor (AMD3100) 8HClPlerixafor (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. |
![]() ![]() 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. |
![]() ![]() 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 |
WZ811WZ811 is a highly potent competitive CXCR4 antagonist with EC50 of 0.3 nM. |
![]() ![]() 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 |
LY2510924LY2510924 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 |
AZD5069AZD5069 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. |
||
S9516新 |
SB 265610SB265610, 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-127MSX-127 (NSC-23026) is a C-X-C chemokine receptor type 4 (CXCR4) receptor antagonist. |
||
S0293 |
MSX-130MSX-130 is an antagonist of C-X-C chemokine receptor type 4 (CXCR4). |
||
S2879 |
AMD3465 hexahydrobromideAMD3465 is a monomacrocyclic CXCR4 antagonist. |
||
S8682 |
AMG 487AMG 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 |
SB225002SB225002 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. |
![]() ![]() 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. |
||
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-927LIT-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-122MSX-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-oxideNicotinamide 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-2341ATI-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 |
UNBS5162UNBS5162 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-682SX-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 acidTannic 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). |
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) 8HClPlerixafor (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. |
2022, 10.1038/s41401-022-00901-x 2022, 10.1002/kjm2.12540 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. |
2022, 10.1021/acsnano.1c07492 2022, 10.1038/s41401-022-00901-x 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 |
WZ811WZ811 is a highly potent competitive CXCR4 antagonist with EC50 of 0.3 nM. |
2022, S1673-8527(22)00125-4 2021, 12(1):652 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 |
LY2510924LY2510924 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 |
AZD5069AZD5069 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. |
2022, 38(10):110490 |
|
S9516新 |
SB 265610SB265610, 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-127MSX-127 (NSC-23026) is a C-X-C chemokine receptor type 4 (CXCR4) receptor antagonist. |
||
S0293 |
MSX-130MSX-130 is an antagonist of C-X-C chemokine receptor type 4 (CXCR4). |
||
S2879 |
AMD3465 hexahydrobromideAMD3465 is a monomacrocyclic CXCR4 antagonist. |
||
S8682 |
AMG 487AMG 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 |
SB225002SB225002 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. |
2022, 14(1):2073785 2022, 12(5):2063-2079 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. |
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-927LIT-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. |
2022, 10.1002/jbm.b.35021 |
|
S6617 |
MSX-122MSX-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-oxideNicotinamide 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-2341ATI-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 |
UNBS5162UNBS5162 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). |