CXCR4 antagonist 1

CXCR4 antagonist 1 is a potent inhibitor of the CXCR4 receptor with notable anti-HIV activity.

CXCR4 antagonist10 (compound 21) is an effective CXCR4 inhibitor with an IC50 value of 7.8 nM. It plays a significant role in cancer research.

Plerixafor (AMD-3329), a chemokine receptor antagonist, blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4.

BX471 (BX 471) is a potent, selective non-peptide CCR1 antagonist.

Motixafortide TFA(664334-36-5,Free) (BKT140 TFA) is an antagonist of CXCR4 with IC50 of ～1 nM. It induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a 16-1 expression.

WZ811 is a novel and effective small molecular CXCR4 antagonist (EC50: 0.3 nM).

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).

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

Motixafortide (BKT140 4-fluorobenzoyl) is a CXCR4 antagonist with an IC50 of 1 nM.

Motixafortide (BKT140 4-fluorobenzoyl) is an antagonist of CXCR4 (IC50: 1 nM). BMS-1166 hydrochloride is an inhibitor of PD-1 PD-L1 interaction (IC50: 1.4 nM). BMS-1166 rivalries the inhibitory effect of PD-1 PD-L1 immune checkpoint on T cell activation.

BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with a Ki of 1 nM for human CCR1, exhibiting 250-fold selectivity over CCR2, CCR5, and CXCR4.

LY2510924 is an effective and selective CXCR4 antagonist. It blocks SDF-1 binding to CXCR4 (IC50: 0.079 nM).

Ly2510924 acetate is an potent and selective CXCR4 antagonist. It prevents the binding of SDF-1 to CXCR4 with an IC50 of 0.079 nM.

USL311 is a CXCR4 receptor antagonist which prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4. USL311 inhibits CXCR4 activation and decreases proliferation and migration of CXCR4-expressing tumor cells, with anti-tumor activ

KRH-3955, a CXCR4 antagonist, is an orally bioavailable and extremely potent inhibitor of HIV-1 infection.

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.

CXCR4 antagonist 7 (Compound PARA-B) is a potent CXCR4 inhibitor (IC50 = 9.3 nM) [1] applicable in research on HIV infection, inflammatory diseases, cancer, and WHIM syndrome.

CXCR4 antagonist 8 (Compound 3) is a potent inhibitor of CXCR4, exhibiting an IC50 value of 57 nM in antagonism and effectively inhibiting CXCL12-induced cytosolic calcium increase with an IC50 of 0.24 nM. Additionally, Compound 3 is efficacious in inhibiting CXCL12 CXCR4-mediated cell migration [1].

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].

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].

CXCR4 antagonist 6 (compound 46) is a highly potent inhibitor of CXCR4 with an IC50 value of 79 nM, effectively inhibiting the cytosolic calcium flux induced by CXCL12 with an IC50 of 0.25 nM. Additionally, it significantly mitigates cell migration mediated by the CXCL12 CXCR4 interaction and demonstrates remarkable efficacy in a mouse model of cancer metastasis [1].

CXCR4 antagonist 9 (Compound 2) is a potent CXCR4 antagonist with an IC50 of 15 nM and effectively inhibits the cytosolic calcium increase induced by CXCL12, exhibiting an IC50 of 1.3 nM [1].

HF50731 is a potent antagonist of CXCR4. HF50731 has a strong binding affinity for CXCR4 (IC50: 19.8 nM). HF50731 utilizes the CXCR4 co-receptor and effectively inhibits calcium mobilization (IC50: 119.2 nM), cell migration (IC50: 621.4 nM) and HIV-1 infection (IC50: 1.5 nM). IC50: 1.5 nM).

HF51116 is a potent antagonist of CXCR4 that significantly inhibits SDF-1α-induced cell migration, calcium mobilization, and CXCR4 internalization. It also prevents HIV-1 infection utilizing CXCR4. HF51116 has shown investigational potential for HIV-1 infection, hematopoietic stem cell mobilization, and cancer metastasis.