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Cat. No. | Product Name | Target | Signaling Pathways |
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T10905 |
CXCR2-IN-1
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CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
CXCR2-IN-1是可渗透中枢神经系统的 CXCR2拮抗剂,pIC50值为9.3。 | |||
T16850 |
SB-265610
GSK-CXCR2 |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
SB-265610 (GSK-CXCR2) 是竞争性非肽变构CXCR2选择性拮抗剂,可阻断大鼠 CINC-1 诱导的钙动员和中性粒细胞趋化性,IC50分别为 3.7 和 70 nM。 | |||
T33763 |
NVP CXCR2 20
NVP-CXCR2 20,NVP CXCR2-20,NVP CXCR220 |
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NVP CXCR2 20 is an effective selective CXCR2 antagonist (IC50 = 40 nM) with oral bioavailability. | |||
T36923 |
CXCR2-IN-2
CXCR2-IN-2 |
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CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM[1]. CXCR2-IN-2 (compound 68) (1-10 mg/kg; p.o.; twice daily for 3 days) dose-dependently reduces neutrophil infiltration in vivo in ra... | |||
T36443 |
(R,R)-CXCR2-IN-2
(R,R)-CXCR2-IN-2 |
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(R,R)-CXCR2-IN-2, diastereoisomer of CXCR2-IN-2 (compound 68), is a brain penetrant CXCR2 antagonist with a pIC50 of 9 and 6.8 in the Tango assay and d in the HWB Gro-α induced CD11b expression assay, respectively[1]. [1]. Lu H, et al. Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists. J Med Chem. 2018;61(6):2518-2532. | |||
T61236 | CXCR2 antagonist 7 | ||
CXCR2 antagonist 7 (compound 19) 是一种有效的CXCR2拮抗剂。CXCR2 antagonist 7 显示出有效的CXCR2结合亲和力 (IC50=0.044 μM) 和钙动员 (IC50=0.66 μM)。 | |||
T60696 |
CXCR2 antagonist 8
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CXCR2 antagonist 8 是可用于研究胰岛素抵抗的,CXCR2受体的选择性拮抗剂。 | |||
T61356 |
CXCR2 antagonist 3
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CXCR2 antagonist 3 (compound 11h) is a highly effective antagonist of CXC chemokine receptor 2 (CXCR2). It displays potent activity in inhibiting neutrophil infiltration into the air pouch, with double-digit nanomolar potencies against CXCR2. Moreover, CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs, while enhancing the infiltration of CD3+ T lymphocytes into Pan02 tumor tissues [1]. | |||
T61235 | CXCR2 antagonist 5 | ||
CXCR2 antagonist 5 (compound 25) 是一种有效的CXCR2拮抗剂。 CXCR2 antagonist 5 显示出有效的CXCR2结合亲和力 (IC50=0.013 μM) 和钙动员 (IC50=0.1 μM)。 | |||
T61386 | CXCR2 antagonist 2 | ||
CXCR2 antagonist 2 是一种有效的癌症免疫治疗的 CXCR2拮抗剂,IC50值为 95 nM。 | |||
T61447 | CXCR2 antagonist 4 | ||
CXCR2 antagonist 4 (compound 7) is a highly potent antagonist that inhibits CXCR2 with an IC50 value of 0.13 μM. It also effectively inhibits the cytosolic calcium increase induced by CXCL8, with an IC50 value of 27 μM. CXCR2 antagonist 4 shows promising potential for anticancer research [1]. | |||
T61359 | CXCR2 antagonist 6 | ||
CXCR2 antagonist 6 (compound 35c) 是一种有效的CXCR2拮抗剂。CXCR2 antagonist 6 显示出有效的CXCR2结合亲和力 (IC50=0.43 μM) 和钙动员 (IC50=0.11 μM)。 | |||
T11179 |
Elubrixin
SB-656933 |
IL Receptor; CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
Elubrixin (SB-656933) 是一种有效和特异性的 CXCR2 和 IL-8 受体拮抗剂。 Elubrixin 可用于炎症性疾病的研究,例如炎症性肠病和气道炎症。 | |||
T1955 |
SB225002
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CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
SB225002 是一种有效的选择性 CXCR2 拮抗剂,抑制白介素 IL-8 与 CXCR2 的结合,IC50为 22 nM。 | |||
T5193 |
Danirixin
GSK1325756 |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
Danirixin (GSK1325756) 是一种选择性可逆的CXCR2拮抗剂,抑制 CXCL8 的IC50值为 12.5 nM。 | |||
T7681 |
AZD-5069
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CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
AZD-5069 是 CXCR2 chemokine 受体拮抗剂,用于癌症的研究。 | |||
T7130 |
Navarixin
MK-7123,SCH 527123 |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
Navarixin (MK-7123) 是一种可口服的 CXCR1和 CXCR2变构拮抗剂,对猕猴 CXCR1的 Kd 值为 41 nM,对大小鼠和猕猴 CXCR2的 Kd 值分别为 0.20、0.20 和 0.08 nM。 | |||
T4163 |
Reparixin
DF 1681Y,Repertaxin,瑞帕利辛 |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
Reparixin (Repertaxin) 是两种 CXCL8 受体 CXCR1/2 的强效抑制剂,它对 CXCR2 介导的细胞迁移具有微弱的抑制作用 ,IC50为 100 nM。它强烈阻断 CXCR1 介导的趋化性,IC50为 1 nM。 | |||
T3047 |
SRT3109
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CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
SRT3109 是 CXCR2拮抗剂,pIC50值为 8.2,可用于趋化因子介导的疾病研究。 | |||
T14384 |
AZD8797
KAN-0440567,KAND567 |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
AZD8797 (KAND567) 是一种可口服且具有选择性和有效性的人 CX3CR1 变构拮抗剂,对 CX3CR1 和 CXCR2 具有抑制作用,对SARS-CoV-2诱导的神经元损伤有潜在的保护作用,可防止癫痫发作后偏头痛模型大鼠痛觉过敏和小胶质细胞活化的恶化。 | |||
T25131 |
AZD8309
AZD 8309,AZD-8309 |
Glutathione Peroxidase; CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation; Metabolism |
AZD8309 是一种强效的、可口服的趋化因子受体CXCR2的拮抗剂, 能够调节中性粒细胞的转运,可显著降低胰腺和肺部的MPO,并降低胰腺内的胰蛋白酶和弹性蛋白酶活性。AZD8309 能够用于研究炎症系列疾病。 | |||
T76662 |
Ac-Pro-Gly-Pro-OH
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Apoptosis; CXCR; Antibiotic | Apoptosis; Autophagy; GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology |
Ac-Pro-Gly-Pro-OH 是乙酰基修饰的三肽化合物,可用作 CXCR2 激动剂。Ac-Pro-Gly-Pro-OH 具有杀菌和抗炎活性,抑制免疫细胞凋亡,抑制促炎细胞因子的产生。Ac-Pro-Gly-Pro-OH 可用于研究脓毒症和肺部炎症。 | |||
T8497 |
SX-682
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CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
SX-682 是口服有效的 CXCR1和 CXCR2变构抑制剂,可以阻断肿瘤髓系抑制细胞募集并增强 T 细胞活化和抗肿瘤免疫,具有治疗去势抵抗性前列腺癌的潜力。 | |||
T16864 |
SCH 563705
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CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
SCH 563705 is an effective and orally available CXCR2 and CXCR1 antagonist (IC50s: 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively). | |||
T16933 |
SRT3190
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CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
SRT3190 is an antagonist of CXCR2. | |||
T27255 |
Elubrixin HCl
SB656933,SB-656933AAF,SB-656933-AAF,SB 656933,SB-656933 AAF,SB-656933 |
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Elubrixin is a interleukin 8 inhibitor and CXCR2 selective antagonist. | |||
T34544 |
SB-332235
SB332235,SB 332235 |
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SB-332235 is an effective specific CXCR2 antagonist. And it is effectively inhibited CS-induced neutrophilia in a dose-dependent manner. | |||
T38850 |
AZD4721
RIST4721,AZD4721 |
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AZD4721 (RIST4721) is the potent and orally active antagonist of acidic CXC chemokine receptor 2 ( CXCR2 ). AZD4721 has the potential for the research of inflammatory disease. | |||
T26699 |
AZ10397767
AZ 10397767,AZ-10397767 |
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AZ10397767 is a potent CXCR2 antagonist (IC50 = 1 nM). AZ10397767 significantly reduced the numbers of infiltrating neutrophils into both in vitro and in vivo tumor models. | |||
T32533 |
Ladarixin
DF 2156A,DF2156A,DF-2156,DF 2156,DF-2156A,DF2156 |
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Ladarixin is a dual, non-competitive allosteric inhibitor of CXCR1 and CXCR2 interleukin8 (IL-8a and IL-8b, respectively). The efficacy of CXCR1/2 inhibition prevents inflammation and autoimmune-mediated islet damage. | |||
T41121 |
Elubrixin tosylate
SB-656933 tosylate,Elubrixin tosylate |
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Elubrixin tosylate (SB-656933 tosylate) is a high-potency, selective, competitive, and reversible CXCR2 antagonist, as well as an antagonist of the IL-8 receptor. It effectively inhibits upregulation of neutrophil CD11b (with an IC50 of 260.7 nM) and shape change (with an IC50 of 310.5 nM). This compound holds promise for the study of inflammatory diseases, including inflammatory bowel disease and airway inflammation. | |||
T79050 |
JBI-589
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JBI-589为一种非共价、选择性PAD4抑制剂,可降低CXCR2表达,阻断中性粒细胞趋化性;此外,JBI-589能减小原发肿瘤体积及其转移,并增强检查点抑制剂的抗肿瘤效果。 | |||
T75642 | Corydalmine hydrochloride | ||
Corydalmine hydrochloride 抑制某些植物病原体的孢子萌发以及腐生真菌。Corydalmine hydrochloride 具有口服活性,可用于缓解疼痛的研究。Corydalmine hydrochloride 通过抑制 NF-κB 依赖性的 CXCL1/CXCR2信号传导途径,可缓解 Vincristine 引起的神经性疼痛。 | |||
T36623 |
Antileukinate
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Antileukinate is a synthetic hexapeptide with an acetylated amino terminus and an amidated carboxyl terminus that inhibits the binding of CXC chemokines to the chemokine receptor CXCR2. It inhibits IL-8 binding to neutrophils (Ki = 2.7-13 μM), prevents neutrophil chemotaxis and β-glucuronidase release, and blocks IL-8-induced skin edema in rabbits. At 53 mg/kg, antileukinate has been shown to protect mice against acute pancreatitis and associated lung injury. | |||
T12705 |
Reparixin L-lysine salt
REPERTAXIN L-赖氨酸盐,Repertaxin L-lysine salt |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
Reparixin L-lysine salt (Repertaxin L-lysine salt) 是趋化因子受体1/2 活化的变构抑制剂。 |
Cat. No. | Product Name | Target | Signaling Pathways |
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T0617 |
Nicotinamide N-oxide
Nicotinamide-N-oxide,Nicotinamide 1-oxide,N-氧代烟酰胺,烟酰胺-N-氧化物,1-oxynicotinamide |
c-Myc; Endogenous Metabolite; CXCR; Drug Metabolite | Autophagy; Cell Cycle/Checkpoint; GPCR/G Protein; Immunology/Inflammation; Metabolism |
Nicotinamide N-oxide (Nicotinamide 1-oxide) 是生物体内烟酰胺分解代谢物,是高效选择性CXCR2受体拮抗剂。 |