Signaling Pathway

CXCR

CXCR

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CXCRs (CXC chemokine receptors) are integral membrane proteins that specifically bind and respond to cytokines of the CXC chemokine family. They represent one subfamily of chemokine receptors, a large family of G protein-linked receptors that are known as seven transmembrane (7-TM) proteins, since they span thecell membrane seven times. There are currently seven known CXC chemokine receptors in mammals, named CXCR1 through CXCR7. CXCR1 and CXCR2 are closely related receptors that recognize CXC chemokines that possess an E-L-R amino acid motif immediately adjacent to their CXC motif. CXCR3 is expressed predominantly on T lymphocytes. CXCR4 is the receptor for a chemokine known as CXCL12 (or SDF-1) and, as with CCR5, is utilized by HIV-1 to gain entry into target cells. The chemokine receptor CXCR5 is selectively expressed on B cells and is involved in lymphocyte homing and the development of normal lymphoid tissue. CXCR6 was formerly called three different names (STRL33, BONZO, and TYMSTR) before being assigned CXCR6 based on its chromosomal location and its similarity to other chemokine receptors in its gene sequence. CXCR7 was originally called RDC-1 (an orphan receptor) but has since been shown to cause chemotaxis in T lymphocytes in response to CXCL12 (the ligand for CXCR4) prompting the renaming of this molecule as CXCR7.

CXCR Inhibitors & Modulators (23)

Product Name Catalog No. Brief Description
AMD 3465

HY-15971A

AMD 3465(GENZ-644494) is a potent, selective CXCR4 antagonist; exhibits 8-fold higher affinity than AMD 3100; inhibits SDF-1α-ligand binding (Ki = 41.7 nM).

AMD 3465 hexahydrobromide

HY-15971

AMD 3465 6HBr(GENZ-644494) is a potent, selective CXCR4 antagonist; exhibits 8-fold higher affinity than AMD 3100; inhibits SDF-1α-ligand binding (Ki = 41.7 nM).

AMD-070

HY-50101

AMD-070 is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay; inhibit the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs.

AMD-070 hydrochloride

HY-50101A

AMD-070 Hcl is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay; inhibit the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs.

AMG 487

HY-15319

AMG 487 is a small molecule antagonist of the chemokine receptor CXCR3; inhibits binding of 125I-IP-10 and 125I-ITAC to CXCR3 (IC50 values are 8.0 and 8.2 nM respectively).

AMG 487 S-enantiomer

HY-15319B

AMG 487 S-enantiomer is the enantiomer of AMG 487.

Baohuoside I

HY-N0011

Baohuoside I (Icariside-II) is a component of Epimedium koreanum; a regulator of CXCR4 expression as well as function in cervical cancer and breast cancer cells; Apoptosis inducer.

BKT140

HY-P0171

BKT140 is a novel CXCR4 antagonist with an IC50 value of ~1 nM.

Danirixin

HY-19768

Danirixin is a small molecule, non-peptide, high affinity (IC50 for CXCL8 binding = 12.5 nM), selective, and reversible CXCR2 antagonist.

MSX-122

HY-13696

MSX-122 is a novel small molecule and partial CXCR4 antagonist, with potent inhibition of CXCR4/CXCL12 actions (IC50 = 10 nM).

NBI-74330

HY-15320

NBI-74330 is a small molecule antagonist for CXCR3, NBI-74330 demonstrates potent inhibition of [(125)I]CXCL10 and [(125)I]CXCL11 specific binding (K(i) of 1.5 and 3.2 nM, respectively.

Plerixafor

HY-10046

Plerixafor is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.

Plerixafor octahydrochloride

HY-50912

Plerixafor octahydrochloride(AMD3100 8HCL) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.

Reparixin

HY-15251

Reparixin(DF 1681Y) is an inhibitor of CXCL8 receptor, also inhibit CXCR1 and CXCR2 activation, which has been shown to attenuate inflammatory responses in various injury models.

Reparixin L-lysine salt

HY-15252

Reparixin L-lysine salt is an inhibitor of CXCL8 receptor, also inhibit CXCR1 and CXCR2 activation,which has been shown to attenuate inflammatory responses in various injury models.

SB225002

HY-16711

SB225002 is a potent and selective non-peptide inhibitor of CXCR2 with IC50 of 22 nM; >150-fold selectivity over CXCR1 and four other 7-TMRs.

SCH 527123

HY-10198

SCH-527123 is a potent antagonist of both CXCR1 and CXCR2 with IC50 of 42 nM and 3 nM, respectively.

SCH 546738

HY-10017

SCH 546738 is a novel, potent and non-competitive small molecule CXCR3 antagonist with Ki of 0.4 nM .

SCH 563705

HY-10011

SCH 563705 is a potent dual CXCR2(IC50= 1.3 nM)/CXCR1(IC50= 7.3 nM) antagonist.

SRT3109

HY-15462

SRT3109 is a CXCR2 ligand for use in the treatment of chemokine mediated diseases and conditions.