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Search Results for " cxcr4 "

89

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T40786	CXCR4 antagonist 1 CXCR4 antagonist 1
	CXCR4 antagonist 1 is a potent inhibitor of the CXCR4 receptor, with notable anti-HIV activity.
T39742	CXCR4 antagonist 2
	CXCR4 antagonist 2 is a CXCR4 antagonist with an IC 50 value of 47 nM.
T83763	EPI-X4 TFA Endogenous Peptide Inhibitor of CXCR4
	EPI-X4是一种源于人血清白蛋白408-423氨基酸的内源性肽段，是趋化因子(C-X-C基序)受体4 (CXCR4)的拮抗剂。在0.8至1,000µM的浓度范围内，EPI-X4能抑制表达CXCR4的HEK293细胞中由趋化因子(C-X-C基序)配体12 (CXCL12)诱发的钙离子动员和受体内化。EPI-X4还能抑制CXCL12诱导的Jurkat T细胞和人类CD34+造血干细胞的迁移。体内实验中，EPI-X4（16µmol/kg）在急性过敏性气道高嗜酸性粒细胞疾病的小鼠模型中减少了Cxcr4依赖的炎症细胞气道浸润。慢性肾脏病患者尿液中EPI-X4的水平增高，并与肾小球滤过率(GFR)成反比。
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。
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].
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].
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].
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)。
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。
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].
T61650	CXCR4 antagonist 9
	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].
T60811	CXCR4 antagonist 7
	CXCR4 antagonist 7 (Compound PARA-B) 是可用于研究HIV 感染、炎症性疾病、癌症和 WHIM 综合症的CXCR4拮抗剂 (IC50 = 9.3 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)。
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。
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。
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。
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。
T15805L	LY2510924 acetate(1088715-84-7 free base)	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	LY2510924 acetate(1088715-84-7 free base) 是一种有效的选择性 CXCR4 拮抗剂。它可防止 SDF-1 与 CXCR4 结合，IC50 为 0.079 nM。
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。
TP1348	FC131 TFA (606968-52-9 free base) FC131 TFA	HIV Protease; CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	FC131 TFA (606968-52-9 free base) (FC131 TFA) 是 CXCR4 的拮抗剂，可抑制 [125I] -sdf-1 与 CXCR4 的结合（IC50：4.5 nM），并具有抗 HIV 活性。
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。
T11693L	IT1t dihydrochloride	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	IT1t dihydrochloride 抑制 CXCL12/CXCR4 相互作用，IC50 为 2.1 nM。 IT1t dihydrochloride 是 CXCR4 的拮抗剂。
T14665L	Motixafortide TFA(664334-36-5,Free) TF 14016 TFA,BKT140 TFA,BL-8040 TFA,T140 TFA	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	Motixafortide TFA(664334-36-5,Free) (BKT140 TFA) 是 CXCR4 的拮抗剂，IC50 为～1 nM。它通过改变 miR-15a/16-1 表达下调 ERK、BCL-2、MCL-1 和 cyclin-D1 来诱导 AML 原始细胞凋亡。
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。
T1776L	Plerixafor octahydrochloride 盐酸普乐沙福,JM3100 octahydrochloride,Plerixafor 8HCl (AMD3100 8HCl),Plerixafor 8HCl,SID791 octahydrochloride,AMD 3100 octahydrochloride,JM 3100 8HCl	Virus Protease; HIV Protease; CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	Plerixafor octahydrochloride (JM3100 octahydrochloride) 是一种选择性的CXCR4拮抗剂，IC50为 44 nM。Plerixafor 是一种具有造血干细胞动员活性的双环霉素。
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。
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。
TP2051L	CTCE 9908 acetate	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	CTCE 9908 acetate 是 CXCR4 的拮抗剂，可抑制表达 CXCR4 的卵巢癌细胞的迁移。
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。
TP2112L	TC14012 acetate TC14012 acetate(368874-34-4 free base)	CXCR; Arrestin	Autophagy; GPCR/G Protein; Immunology/Inflammation
	TC14012 acetate 是 T140 的血清稳定衍生物，是一种选择性的肽模拟 CXCR4 拮抗剂，IC50 为 19.3 nM。 TC14012 还是一种有效的 CXCR7 激动剂，EC50 为 350 nM，可将 β-arrestin 2 募集到 CXCR7。 TC14012 具有抗癌活性和抗 HIV 活性。
T5207	LIT927 LIT 927,LIT-927	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	LIT927 (LIT-927) 是一种具有口服活性的 CXCL12 中性配体（对于 CXCL12 与 CXCR4 的结合，Ki：267 nM）。
T22565	AMD-070 hydrochloride N-(1H-苯并咪唑-2-基甲基)-N-[(8S)-5,6,7,8-四氢-8-喹啉基]-1,4-丁二胺单盐酸盐	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	AMD-070 hydrochloride 是一种 CXCR4 拮抗剂，可用于抗 HIV。
T12269	NUCC-390	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	NUCC-390 是新型的选择性小分子 CXCR4 receptor 受体激动剂。NUCC-390 可以诱导 CXCR4 受体的内化，作用方式与 AMD3100相反。NUCC-390 在动物模型中，有助于神经退行性变后神经功能恢复。
T76794	Ulocuplumab BMS 936564,MDX 1338	Apoptosis; CXCR	Apoptosis; Autophagy; GPCR/G Protein; Immunology/Inflammation
	Ulocuplumab (BMS-936564) 是一种完全人抗 CXCR4 的 IgG4 抗体。Ulocplumab 在急性髓系白血病 (AML)，非霍奇金淋巴瘤 (NHL) 和多发性骨髓瘤移植模型中展现出抗肿瘤活性。Ulocplumab 对 CXCL12 介导的慢性淋巴细胞白血病 (CLL) 细胞在 CXCR4 激活下的迁移有抑制作用，诱导癌细胞凋亡 (apoptosis)，。
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。
T6764L	ATI-2341 acetate(1337878-62-2 free base)	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	ATI-2341 acetate(1337878-62-2 free base) 是一种有效的 CXCR4 变构激动剂，它激活 Gα1 而不是 Gα13。 ATI-2341 acetate 激活抑制性异源三聚体 G 蛋白 (GI) 以促进对 cAMP 产生的抑制并诱导钙动员。
TP1364L	ALX 40-4C acetate ALX 40-4C acetate(143413-49-4 free base)	Apelin receptor; CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	ALX 40-4C acetate 是趋化因子受体 (Ki = 1 μM) 的 CXCR4 抑制剂，可抑制 HIV-1 X4 株的复制。 ALX 40-4C acetate 是 APJ 受体的拮抗剂 (IC50 = 2.9 μM)。
T2375	BX471 BX 471,BX-471,ZK-811752	CCR	Immunology/Inflammation; Microbiology/Virology
	BX471 (BX 471) 是可口服的非多肽 CCR1选择性拮抗剂，Ki 值为 1 nM，对其选择性是对 CCR2、CCR5 和 CXCR4 的 250 倍。
T20482L	Acth (1-4) acetate(19405-50-6 free base)	Others	Others
	Acth (1-4) acetate(19405-50-6 free base) 是 ACTH N 端四肽。
T15805	LY2510924	Others	Others
	LY2510924 is an effective and selective CXCR4 antagonist. It blocks SDF-1 binding to CXCR4 (IC50: 0.079 nM).
T22777	FC131 FC 131	Others	Others
	CXCR4 antagonist
T14665	Motixafortide BL-8040,BKT140 (4-fluorobenzoyl),TF14016	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	Motixafortide (BKT140 4-fluorobenzoyl) is an antagonist of CXCR4 (IC50: 1 nM).
TP2141	Balixafortide TFA (1051366-32-5 free base) Balixafortide TFA,POL6326 TFA	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	Balixafortide TFA (POL6326 TFA) is a selective, well-tolerated peptidic CXCR4 antagonist (IC50 < 10 nM). It shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium fl
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。
T11693	IT1t	Others	Others
	IT1t inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM. is a potent CXCR4 antagonist.
TP2141L	Balixafortide POL6326	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM and it is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects[1][2]. Balixafortide blocks β-arresti
T39787	KRH-3955 hydrochloride
	KRH-3955 hydrochloride is a CXCR4 antagonist with oral bioavailability. It effectively inhibits the binding of SDF-1α to CXCR4, exhibiting an IC 50 of 0.61 nM. Additionally, KRH-3955 hydrochloride displays high potency and selectivity as an inhibitor of X4 HIV-1, with an EC 50 ranging from 0.3 to 1.0 nM.
T69583	AMD-3451 trihydrochloride
	AMD-3451 trihydrochloride is a CCR5/CXCR4 dual antagonist that may be useful in the treatment of HIV.
T25523	ICT5040 ICT-5040,ICT 5040
	ICT5040 is a CXCR4 antagonist.

化合物

CXCR4 antagonist 1

Cat.No: T40786

Synonym: CXCR4 antagonist 1

CXCR4 antagonist 2

Cat.No: T39742

Cat.No: T83763

Synonym: Endogenous Peptide Inhibitor of CXCR4

CXCR4 probe 1

Cat.No: T64306

CXCR4 antagonist 6

Cat.No: T61420

CXCR4 antagonist 3

Cat.No: T61409

CXCR4 antagonist 8

Cat.No: T61363

CXCR4 antagonist 4

Cat.No: T63369

CXCR4 modulator-2

Cat.No: T62352

CXCR4 modulator-1

Cat.No: T62007

CXCR4 antagonist 5

Cat.No: T61419

CXCR4 antagonist 9

Cat.No: T61650

CXCR4 antagonist 7

Cat.No: T60811

Cat.No: T78879

Target: CXCR

Cat.No: T80216

Target: CXCR

Cat.No: T79059

Target: CXCR

Cat.No: T4032

Synonym: MSX 127

Target: CXCR

Cat.No: T4033

Synonym: MSX 130

Target: CXCR

LY2510924 acetate(1088715-84-7 free base)

Cat.No: T15805L

Target: CXCR

Cat.No: T3992

Synonym: MSX 122,MSX122

Target: CXCR

FC131 TFA (606968-52-9 free base)

Cat.No: TP1348

Synonym: FC131 TFA

Target: HIV Protease, CXCR

Cat.No: T1739

Target: CXCR

IT1t dihydrochloride

Cat.No: T11693L

Target: CXCR

Motixafortide TFA(664334-36-5,Free)

Cat.No: T14665L

Synonym: TF 14016 TFA,BKT140 TFA,BL-8040 TFA,T140 TFA

Target: CXCR

Cat.No: T17208

Target: CXCR

Plerixafor octahydrochloride

Cat.No: T1776L

Synonym: 盐酸普乐沙福,JM3100 octahydrochloride,Plerixafor 8HCl (AMD3100 8HCl),Plerixafor 8HCl,SID791 octahydrochloride,AMD 3100 octahydrochloride,JM 3100 8HCl

Target: Virus Protease, HIV Protease, CXCR

Cat.No: T1776

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

Target: Virus Protease, HIV Protease, CXCR

Cat.No: TQ0174

Synonym: AMD-070

Target: CXCR

CTCE 9908 acetate

Cat.No: TP2051L

Target: CXCR

AMD 3465 hexahydrobromide

Cat.No: T7208

Synonym: GENZ-644494 (hexahydrobromide)

Target: HIV Protease, CXCR

TC14012 acetate

Cat.No: TP2112L

Synonym: TC14012 acetate(368874-34-4 free base)

Target: CXCR, Arrestin

Cat.No: T5207

Synonym: LIT 927,LIT-927

Target: CXCR

AMD-070 hydrochloride

Cat.No: T22565

Synonym: N-(1H-苯并咪唑-2-基甲基)-N-[(8S)-5,6,7,8-四氢-8-喹啉基]-1,4-丁二胺单盐酸盐

Target: CXCR

Cat.No: T12269

Target: CXCR

Cat.No: T76794

Synonym: BMS 936564,MDX 1338

Target: Apoptosis, CXCR

Cat.No: T9721

Target: CXCR

ATI-2341 acetate(1337878-62-2 free base)

Cat.No: T6764L

Target: CXCR

ALX 40-4C acetate

Cat.No: TP1364L

Synonym: ALX 40-4C acetate(143413-49-4 free base)

Target: Apelin receptor, CXCR

Cat.No: T2375

Synonym: BX 471,BX-471,ZK-811752

Target: CCR

Acth (1-4) acetate(19405-50-6 free base)

Cat.No: T20482L

Target: Others

Cat.No: T15805

Target: Others

Cat.No: T22777

Synonym: FC 131

Target: Others

Cat.No: T14665

Synonym: BL-8040,BKT140 (4-fluorobenzoyl),TF14016

Target: CXCR

Balixafortide TFA (1051366-32-5 free base)

Cat.No: TP2141

Synonym: Balixafortide TFA,POL6326 TFA

Target: CXCR

Cat.No: T6764

Synonym: ATI2341

Target: CXCR

Cat.No: T11693

Target: Others

Cat.No: TP2141L

Synonym: POL6326

Target: CXCR

KRH-3955 hydrochloride

Cat.No: T39787

AMD-3451 trihydrochloride

Cat.No: T69583

Cat.No: T25523

Synonym: ICT-5040,ICT 5040

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。
T6S1315	Oroxylin A 千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether	Virus Protease; HIF/HIF Prolyl-Hydroxylase; Autophagy	Autophagy; Chromatin/Epigenetic; Metabolism; Microbiology/Virology
	Oroxylin A (Baicalein 6-methyl ether) 是一种有活性的黄酮，具有较强的抗癌作用。

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: T6S1315

Synonym: 千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether

Target: Virus Protease, HIF/HIF Prolyl-Hydroxylase, Autophagy

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