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.


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CXCR4 modulator-2

CXCR4 modulator-2 (compound Z7R) is a highly potent CXCR4 modulator with an IC50 value of 1.25 nM. CXCR4 modulator-2 has acceptable stability (t1/2 = 77.1 min) in mouse serum and exhibits anti-inflammatory activity in mouse edema model[1].

  • CAS Number: 2488943-55-9
  • MF: C21H32N8O2
  • MW: 428.53
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Polyphemusin II-Derived Peptide

Polyphemusin II-Derived Peptide (T140), a CXCR4 inhibitor, shows high inhibitory activity against HIV-1 entry and the inhibitory effect on the binding of an anti-CXCR4 monoclonal antibody (12G5) to CXCR4[1].

  • CAS Number: 229030-20-0
  • MF: C90H141N33O18S2
  • MW:
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

VUF11207 fumarate

VUF11207 fumarate (Compound 29) is a CXCR7 agonist and a high-potency CXCR7 (pKi of 8.1) ligand that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7[1].

  • CAS Number: 1785665-61-3
  • MF: C31H39FN2O8
  • MW: 586.65
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

FC131

FC131 TFA 是一种 CXCR4 拮抗剂,抑制 [125I]-SDF-1 与 CXCR4 结合,IC50 值为 4.5 nM。FC131 TFA 具有抗 HIV 的活性。

  • CAS Number: 606968-52-9
  • MF: C36H47N11O6
  • MW: 729.828
  • Catalog: HIV
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ulocuplumab

Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) is a fully human IgG4 anti-CXCR4 antibody. Ulocuplumab induces apoptosis and inhibits CXCL12 mediated CXCR4 activation-migration of chronic lymphocytic leukemia (CLL). Ulocuplumab exhibits antitumor activity in established tumors including acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma xenograft models[1][2].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Reparixin

Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.

  • CAS Number: 266359-83-5
  • MF: C14H21NO3S
  • MW: 283.38600
  • Catalog: CXCR
  • Density: 1.137g/cm3
  • Boiling Point: N/A
  • Melting Point: 103-105 ºC
  • Flash Point: N/A

CXCR4 antagonist 6

CXCR4 antagonist 6 (compound 46) is a potent CXCR4 antagonist with an IC50 value of 79 nM. CXCR4 antagonist 6 inhibits CXCL12 induced cytosolic calcium flux (IC50 = 0.25 nM). CXCR4 antagonist 6 significantly mitigates CXCL12/CXCR4 mediated cell migration. CXCR4 antagonist 6 exhibits marked efficacy in a cancer metastasis model in mice[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Corydalmine hydrochloride

Corydalmine hydrochloride inhibits spore germination of some plant pathogenic as well as saprophytic fungi[1]. Corydalmine hydrochloride acts as an oral analgesic agent, exhibiting potent analgesic activity[2]. Corydalmine hydrochloride alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway[3].

  • CAS Number: 2428393-60-4
  • MF: C20H24ClNO4
  • MW: 377.86
  • Catalog: Fungal
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AMD-070

AMD-070 is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 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 with an IC50 of 1 and 9 nM, respectively.

  • CAS Number: 558447-26-0
  • MF: C21H27N5
  • MW: 349.473
  • Catalog: HIV
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 597.0±50.0 °C at 760 mmHg
  • Melting Point: 108-110ºC
  • Flash Point: 314.9±30.1 °C

Minecoside

Minecoside is a CXCR4/STAT3 inhibitor with anticancer and anti-inflammatory activity. Minecoside decreases CXCR4 expression and suppresses STAT3 activation, thus to inhibit CXCL 12-induced invasion. Minecoside potently inhibits cancer metastasis and promotes apoptotic progression[1][2].

  • CAS Number: 51005-44-8
  • MF: C25H30O13
  • MW: 538.50
  • Catalog: CXCR
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 815.9±65.0 °C at 760 mmHg
  • Melting Point: 142℃
  • Flash Point: 275.7±27.8 °C

ATI-2341 TFA

ATI-2341 is a CXCR4 agonist, induces CXCR4-dependent calcium flux, with an EC50 of 194 nM in CCRF-CEM cells. ATI-2341 is also a potent and efficacious mobilizer of bone marrow hematopoietic cells[1].

  • CAS Number: 1337878-62-2
  • MF: C104H178N26O25S2
  • MW: 2256.82
  • Catalog: CXCR
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CXCR4 antagonist 9

CXCR4 antagonist 9 (Compound 2) is a CXCR4 antagonist with an IC50 of 15 nM. CXCR4 antagonist 9 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 1.3 nM[1].

  • CAS Number: 2304750-83-0
  • MF: C21H27FN6
  • MW: 382.48
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MSX-130

MSX-130 is a CXCR4 antagonist. MSX-130 inhibits cancer metastasis[1].

  • CAS Number: 4051-59-6
  • MF: C36H26N4
  • MW: 514.618
  • Catalog: CXCR
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 766.3±48.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 326.5±22.5 °C

Eldelumab

Eldelumab (BMS-936557) is a humanised anti-CXCL10 (IP-10) monoclonal antibody (IgG1 type). Eldelumab selectively binds to CXCL10 and blocks CXCL10-induced calcium flux and cell migration. Eldelumab can be used in studies of autoimmune and auto-inflammatory diseases such as rheumatoid arthritis, ulcerative colitis and crohn's disease[1][2].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SCH 563705

SCH 563705 is a potent and orally available CXCR2 and CXCR1 antagonist, with IC50s of 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively.

  • CAS Number: 473728-58-4
  • MF: C23H27N3O5
  • MW: 425.47800
  • Catalog: CXCR
  • Density: 1.29g/cm3
  • Boiling Point: 555.9ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 290ºC

USL311

USL311 is a selective CXCR4 antagonist, with anti-tumor activity[1].

  • CAS Number: 1373268-67-7
  • MF: C24H34N6O
  • MW: 422.57
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CXCR7 antagonist-1

CXCR7 antagonist-1 is an inhibitor of the binding of the SDF-1 chemokine (CXCL12 chemokine) or I-TAC (CXCL11) to the chemokine receptor CXCR. CXCR7 antagonist-1 prevents tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases (extracted from patent WO2014085490A1, compound 1.128)[1].

  • CAS Number: 1613021-99-0
  • MF: C21H19FN6O
  • MW: 390.41
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CXCR4 antagonist 7

CXCR4 antagonist 7 (Compound PARA-B) is a CXCR4 antagonist with the IC50 of 9.3 nM. CXCR4 antagonist 7 can be used for the research of HIV infection, inflammatory diseases, cancer, and WHIM syndrome[1].

  • CAS Number: 1185451-72-2
  • MF: C15H17N5O3
  • MW: 315.33
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ML 339

ML339 is a potent and selective CXCR6 (IC50 of 140 nM) antagonist that is selective (IC50 >79 μM) against CXCR5, CXCR4, CCR6 and Apelin receptor (APJ). ML339 holds potential to advance the field of prostate cancer research[1].

  • CAS Number: 2080300-49-6
  • MF: C26H32ClN3O5
  • MW: 502.00
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

JMS-17-2

JMS-17-2 is a potent and selective CX3CR1 antagonist with an IC50 of 0.32 nM[1].

  • CAS Number: 1380392-05-1
  • MF: C25H26ClN3O
  • MW: 419.95
  • Catalog: CXCR
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 603.8±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 319.0±31.5 °C

CTCE 9908 TFA

CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, inhibits migration and induces cytotoxicity in CXCR4-expressing ovarian cancer cells[1][2].

  • CAS Number: 1030384-98-5
  • MF: C86H147N27O23
  • MW: 2041.25
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CXCR4 modulator-1

CXCR4 modulator-1 (compound ZINC72372983) is a potent CXCR4 modulator with an EC50 value of 100 nM. CXCR4 modulator-1 can be used for researching anti-inflammatory, anticancer and anti-HIV[1].

  • CAS Number: 1381178-26-2
  • MF: C23H27N5O2
  • MW: 405.49
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CXCR2 antagonist 2

CXCR2 antagonist 2 is a potent CXCR2 antagonist for cancer immunotherapy with an IC50 value of 95 nM.

  • CAS Number: 2647464-91-1
  • MF: C17H17FN2O4S
  • MW: 364.39
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ACT-660602

ACT-660602 is an orally active antagonist of chemokine receptor (CXCR3) with an IC50 value of 204 nM. ACT-660602 inhibits T-cell migration and shows efficacy in acute lung ingury model. ACT-660602 can be used for autoimmune diseases research[1][2].

  • CAS Number: 1646267-59-5
  • MF: C20H20F6N8OS
  • MW: 534.48
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CXCR2 antagonist 3

CXCR2 antagonist 3 (compound 11h) is a potent antagonist of CXC chemokine receptor 2 (CXCR2). CXCR2 antagonist 3 demonstrates double-digit nanomolar potencies against CXCR2 and significantly inhibited neutrophil infiltration into the air pouch. CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs and enhance the infiltration of CD3+ T lymphocytes into the Pan02 tumor tissues[1].

  • CAS Number: 2647464-92-2
  • MF: C17H15FN2O4S
  • MW: 362.38
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CXCR4 antagonist 8

CXCR4 antagonist 8 (Compound 3) is a CXCR4 antagonist with an IC50 of 57 nM. CXCR4 antagonist 8 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 0.24 nM. CXCR4 antagonist 8 inhibits CXLC12/CXCR4 mediated cell migration[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ac-Pro-Gly-Pro-OH

Ac-Pro-Gly-Pro-OH is an endogenous degradation product of extracellular collagen and can be used as CXCR2 agonist. Ac-Pro-Gly-Pro-OH elicits bactericidal activity and inhibits lung inflammation, reducing immune cell apoptosis. Ac-Pro-Gly-Pro-OH enhances the production of type 1 cytokines (IFN-γ and IL-12) but inhibits the production of proinflammatory cytokines. Ac-Pro-Gly-Pro-OH has the potential for the research of sepsis[1][2].

  • CAS Number: 292171-04-1
  • MF: C14H21N3O5
  • MW: 311.33
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Antileukinate

Antileukinate, a hexapeptide, is a potent inhibitor of CXC-chemokine receptor (CXCR). Antileukinate inhibits neutrophil chemotaxis and activation. Antileukinate can be used for the research of acute inflammation and injury[1][2][3].

  • CAS Number: 138559-60-1
  • MF: C45H66N18O7S
  • MW: 1003.19000
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Peptide R

Peptide R, a cyclic peptide, is a specific CXCR4 antagonist. Peptide R shows outstanding capacities to profoundly remodel the tumor stroma. Peptide R has the potential for tumor research[1][2].

  • CAS Number: 1774344-28-3
  • MF: C39H59N13O8S2
  • MW: 902.10
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MSX-122

MSX-122 is a partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC50 of ∼10 nM; MSX-122 has anti-inflammatory and anti-metastatic activity.

  • CAS Number: 897657-95-3
  • MF: C16H16N6
  • MW: 292.33800
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A