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Cat. No. | Product Name | ||
---|---|---|---|
L7600 | 趋化因子抑制剂库 | 59 compounds | |
59 种趋化因子或其受体抑制剂的独特集合,可用于高通量筛选和高内涵筛选; |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10905 |
CXCR2-IN-1
|
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。 | |||
T39078 |
CXCR7 antagonist-1
CXCR7 antagonist-1 |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
CXCR7 antagonist-1 是 SDF-1 趋化因子或 I-TAC 与趋化因子受体 CXCR7 结合的特异性拮抗剂。 CXCR7 antagonist-1 可防止肿瘤细胞增殖和肿瘤形成,可用于炎症性疾病的研究。 | |||
T39742 |
CXCR4 antagonist 2
|
Others | Others |
CXCR4 antagonist 2 is a CXCR4 antagonist with an IC 50 value of 47 nM. | |||
T36923 |
CXCR2-IN-2
CXCR2-IN-2 |
Others | Others |
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... | |||
T36982 |
CXCR3 Antagonist 6c
|
Others | Others |
CXCR3 antagonist 6c is an antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3).1It inhibits calcium mobilization induced by chemokine (C-X-C motif) ligand 11 (CXCL11) in HEK293 cells expressing the human receptor (IC50= 0.06 μM). It is selective for CXCR3 over a panel of 14 human G protein-coupled receptors at 10 μM. CXCR3 antagonist 6c inhibits CXCR3-mediated migration of isolated human T cells (IC50= ~100 nM). 1.Cole, A.G., Stroke, I.L., Brescia, M.-R., et al.Identification and initial eva... | |||
T40786 |
CXCR4 antagonist 1
CXCR4 antagonist 1 |
Others | Others |
CXCR4 antagonist 1 is a potent inhibitor of the CXCR4 receptor, with notable anti-HIV activity. | |||
T1955 |
SB225002
|
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。 | |||
T7681 |
AZD-5069
|
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
AZD-5069 是 CXCR2 chemokine 受体拮抗剂,用于癌症的研究。 | |||
T3047 |
SRT3109
|
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。 | |||
T1739 |
WZ811
|
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
WZ811 是可口服的高竞争性CXCR4拮抗剂,抑制细胞中 CXCR4/SDF-1 介导的 cAMP 水平调节和 SDF-1 诱导的基质胶侵入,EC50为 1.2 和 5.2 nM。 | |||
T84325 |
CXCL-CXCR1/2-IN-1
|
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
CXCL-CXCR1/2-IN-1 是一种具有口服活性哈和高效性的 ELR+CXCL-CXCR1/2 通路抑制剂,具有抗癌和抗血管生成活性,可用于研究心血管疾病和癌症。 | |||
T2477 |
UNBS5162
UNBS 5162,UNBS-5162 |
CXCR; Autophagy | Autophagy; GPCR/G Protein; Immunology/Inflammation |
UNBS5162 (UNBS-5162) 是一种新型萘酰亚胺,可降低实验性前列腺癌中 CXCL 趋化因子的表达。它是一种广谱趋化因子配体CXCL 拮抗剂,具有抗肿瘤活性。 | |||
T36443 |
(R,R)-CXCR2-IN-2
(R,R)-CXCR2-IN-2 |
Others | Others |
(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. | |||
T4033 |
MSX-130
MSX 130 |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
MSX-130 是一种CXCR4拮抗剂,可抑制肿瘤转移。 | |||
T9721 |
ML339
|
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
ML339 是有效的CXCR6选择性拮抗剂,IC50为 140 nM。ML339 对 CXCR5,CXCR4,CCR6 和 Apelin 受体 (APJ) 无拮抗作用,IC50>79 μM。ML339 在前列腺癌研究领域有研究的价值。 | |||
T4032 |
MSX-127
MSX 127 |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
MSX-127 是一种CXCR4拮抗剂,可抑制肿瘤转移。 | |||
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。 | |||
T17208 |
USL311
|
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
USL311 是选择性 CXCR4拮抗剂,可防止基质细胞衍生因子 1(SDF-1 或 CXCL12)与 CXCR4 结合。它抑制 CXCR4 活化并减少表达 CXCR4 的肿瘤细胞的增殖和迁移,具有抗肿瘤活性。 | |||
T3992 |
MSX-122
MSX 122,MSX122 |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
MSX-122 是可口服的CXCR4部分拮抗剂,具有抗炎和抗转移活性,可抑制CXCR4/CXCL12相互作用,IC50值约为 10 nM。 | |||
TQ0174 |
Mavorixafor
AMD-070 |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
Mavorixafor (AMD-070) 是一种有效的特异性 CXCR4 拮抗剂,对 CXCR4 125I-SDF 结合的 IC50 值为 13 nM。 Mavorixafor 在 MT-4 细胞 (IC50 = 1 nM) 和 PBMC (IC50 = 9 nM) 中抑制 T-tropic HIV-1 (NL4.3 株) 的复制。 | |||
T8497 |
SX-682
|
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T10297L |
AMG 487
|
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
AMG 487 是可口服的选择性趋化因子受体3拮抗剂,对 I-IP-10、I-ITAC 和 MIG 的 IC50 值分别为 8、15 和 36nM。 | |||
T13324 |
VUF11207 fumarate
|
CXCR; Arrestin | Autophagy; GPCR/G Protein; Immunology/Inflammation |
VUF11207 fumarate 是一种 CXCR7激动剂和高效CXCR7配体,pKi 为 8.1。它可诱导CXCR7的β-arrestin2募集和随后的内在化,pEC50分别为 8.8 和 7.9。 | |||
T7499 |
TAK-779
Takeda 779 |
HIV Protease; CXCR; CCR | Autophagy; GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome |
TAK-779 (Takeda 779) 是一种非肽类CCR5和CXCR3 拮抗剂,对CCR5的Ki 值为 1.1 nM,并选择性抑制R5 HIV-1。 | |||
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。 | |||
T7208 |
AMD 3465 hexahydrobromide
GENZ-644494 (hexahydrobromide) |
HIV Protease; CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome |
AMD 3465 hexahydrobromide (GENZ-644494 (hexahydrobromide)) 是一种 CXCR4受体拮抗剂,具有潜在的抗癌和抗 HIV 活性。 | |||
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。 | |||
T10906 | CXCR7 modulator 1 | Others | Others |
CXCR7 modulator 1 is an effective and orally bioavailable peptoid hybrid CXCR7 modulator with Ki of 9 nM. | |||
T10907 |
CXCR7 modulator 2
|
Others | Others |
CXCR7 modulator 2 is a 7-type C-X-C chemokine receptor (CXCR7) modulator with a Ki of 13 nM. | |||
T33763 |
NVP CXCR2 20
NVP-CXCR2 20,NVP CXCR2-20,NVP CXCR220 |
Others | Others |
NVP CXCR2 20 is an effective selective CXCR2 antagonist (IC50 = 40 nM) with oral bioavailability. | |||
T78879 |
CXCR4-IN-2
|
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
CXCR4-IN-2(compound A1)是一款具有抗癌活性的双功能氟化小分子,是CXCR4的强效抑制剂。它对小鼠结直肠癌(CRC)细胞展现出显著的细胞毒性(IC50:60 μg/mL;72小时)和抗增殖能力,能够引导细胞在G2/M期发生阻滞并诱导细胞凋亡(apoptosis)。 | |||
T61356 |
CXCR2 antagonist 3
|
Others | Others |
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]. | |||
T64306 |
CXCR4 probe 1
|
Others | Others |
CXCR4 probe 1 (compound 5) 是一种有效地、特异性的 CXCR4 靶向 PET 示踪剂,能够作用于 CXCR4 特异性拮抗剂 TN14003 (IC50: 6.9 nM)。CXCR4 probe 1 具有潜力作为 CXCR4 特异性成像探针,用于炎性疾病、CXCR4 阳性肿瘤和转移性肿瘤的诊断和预后监测。 | |||
T60696 |
CXCR2 antagonist 8
|
Others | Others |
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。 | |||
T79059 |
CXCR4-IN-1
|
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
CXCR4-IN-1 (Example C5) 为CXCR4抑制剂,IC50值为20 nM。该化合物主要适用于癌症、HIV、糖尿病视网膜病变、炎症等领域的研究。 | |||
T62352 |
CXCR4 modulator-2
|
Others | Others |
CXCR4 modulator-2 (compound Z7R) 是一种 CXCR4 的高效调节剂 (IC50: 1.25 nM)。CXCR4 modulator-2 在小鼠血清中表现出较好的稳定性 (t1/2= 77.1 min),在小鼠水肿模型中具有抗炎作用。 | |||
T6764 |
ATI-2341
ATI2341 |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
ATI-2341 是 C-X-C 趋化因子受体 4 型功能选择性变构激动剂,作为偏向配体有利于 Gα1 激活。它是一种变构激动剂,可激活抑制性异源三聚体 G 蛋白 (Gi) 以促进抑制 cAMP 产生并诱导钙动员。 | |||
T63369 |
CXCR4 antagonist 4
|
||
CXCR4 antagonist 4 是口服具有活力的、有效的CXCR4拮抗剂,IC50 值为 24 nM。CXCR4 antagonist 4能够抑制 CYP 2D6 的活性,增加 PAMPA 的通透性,有效阻碍人类免疫缺陷病毒的进入 (IC50=7 nM)。 | |||
T61409 |
CXCR4 antagonist 3
|
Others | Others |
CXCR4 antagonist 3 (compound 12a), an effective antagonist of CXCR4, exhibits an IC50 of 11 nM. It is a congener of TIQ15, showcasing exceptional properties such as CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. With its potential for research on the human immunodeficiency virus, CXCR4 antagonist 3 holds great promise [1]. | |||
T61236 |
CXCR2 antagonist 7
|
Others | Others |
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)。 | |||
T61363 |
CXCR4 antagonist 8
|
Others | Others |
CXCR4 antagonist 8 (Compound 3) is a potent inhibitor of CXCR4. It demonstrates an IC50 value of 57 nM in CXCR4 antagonism. In addition, it effectively inhibits the increase in cytosolic calcium induced by CXCL12 with an IC50 value of 0.24 nM. Furthermore, Compound 3 shows efficacy in the inhibition of CXCL12/CXCR4-mediated cell migration [1]. | |||
T80216 |
DOTA-CXCR4-L
|
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
DOTA-CXCR4-L为针对CXCR4的靶向肽,适用于癌症研究,如胶质母细胞瘤和三阴性乳腺癌。 | |||
T61359 |
CXCR2 antagonist 6
|
Others | Others |
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)。 | |||
T61419 |
CXCR4 antagonist 5
|
Others | Others |
CXCR4 antagonist 5 (compound 23), a potent CXCR4 antagonist, exhibits high inhibition efficacy against CXCR4 with an IC50 value of 8.8 nM. It effectively suppresses CXCL12-induced cytosolic calcium increase (IC50 = 0.02 nM) and hinders CXCR4/CXCL12-mediated chemotaxis. Moreover, Compound 23 demonstrates favorable physicochemical properties and in vitro safety profiles, exhibiting only marginal to moderate inhibition of CYP isozymes and hERG [1]. | |||
T61420 |
CXCR4 antagonist 6
|
Others | Others |
CXCR4 antagonist 6 (compound 46) is a highly potent inhibitor of CXCR4 with an IC50 value of 79 nM. It effectively inhibits the cytosolic calcium flux induced by CXCL12, achieving an IC50 of 0.25 nM. Moreover, CXCR4 antagonist 6 demonstrates significant mitigation of cell migration mediated by the CXCL12/CXCR4 interaction. Notably, this compound exhibits remarkable efficacy in a mouse model of cancer metastasis [1]. | |||
T62325 |
CXCR7 antagonist-1 hydrochloride
|
Others | Others |
CXCR7 antagonist-1 hydrochloride 是一种 CXCR7 拮抗剂,对 SDF-1 趋化因子(也称为 CXCL12 趋化因子)或 I-TAC(也称为 CXCL11)与趋化因子受体 CXCR7 结合具有抑制作用。CXCR7 antagonist-1 hydrochloride 能够用于肿瘤细胞增殖,肿瘤形成,炎症疾病和许多其他疾病的预防。 | |||
T61650 |
CXCR4 antagonist 9
|
Others | Others |
CXCR4 antagonist 9 (Compound 2) is a potent CXCR4 antagonist displaying an IC50 of 15 nM. It effectively inhibits the cytosolic calcium increase induced by CXCL12, with an IC50 value of 1.3 nM [1]. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3396 |
Baohuoside I
Icariside-II,宝藿苷I,Icariin-II,宝藿苷 I |
Apoptosis; CXCR | Apoptosis; Autophagy; GPCR/G Protein; Immunology/Inflammation |
Baohuoside I (Icariside-II) 是从朝鲜淫羊藿中得到的一种黄酮类天然产物,是CXCR4抑制剂,抑制 CXCR4 的表达,诱导凋亡,具有抗肿瘤活性。 | |||
T3S1416 |
Decursin
Decursinol angelate,前胡素,(+)-Decursin,紫花前胡素 |
Apoptosis; PKC | Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling |
Decursin (Decursinol angelate) 是一种细胞毒性剂,是一种来自朝鲜当归根的有效蛋白激酶 C 激活剂。它通过 Hippo/YAP 信号通路抑制 HepG2 细胞的生长。它通过下调 CXCR7 表达来抑制胃癌中的肿瘤生长,迁移和侵袭。 | |||
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。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPH-02612 |
CXCR3 Protein, Mouse, Recombinant (His & KSI)
CXC-R3,CKR-L2,CXCR3,CD183,GPR9,Interferon-inducible... |
Mouse | E. coli |
Receptor for the C-X-C chemokine CXCL9, CXCL10 and CXCL11 and mediates the proliferation, survival and angiogenic activity of mesangial cells through a heterotrimeric G-protein signaling pathway. Probably promotes cell chemotaxis response. Binds to CCL21. | |||
TMPH-01162 |
CXCR3 Protein, Human, Recombinant (GST & His)
IP-10 receptor,CXCR3,CXC-R3,GPR9,Interferon-inducib... |
Human | E. coli |
CXCR3 Protein, Human, Recombinant (GST & His) is expressed in E. coli. | |||
TMPY-06553 |
CXCR4 Protein, Human, Recombinant
NPYY3R,chemokine (C-X-C motif) receptor 4,D2S201E,HM89,NPYRL... |
Human | HEK293 Cells |
CXCR4 Protein, Human, Recombinant is expressed in HEK293 mammalian cells. The predicted molecular weight is 39.75 kDa and the accession number is P61073-1. | |||
TMPJ-01037 |
CXCR4 Protein, Human, Recombinant (hFc)
CXCR4,CD184,Fusin,D2S201E,FB22,HM89,HSY3RR,LAP3,LCR... |
Human | HEK293 Cells |
C-X-C chemokine receptor type 4 (CXCR4) is an alpha-chemokine receptor specific for stromal-derived-factor-1 (SDF-1 also called CXCL12), a molecule endowed with potent chemotactic activity for lymphocytes. This receptor is one of several chemokine receptors that HIV isolates can use to infect CD4+ T cells. CXCR4 stands out for its pleiotropic roles in both physiological and pathological conditions and it represents a crucial target in drug development. CXCL12 is the principal CXCR4 specific liga... | |||
TMPJ-00760 |
CXCL7 Protein, Human, Recombinant
SCYB7,C-X-C Motif Chemokine 7,Leukocyte-Derived Growth Facto... |
Human | E. coli |
Human Chemokine (C-X-C motif) Ligand 7 (CXCL7), also known as neutrophil activating peptide 2 (NAP-2), is a member of the CXC chemokines containing an ELR domain (Glu-Leu-Arg tripeptide motif). Similar to other ELR domain containing CXC chemokines, such as IL-8 and the GRO proteins, CXCL7 binds CXCR2, chemoattracts and activates neutrophils. CXCL7, Connective Tissue Activating Protein III (CTAPIII) and βthrombogulin (βTG), are proteolytically processed carboxylterminal fragments of platelet basi... |