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19

抑制剂 & 化合物

4

重组蛋白

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Cat. No.	Product Name	Target	Signaling Pathways
T39440	CXCL12 ligand 1
	CXCL12 ligand 1 is the first ligand of the sY12-binding pocket on chemokine CXCL12 .
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）。
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。
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。
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)，。
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。
T11693	IT1t	Others	Others
	IT1t inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM. is a potent CXCR4 antagonist.
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。
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].
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].
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。
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].
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].
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。
T83769	TC 14012 hydrochloride H-Arg-Arg-Nal-Cys-Tyr-Cit-Lys-D-Cit-Pro-Tyr-Arg-Cit-Cys-Arg-NH2
	TC 14012是一种化学肽模拟的拮抗剂，针对趋化因子(C-X-C motif)受体4（CXCR4；IC50 = 2.9 nM）和CXCR7激动剂。它能在表达CXCR7的HEK293T细胞中诱导β-arrestin招募（EC50 = 350 nM）。TC 14012可减少HIV在MT-4细胞中的细胞病理效应（EC50 = 0.4 nM），并以CXCR4依赖的方式抑制HIV在体外进入（IC50 = 19.3 nM）。它还能抑制由趋化因子(C-X-C motif)配体12（CXCL12）在MDA-MB-231乳腺癌细胞和人脐静脉内皮细胞（HUVECs）中诱导的迁移，当使用浓度范围从10到1,000 nM时。在通过左前降（LAD）冠状动脉结扎诱导的急性心肌梗死小鼠模型中，TC 14012（10 mg/kg）能减少梗死面积。
T83926	S-Geranylgeranyl-L-glutathione GGG
	S-Geranylgeranyl-L-glutathione是孤儿G蛋白偶联受体（GPCR）P2RY8的配体。该化合物在100 nM浓度下，选择性地诱导P2RY8而非鞘氨醇-1-磷酸受体2（S1P2）、GPR55、半胱氨酸白三烯受体1（CysLT1 receptor）以及CysLT2 receptor的内吞作用。在10 nM浓度下，S-Geranylgeranyl-L-glutathione抑制了表达P2RY8的WEHI-231 B细胞淋巴瘤细胞和分离的人扁桃体生发中心B细胞由趋化因子（C-X-C motif）配体12（CXCL12）诱导的迁移。
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。
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

化合物

CXCL12 ligand 1

Cat.No: T39440

Cat.No: T5207

Synonym: LIT 927,LIT-927

Target: CXCR

IT1t dihydrochloride

Cat.No: T11693L

Target: CXCR

Cat.No: T3992

Synonym: MSX 122,MSX122

Target: CXCR

Cat.No: T76794

Synonym: BMS 936564,MDX 1338

Target: Apoptosis, 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: T11693

Target: Others

Cat.No: T1776

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

Target: Virus Protease, HIV Protease, CXCR

CXCR4 antagonist 8

Cat.No: T61363

CXCR4 antagonist 5

Cat.No: T61419

CXCR7 antagonist-1 hydrochloride

Cat.No: T62325

CXCR4 antagonist 9

Cat.No: T61650

CXCR4 antagonist 6

Cat.No: T61420

Cat.No: T83763

Synonym: Endogenous Peptide Inhibitor of CXCR4

TC 14012 hydrochloride

Cat.No: T83769

Synonym: H-Arg-Arg-Nal-Cys-Tyr-Cit-Lys-D-Cit-Pro-Tyr-Arg-Cit-Cys-Arg-NH2

S-Geranylgeranyl-L-glutathione

Cat.No: T83926

Synonym: GGG

AMD 3465 hexahydrobromide

Cat.No: T7208

Synonym: GENZ-644494 (hexahydrobromide)

Target: HIV Protease, CXCR

Cat.No: T14208

Synonym: GENZ-644494

Target: HIV Protease

Species：

Expression System：

Tag：

Cat. No.	Product Name	Species	Expression System
TMPJ-00952	CXCL12 Protein, Mouse, Recombinant Sdf1,C-X-C motif chemokine 12,Thymic lymphoma cell-...	Mouse	E. coli
	Mouse Cxcl12 is a secreted and highly conserved protein which belongs to the intercrine alpha (chemokine CxC) family.CXCL12 is widely expressed in various organs including brain, kidney, skeletal muscle, heart, liver, and lymphoid organs. Cxcl12 activates the C-X-C chemokine receptor CXCR4 to induce a rapid and transient rise in the level of intracellular calcium ions and chemotaxis. It also binds to atypical chemokine receptor ACKR3 which activates the beta-arrestin pathway and acts as a scaven...
TMPJ-01037	CXCR4 Protein, Human, Recombinant (hFc) CXCR4,CD184,Fusin,D2S201E,FB22,HM89,HSY3RR,LAP3,LCR1,LESTR,N...	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...
TMPK-00271	TPBG/5T4 Protein, Human, Recombinant (His & Avi) M6P1,WAIF1,5T4,TPBG,5T4AG	Human	HEK293 Cells
	The oncofetal tumor-associated antigen 5T4 (TBGP) has been linked with CSC properties in several different malignancies. 5T4 has functional attributes that are relevant to the spread of tumors including through EMT, CXCR4/CXCL12, Wnt, and Hippo pathways which may all contribute through the mobilization of CSCs. TPBG/5T4 Protein, Human, Recombinant (His & Avi) is expressed in HEK293 mammalian cells with C-His-Avi tag. The predicted molecular weight is 38.2 kDa and the accession number is Q13641-1...
TMPK-00270	TPBG/5T4 Protein, Human, Recombinant (His & Avi), FITC-Labeled WAIF1,TPBG,5T4AG,5T4,M6P1	Human	HEK293 Cells
	The oncofetal tumor-associated antigen 5T4 (TBGP) has been linked with CSC properties in several different malignancies. 5T4 has functional attributes that are relevant to the spread of tumors including through EMT, CXCR4/CXCL12, Wnt, and Hippo pathways which may all contribute through the mobilization of CSCs. TPBG/5T4 Protein, Human, Recombinant (His & Avi), FITC-Labeled is expressed in HEK293 mammalian cells with C-His-Avi tag. The predicted molecular weight is 38.2 kDa and the accession numb...

重组蛋白

CXCL12 Protein, Mouse, Recombinant

Cat.No: TMPJ-00952

Species: Mouse

Expression System: E. coli

CXCR4 Protein, Human, Recombinant (hFc)

Cat.No: TMPJ-01037

Species: Human

Expression System: HEK293 Cells

TPBG/5T4 Protein, Human, Recombinant (His & Avi)

Cat.No: TMPK-00271

Species: Human

Expression System: HEK293 Cells

TPBG/5T4 Protein, Human, Recombinant (His & Avi), FITC-Labeled

Cat.No: TMPK-00270

Species: Human

Expression System: HEK293 Cells

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