CXCR4 选择性抑制剂 | 激动剂 | 拮抗剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S3951 Tannic acid

Tannic acid (Gallotannic acid), a polyphenolic compound, is a CXCL12/CXCR4 inhibitor with antiangiogenic, anti-inflammatory and antitumor activity.

Selective
S8505 LY2510924

LY2510924 is a potent and selective CXCR4 antagonist that specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nmol/L and inhibits SDF-1-induced GTP binding with Kb value of 0.38 nmol/L.

Selective CXCR4, IC50: 0.079 nM
S2912 WZ811

WZ811是一种高效的,竞争性的CXCR4拮抗剂,EC50为0.3 nM。

Selective CXCR4, EC50: 0.3 nM
S9665 Motixafortide (BL-8040)

Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ~1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.

Selective CXCR4, IC50: 1 nM
S6617 MSX-122

MSX-122 is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM).

Selective CXCR4, IC50: ~10 nM
S8030 Plerixafor (AMD3100)

Plerixafor (AMD3100)是一种趋化因子受体拮抗剂,作用于CXCR4和CXCL12介导的趋化性,无细胞试验中IC50分别为44 nM和5.7 nM。

Selective CXCR4, IC50: 44 nM
S3013 Plerixafor (AMD3100) 8HCl

Plerixafor 8HCl (AMD3100 8HCl)是Plerixafor的盐酸盐,是CXCR4趋化因子受体拮抗剂,作用于CXCR4和CXCL12介导调节的趋化性, IC50分别为44 nM和5.7 nM。

Selective CXCR4, IC50: 44 nM
S8309 ATI-2341

ATI-2341,一种靶向C-X-C 4型趋化因子受体(CXCR4)的肽段,是一个变构受体激动剂,能够激活异源三聚体G蛋白(Gi)、抑制cAMP生成以及诱导钙动员。

Selective CXCR4, EC50: 194 nM
S8813 LIT-927

LIT-927 is a novel neutraligand of CXCL12 with Ki value of 267 nM for inhibition of Texas red-labeled CXCL12 (CXCL12-TR) binding. It shows high selectivity toward CXCL12 vs other chemokines also involved in asthma.

Selective
S2879 AMD3465 hexahydrobromide

AMD3465是一种单一大环类CXCR4的拮抗剂。

Selective
S9725 Balixafortide (POL6326)

Balixafortide (POL6326) is an orally bioavailable peptidic CXC chemokine receptor 4 (CXCR4) antagonist.

Selective
S0292 MSX-127

MSX-127 (NSC-23026) is a CXCR4 receptor modulator.

Selective
S0293 MSX-130

MSX-130 is an antagonist of CXCR4.

Selective