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Search Results for " cxcr "

59

抑制剂 & 化合物

3

天然产物

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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
	CXCR4 antagonist 2 is a CXCR4 antagonist with an IC 50 value of 47 nM.
T40786	CXCR4 antagonist 1 CXCR4 antagonist 1
	CXCR4 antagonist 1 is a potent inhibitor of the CXCR4 receptor, with notable anti-HIV activity.
T36923	CXCR2-IN-2 CXCR2-IN-2
	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...
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。
T36982	CXCR3 Antagonist 6c
	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...
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。
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。
T36443	(R,R)-CXCR2-IN-2 (R,R)-CXCR2-IN-2
	(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.
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
T10906	CXCR7 modulator 1	Others	Others
	CXCR7 modulator 1 is an effective and orally bioavailable peptoid hybrid CXCR7 modulator with Ki of 9 nM.
T33763	NVP CXCR2 20 NVP-CXCR2 20,NVP CXCR2-20,NVP CXCR220
	NVP CXCR2 20 is an effective selective CXCR2 antagonist (IC50 = 40 nM) with oral bioavailability.
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.
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)。
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)。
T61409	CXCR4 antagonist 3
	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].
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)。
T61363	CXCR4 antagonist 8
	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].
T61420	CXCR4 antagonist 6
	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].
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。
T61356	CXCR2 antagonist 3
	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].
T60696	CXCR2 antagonist 8
	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。
T64306	CXCR4 probe 1
	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。
T62007	CXCR4 modulator-1
	CXCR4 modulator-1 (compound ZINC72372983) 是有效的CXCR4调节剂（EC50= 100 nM）。CXCR4 modulator-1 在抗炎、抗癌及抗 HIV 感染方面有研究价值。
T61419	CXCR4 antagonist 5
	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].
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)。
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。
T62352	CXCR4 modulator-2
	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。
T62325	CXCR7 antagonist-1 hydrochloride
	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。
T1776	Plerixafor 普乐沙福,JM3100,AMD 3100,AMD-3329	Virus Protease; HIV Protease; CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	Plerixafor (AMD-3329) 是一种趋化因子受体拮抗剂，可阻断基质细胞衍生因子与细胞受体 CXCR4 的结合。它也是 CXCR7 的变构激动剂，是免疫刺激剂和造血干细胞动员剂，还抑制HIV-1和HIV-2的复制，EC50为 1-10 nM。

化合物

Cat.No: T10905

Target: CXCR

CXCR7 antagonist-1

Cat.No: T39078

Synonym: CXCR7 antagonist-1

Target: CXCR

CXCR4 antagonist 2

Cat.No: T39742

CXCR4 antagonist 1

Cat.No: T40786

Synonym: CXCR4 antagonist 1

Cat.No: T36923

Synonym: CXCR2-IN-2

Cat.No: T1955

Target: CXCR

CXCR3 Antagonist 6c

Cat.No: T36982

Cat.No: T3047

Target: CXCR

Cat.No: T7681

Target: CXCR

(R,R)-CXCR2-IN-2

Cat.No: T36443

Synonym: (R,R)-CXCR2-IN-2

Cat.No: T1739

Target: CXCR

Cat.No: T9721

Target: CXCR

Cat.No: T3992

Synonym: MSX 122,MSX122

Target: CXCR

Cat.No: T5193

Synonym: GSK1325756

Target: CXCR

Cat.No: T17208

Target: CXCR

Cat.No: T4032

Synonym: MSX 127

Target: CXCR

Cat.No: T2477

Synonym: UNBS 5162,UNBS-5162

Target: CXCR, Autophagy

Cat.No: T4033

Synonym: MSX 130

Target: CXCR

Cat.No: T4163

Synonym: DF 1681Y,Repertaxin,瑞帕利辛

Target: CXCR

Cat.No: TQ0174

Synonym: AMD-070

Target: CXCR

Cat.No: T8497

Target: CXCR

Cat.No: T11179

Synonym: SB-656933

Target: IL Receptor, CXCR

Cat.No: T10297L

Target: CXCR

VUF11207 fumarate

Cat.No: T13324

Target: CXCR, Arrestin

Cat.No: T16850

Synonym: GSK-CXCR2

Target: CXCR

Cat.No: T7499

Synonym: Takeda 779

Target: HIV Protease, CXCR, CCR

Cat.No: T7130

Synonym: MK-7123,SCH 527123

Target: CXCR

AMD 3465 hexahydrobromide

Cat.No: T7208

Synonym: GENZ-644494 (hexahydrobromide)

Target: HIV Protease, CXCR

Reparixin L-lysine salt

Cat.No: T12705

Synonym: REPERTAXIN L-赖氨酸盐,Repertaxin L-lysine salt

Target: CXCR

CXCR7 modulator 1

Cat.No: T10906

Target: Others

Cat.No: T33763

Synonym: NVP-CXCR2 20,NVP CXCR2-20,NVP CXCR220

CXCR7 modulator 2

Cat.No: T10907

Target: Others

Cat.No: T78879

Target: CXCR

CXCR2 antagonist 7

Cat.No: T61236

CXCR4 antagonist 3

Cat.No: T61409

CXCR4 antagonist 4

Cat.No: T63369

CXCR4 antagonist 8

Cat.No: T61363

CXCR4 antagonist 6

Cat.No: T61420

Cat.No: T79059

Target: CXCR

CXCR2 antagonist 3

Cat.No: T61356

CXCR2 antagonist 8

Cat.No: T60696

CXCR4 probe 1

Cat.No: T64306

CXCR4 modulator-1

Cat.No: T62007

CXCR4 antagonist 5

Cat.No: T61419

CXCR2 antagonist 6

Cat.No: T61359

Cat.No: T80216

Target: CXCR

CXCR4 modulator-2

Cat.No: T62352

Cat.No: T6764

Synonym: ATI2341

Target: CXCR

CXCR7 antagonist-1 hydrochloride

Cat.No: T62325

Cat.No: T1776

Synonym: 普乐沙福,JM3100,AMD 3100,AMD-3329

Target: Virus Protease, HIV Protease, CXCR

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。

天然产物

Cat.No: T3396

Synonym: Icariside-II,宝藿苷I,Icariin-II,宝藿苷 I

Target: Apoptosis, CXCR

Cat.No: T3S1416

Synonym: Decursinol angelate,前胡素,(+)-Decursin,紫花前胡素

Target: Apoptosis, PKC

Nicotinamide N-oxide

Cat.No: T0617

Synonym: Nicotinamide-N-oxide,Nicotinamide 1-oxide,N-氧代烟酰胺,烟酰胺-N-氧化物,1-oxynicotinamide

Target: c-Myc, Endogenous Metabolite, CXCR, Drug Metabolite

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