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抑制剂 & 化合物

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天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
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。
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。
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。
T10296	Mavorixafor trihydrochloride AMD-070 trihydrochloride	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	Mavorixafor trihydrochloride is a selective and orally available CXCR4 antagonist (IC50: 13 nM against CXCR4 125I-SDF binding) and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs (IC50s: 1 and 9 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。
T14208	AMD 3465 GENZ-644494	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM). However, it has no effect on CCR5-using (R5) viruses. AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC
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。
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].
T75802	CTCE-9908 TFA
	CTCE-9908 TFA 是一种有效的，选择性的 CXCR4抑制剂。CTCE-9908 TFA 在表达 CXCR4的卵巢癌细胞中诱导有丝分裂突变，诱导细胞毒性，抑制迁移。
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].
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)。
T63004	NUCC-390 dihydrochloride
	NUCC-390 dihydrochloride 是新型的选择性小分子CXCR4receptor 受体激动剂。NUCC-390 dihydrochloride 可以诱导CXCR4受体的内化，作用方式与 AMD3100 相反。NUCC-390 dihydrochloride 在动物模型中，有助于神经退行性变后神经功能恢复。
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。
T69582	AMD-3451 free base
	AMD-3451 free base is a dual CCR5/CXCR4 antagonist which may be useful in the treatment of a wide variety of R5, R5/X4, and X4 strains of human immunodeficiency virus type 1 (HIV-1) and HIV-2. AMD3451 is the first low-molecular-weight anti-HIV agent with selective HIV coreceptor, CCR5 and CXCR4, interaction.
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].
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)。
T69081	KRH-1636
	KRH-1636 is an orally active, selective and extremely potent CXC chemokine receptor 4 antagonist. KRH-1636 exhibits a potent and selective anti-HIV-1 activity. KRH-1636 efficiently blocked replication of various T cell line-tropic (X4) HIV type 1 (HIV-1) in MT-4 cells and peripheral blood mononuclear cells through the inhibition of viral entry and membrane fusion via the CXC chemokine receptor (CXCR)4 coreceptor but not via CC chemokine receptor 5. KRH-1636 also inhibits binding of the CXC chem...
T68457	GSK812397
	GSK812397 is a potent entry inhibitor of X4-tropic strains of HIV-1, as demonstrated in multiple in vitro cellular assays. GSK812397 is a noncompetitive antagonist of the CXCR4 receptor, with GSK812397 producing a concentration-dependent decrease in both an SDF-1-mediated chemotaxis and intracellular calcium release (IC50s were 0.34+/-0.01 nM and 2.41+/-0.50 nM, respectively). GSK812397 is effective against a broad range of X4- and X4R5-utilizing clinical isolates. The potency and efficacy of GS...
T80130	SDF-1α (human)	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	SDF-1α (human) 是一种能够与CXCR4受体相结合的单核细胞趋化剂，它在心肌梗死模型中的干细胞归巢、维持、生存、增殖、心肌细胞修复、血管形成以及心室重构过程扮演关键角色。SDF-1α (human) 常用于心血管病研究。
T76543	NoxaBH3
	NoxaBH3，一种基于半胱氨酸的交联肽，具备提高的细胞渗透性及较高对Mcl-1的抑制效能。该化合物通过与CXCR4的内源性配体结合，形成泛素-NoxaBH3偶联物，进而被导向癌细胞。
T76327	CTCE-0214
	CTCE-0214 是一种 CXCR4(chemokine CXC receptor 4) 激动剂，是 SDF-1α 肽类似物。CTCE-0214 具有抗炎活性，可用于炎症败血症和系统性炎症综合征的研究。
T70259	AMD-3329 free base
	AMD-3329 free base is a biochemical in the class of potent and selective anti-HIV-1 and HIV-2 agents that inhibit virus replication by binding to the chemokine receptor CXCR4, the co-receptor for entry of X4 viruses.
T76548	Peptide R
	Peptide R 是一种环状肽，是一种特异性 CXCR4拮抗剂。Peptide R 显示出有效的重塑肿瘤间质的出色能力。Peptide R 具有用于肿瘤研究的潜力。
T70260	AMD-3329 hydrobromide
	AMD-3329 hydrobromide is a biochemical in the class of potent and selective anti-HIV-1 and HIV-2 agents that inhibit virus replication by binding to the chemokine receptor CXCR4, the co-receptor for entry of X4 viruses.
TP1354	ATI-2341 TFA (1337878-62-2 free base) ATI-2341 TFA
	ATI-2341 is an effective functionally selective allosteric agonist for the c-x-c chemokine receptor type 4 (CXCR4), which ACTS as a biased ligand in favor of G G G G G 1 activation instead of G G G G G 13.ATI-2341 activates the inhibitory heterotrimer G p
T37604	ITK inhibitor
	Interleukin-2-inducible T cell kinase (ITK) is a non-receptor tyrosine kinase expressed in T cells, NKT cells and mast cells which plays a crucial role in regulating the T cell receptor (TCR), CD28, CD2, chemokine receptor CXCR4, and FcepsilonR-mediated signaling pathways. ITK inhibitors can be used for the treatment of inflammation and immune-mediated disorders. ITK inhibitor (N-[5-[[3-[(4-Acetylpiperazin-1-yl)carbonyl]-4-methyl-6-methoxy-phenyl]thio]thiazol-2-yl]-4-(N-1,2-dimethylpropylaminome...
T11693	IT1t	Others	Others
	IT1t inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM. is a potent CXCR4 antagonist.

化合物

Cat.No: T79059

Target: CXCR

Cat.No: TQ0174

Synonym: AMD-070

Target: CXCR

IT1t dihydrochloride

Cat.No: T11693L

Target: CXCR

Mavorixafor trihydrochloride

Cat.No: T10296

Synonym: AMD-070 trihydrochloride

Target: HIV Protease

AMD 3465 hexahydrobromide

Cat.No: T7208

Synonym: GENZ-644494 (hexahydrobromide)

Target: HIV Protease, CXCR

Cat.No: T14208

Synonym: GENZ-644494

Target: HIV Protease

CXCR4 modulator-1

Cat.No: T62007

CXCR4 antagonist 8

Cat.No: T61363

Cat.No: T75802

CXCR4 antagonist 6

Cat.No: T61420

Cat.No: T78879

Target: CXCR

NUCC-390 dihydrochloride

Cat.No: T63004

Cat.No: T80216

Target: CXCR

AMD-3451 free base

Cat.No: T69582

CXCR4 antagonist 5

Cat.No: T61419

CXCR4 antagonist 7

Cat.No: T60811

Cat.No: T69081

Cat.No: T68457

SDF-1α (human)

Cat.No: T80130

Target: CXCR

Cat.No: T76543

Cat.No: T76327

AMD-3329 free base

Cat.No: T70259

Cat.No: T76548

AMD-3329 hydrobromide

Cat.No: T70260

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

Cat.No: TP1354

Synonym: ATI-2341 TFA

Cat.No: T37604

Cat.No: T11693

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
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: 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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