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.

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.

S2879 AMD3465 hexahydrobromide


S9725 Balixafortide (POL6326)

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

S0292 MSX-127

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

S0293 MSX-130

MSX-130 is an antagonist of CXCR4.