Search Result
Results for "
CXCR4 antagonist
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-147808
-
|
CXCR
HIV
|
Infection
Inflammation/Immunology
Cancer
|
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 .
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-
-
- HY-136437
-
|
CXCR
HIV
|
Infection
|
CXCR4 antagonist 1 is a potent CXCR4 antagonist. CXCR4 antagonist 1 has anti-HIV activity .
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-
-
- HY-147978
-
|
CXCR
|
Infection
Cancer
|
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 .
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-
-
- HY-144286
-
|
CXCR
|
Infection
|
CXCR4 antagonist 3 (compound 12a) is a potent antagonist of CXCR4 with an IC50 of 11 nM. CXCR4 antagonist 3 is a congener of TIQ15. CXCR4 antagonist 3 demonstrates the best overall properties including CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. CXCR4 antagonist 3 has the potential for the research of human immunodeficiency virus .
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-
-
- HY-146401
-
|
CXCR
|
Cancer
|
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 .
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-
-
- HY-132936
-
|
CXCR
|
Others
|
CXCR4 antagonist 2 is a CXCR4 antagonist with an IC50 value of 47 nM.
|
-
-
- HY-168095
-
|
CXCR
|
Cancer
|
CXCR4 antagonist 10 (compound 21) is a potent antagonist of CXCR4, with the IC50 of 7.8 nM. CXCR4 antagonist 10 plays an important role in cancer research .
|
-
-
- HY-147979
-
|
CXCR
|
Infection
Cancer
|
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 .
|
-
-
- HY-146372
-
|
CXCR
|
Cancer
|
CXCR4 antagonist 5 (compound 23) is a highly potent CXCR4 antagonist with an IC50 value of 8.8 nM. CXCR4 antagonist 5 can inhibit CXCL12-induced cytosolic calcium increase (IC50 = 0.02 nM) and inhibits CXCR4/CXLC12-mediated chemotaxis. CXCR4 antagonist 5 has good physicochemical properties and in vitro safety profiles, inhibiting CYP isozymes and hERG marginally or moderately .
|
-
-
- HY-144285
-
|
CXCR
HIV
|
Inflammation/Immunology
|
CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM) .
|
-
-
- HY-P11011
-
Pep R54; CXCR4 antagonist peptide 19
|
CXCR
|
Cancer
|
Peptide R54 (Pep R54; CXCR4 antagonist peptide 19) is an antagonistic peptide targeting CXCR4 with significant anticancer activity. Peptide R54 inhibits CXCR4-dependent cell migration, epithelial-mesenchymal transition, and lung metastasis development, with better serum stability and higher CXCR4 affinity than the lead compound (IC50=20 nM). Peptide R54 synergizes with anti-PD-1 therapy to exert anti-tumor activity in vivo, enhances granzyme activity, and reduces infiltration of Foxp3 cells. Peptide R54 can be used in the study of colon cancer, ovarian cancer, and melanoma .
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-
-
- HY-103009
-
MSX-127
1 Publications Verification
|
CXCR
|
Cancer
|
MSX-127 is a CXCR4 antagonist. MSX-127 inhibits cancer metastasis .
|
-
-
- HY-103010
-
|
CXCR
|
Cancer
|
MSX-130 is a CXCR4 antagonist. MSX-130 inhibits cancer metastasis .
|
-
-
- HY-146413
-
|
CXCR
HIV
|
Infection
Cancer
|
HF50731 (compound 21) is a potent CXCR4 antagonist. HF50731 shows strong CXCR4 binding affinity, with IC50 of 19.8 nM. HF50731 effectively inhibits calcium mobilization, cell migration, and HIV-1 infection via CXCR4 coreceptor, with IC50 values of 119.2 nM, 621.4 nM and 1.5 μM .
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-
-
- HY-101458
-
-
-
- HY-101458A
-
-
-
- HY-12488
-
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CXCR
|
Endocrinology
Cancer
|
LY2510924 is a potent and selective CXCR4 antagonist that blocks SDF-1 binding to CXCR4 with an IC50 of 0.079 nM.
|
-
-
- HY-P1103
-
|
CXCR
|
Cancer
|
CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells .
|
-
-
- HY-P1104A
-
|
CXCR
HIV
|
Infection
|
FC131 TFA is a CXCR4 antagonist, inhibits [ 125I]-SDF-1 binding to CXCR4, with an IC50 of 4.5 nM. Anti-HIV activity .
|
-
-
- HY-13696
-
-
-
- HY-P1103A
-
|
CXCR
|
Cancer
|
CTCE-9908 TFA is a potent and selective CXCR4 antagonist. CTCE-9908 TFA induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells .
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-
-
- HY-111224
-
|
HIV
CXCR
|
Infection
|
GSK812397 is a CXCR4 antagonist with potential for the treatment of HIV infection. To evaluate the clinical potential of GSK812397, kilogram-scale agent candidates are needed. Here, an improved, scalable synthetic route for the CXCR4 antagonist GSK812397 is described. This new route has been scaled up in a 50-liter stationary facility to obtain 1.2 kg of agent substance in 20% overall yield and >99% chemical and enantiomeric purity in five steps. CXC chemokine receptor 4 (CXCR4) is a 7-transmembrane protein that functions in part as a host co-receptor for multiple strains of HIV-1. It is thought that targeting CXCR4 will help inhibit the replication of several late cytopathic viruses; therefore, CXCR4 antagonists are one of the most promising new classes of experimental anti-HIV agents. GSK812397 is a potent CXCR4 antagonist and is therefore a candidate for investigation for the treatment of HIV infection.
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-
-
- HY-114244
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USL311
1 Publications Verification
|
CXCR
|
Endocrinology
Cancer
|
USL311 is a potent and selective CXCR4 antagonist, with anti-tumor activity. USL311 prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4 .
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-
-
- HY-P10427A
-
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CXCR
HIV
|
Infection
|
DV1 TFA is a selective antagonist for CXC chemokine receptor 4 (CXCR4). DV1 TFA exhibits antiviral activity by blocking HIV-1 entry through the CXCR4 co-receptor .
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-
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- HY-P1104
-
|
CXCR
HIV
|
Infection
|
FC131 is a potent CXCR4 antagonist. FC131 inhibits [ 125I]-SDF-1 binding to CXCR4 with an IC50 of 4.5 nM. FC131 has anti-HIV activity .
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-
-
- HY-P10973
-
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CXCR
ERK
|
Cancer
|
Peptide R analogue 10 (compound 10) is an analog of the CXCR4 antagonist peptide Peptide R (HY-P4111) with stronger antagonistic potency, specificity and plasma stability. Peptide R analogue 10 can inhibit CXCL12-mediated cell migration, ERK phosphorylation and CXCR4 internalization. Peptide R analogue 10 can be used in the study of CXCR4 overexpressing leukemia and colon cancer .
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-
-
- HY-115493
-
|
CXCR
|
Others
|
TIQ-15 is a potent CXCR4 antagonist with an IC50 value of 6 nM for CXCR4 Ca 2+ flux. TIQ-15 inhibits CYP450 2D6 with an IC50 value of 0.32 μM .
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-
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- HY-144347
-
|
CXCR
|
Infection
Cancer
|
HF51116 is a potent antagonist of CXCR4. HF51116 strongly antagonizes SDF-1α-induced cell migration, calcium mobilization, and CXCR4 internalization. HF51116 inhibits HIV-1 infection via CXCR4. HF51116 has the potential for the research of HIV-1 infection, hematopoietic stem cell mobilization, and cancer metastasis .
|
-
-
- HY-50912
-
-
-
- HY-P0171
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BKT140 (4-fluorobenzoyl); BL-8040; TF14016
|
CXCR
|
Endocrinology
Cancer
|
Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ~1 nM.
|
-
-
- HY-122058
-
|
HIV
|
Infection
|
KRH-3955 is a CXCR4 antagonist with good bioavailability and potent anti-HIV-1 activity. KRH-3955 can effectively inhibit the replication of X4 HIV-1, including clinical isolates from different donors. KRH-3955 also shows activity against recombinant X4 HIV-1 containing reverse transcriptase, protease and tyrosinase resistance mutations. KRH-3955 can inhibit the binding of SDF-1alpha to CXCR4 and calcium ion signaling through this receptor. KRH-3955 inhibits the binding of an antibody against CXCR4 to CXCR4, showing a potent antagonistic effect on CXCR4. KRH-3955 shows an oral bioavailability of 25.6% in rats and can inhibit the replication of X4 HIV-1 in vivo .
|
-
-
- HY-P10427
-
|
CXCR
HIV
|
Infection
|
DV1 is a selective antagonist for CXC chemokine receptor 4 (CXCR4). DV1 exhibits antiviral activity by blocking HIV-1 entry through the CXCR4 co-receptor. DV1 is stable in rat plasma and exhibits good pharmacokinetic characteristics in rat models .
|
-
-
- HY-15478
-
WZ811
3 Publications Verification
|
CXCR
|
Endocrinology
Cancer
|
WZ811 is an orally active, highly potent competitive antagonist of CXCR4. WZ811 efficiently inhibits CXCR4/SDF-1 (or CXCL12)-mediated modulation of cAMP levels (EC50=1.2 nM) and SDF-1 induced Matrigel invasion in cells (EC50=5.2 nM) .
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-
-
- HY-168531
-
|
CXCR
|
Cancer
|
EMU-116 is an orally active CXCR4 antagonist. EMU-116 can be used in the study of cancer .
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-
-
- HY-P10429
-
|
CXCR
|
Infection
|
RCP168 is a highly selective and affinity CXCR4 receptor antagonist (IC50=5 nM). RCP168 has a stronger ability than natural chemical factors to inhibit the entry of HIV-1 (human immunodeficiency virus type 1) into host cells via CXCR4 receptors. RCP168 inhibits HIV-1 infection by blocking viral binding sites or inducing receptor internalization. RCP168 can be used to analyze the interaction between CXCR4 receptor and other chemical factor receptors .
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-
-
- HY-122058A
-
|
CXCR
HIV
|
Infection
Inflammation/Immunology
|
KRH-3955 hydrochloride is an orally bioavailable CXCR4 antagonist. KRH-3955 hydrochloride inhibits SDF-1α binding to CXCR4 with an IC50 of 0.61 nM. KRH-3955 hydrochloride is also a highly potent and selective inhibitor of X4 HIV-1, with an EC50 of 0.3 to 1.0 nM .
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-
-
- HY-P991656
-
|
CXCR
Apoptosis
p38 MAPK
Akt
|
Cancer
|
LY-2624587 is a humanized IgG4 monoclonal antibody antagonist targeting CXCR4. LY-2624587 blocks SDF-1/CXCR4 interaction and SDF-1-induced GTP binding. LY-2624587 significantly inhibits cell migration and induces apoptosis in human lymphoma and leukemia cells. LY-2624587 also inhibits CXCR4 and SDF-1 mediated cell signaling including activation of MAPK and AKT. LY-2624587 can be used for human hematological malignancies like acute myeloid leukemia (AML) research .
|
-
-
- HY-19867A
-
TG-0054 hydrobromide
|
CXCR
VEGFR
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
Cancer
|
Burixafor (TG-0054) hydrobromide is a selective, orally active CXCR4 antagonist that effectively blocks the interaction between CXCR4 and its ligand, stromal cell-derived factor SDF-1. Burixafor hydrobromide interferes with the SDF-1/CXCR4 signaling pathway, prompting the release of bone marrow stem cells into the peripheral circulation, exerting immunomodulatory and anti-inflammatory activities. Burixafor hydrobromide can be used in the study of cancer, Intraocular neovascular diseases (such as choroidal neovascularization), myocardial infarction and other diseases, with the potential to mobilize stem cells, improve cardiac function and reduce inflammatory responses .
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-
-
- HY-P7061A
-
|
Apelin Receptor (APJ)
CXCR
|
Infection
Endocrinology
|
ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
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-
-
- HY-P7061
-
|
CXCR
Apelin Receptor (APJ)
|
Infection
Endocrinology
|
ALX 40-4C is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
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-
-
- HY-50101A
-
AMD-070 trihydrochloride; AMD-11070 trihydrochloride
|
CXCR
HIV
|
Infection
Endocrinology
Cancer
|
Mavorixafor trihydrochloride (AMD-070 trihydrochloride) 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.Mavorixafor trihydrochloride can be used for the study of WHIM syndrome .
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-
-
- HY-50101
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AMD-070; AMD-11070
|
CXCR
HIV
|
Infection
Endocrinology
Cancer
|
Mavorixafor (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. Mavorixafor can be used for the study of WHIM syndrome .
|
-
-
- HY-50101C
-
AMD-070 hydrochloride; AMD-11070 hydrochloride
|
CXCR
HIV
|
Infection
Cancer
|
Mavorixafor (AMD-070) hydrochloride is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding. Mavorixafor hydrochloride also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 nM and 9 nM, respectively. Mavorixafor hydrochloride can be used for the study of WHIM syndrome .
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-
-
- HY-15971A
-
GENZ-644494
|
CXCR
HIV
|
Infection
Endocrinology
|
AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
|
-
-
- HY-50912R
-
|
CXCR
HIV
Virus Protease
|
Inflammation/Immunology
Endocrinology
Cancer
|
Plerixafor (octahydrochloride) (Standard) is the analytical standard of Plerixafor (octahydrochloride). This product is intended for research and analytical applications. Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an IC50 of 44 nM.
|
-
-
- HY-P1682
-
POL6326
|
CXCR
Arrestin
|
Cancer
|
Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
|
-
-
- HY-15971
-
GENZ-644494 hexahydrobromide
|
CXCR
HIV
|
Infection
Endocrinology
|
AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
|
-
-
- HY-P4111
-
|
CXCR
|
Cancer
|
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 .
|
-
-
- HY-P10415
-
EPI-X4
1 Publications Verification
hSA(408–423) peptide
|
CXCR
|
Infection
Inflammation/Immunology
Cancer
|
EPI-X4 (hSA408–423 peptide) is an antagonist for C-X-C motif chemokine receptor 4 (CXCR4) with IC50 of 8.6 μM. EPI-X4 blocks the CXCL12-mediated signaling, inhibits chemokine-mediated migration and invasion of leukemia cell. EPI-X4 exhibits anti-inflammatory activity in mouse model. EPI-X4 exhibits antiviral activity against CXCR4-tropic HIV with IC50 of 8.6 μM .
|
-
-
- HY-P1682A
-
POL6326 TFA
|
CXCR
Arrestin
|
Cancer
|
Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
|
-
- HY-15971AR
-
|
CXCR
HIV
|
Infection
Endocrinology
|
AMD 3465 (Standard) is the analytical standard of AMD 3465. This product is intended for research and analytical applications. AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
|
-
- HY-12080
-
ZK-811752
|
CCR
|
Inflammation/Immunology
Endocrinology
|
BX471 (ZK-811752) is an orally active, potent and selective non-peptide CCR1 antagonist with a Ki of 1 nM, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
|
-
- HY-12080A
-
ZK-811752 hydrochloride
|
CCR
|
Inflammation/Immunology
Endocrinology
|
BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with Ki of 1 nM for human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
|
-
- HY-P4111A
-
|
CXCR
|
Cancer
|
Peptide R (TFA) is a synthetic and specific CXCR4 antagonist. Peptide R (TFA) shows outstanding capacities to remodel the tumor stroma. Peptide R (TFA) can be used for solid tumor (glioblastoma, etc.) research .
|
-
- HY-15971R
-
|
CXCR
HIV
|
Infection
Endocrinology
|
AMD 3465 (hexahydrobromide) (Standard) is the analytical standard of AMD 3465 (hexahydrobromide). This product is intended for research and analytical applications. AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
|
-
- HY-10046
-
Plerixafor
Maximum Cited Publications
88 Publications Verification
AMD 3100; JM3100; SID791
|
CXCR
HIV
|
Infection
Inflammation/Immunology
Endocrinology
Cancer
|
Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM .
|
-
- HY-129094
-
|
CXCR
|
Cancer
|
ICT5040 is a small molecule CXCR4 antagonist (IC50=3.8 μM). ICT5040 inhibits CXCL12-mediated proliferation and migration, and suppresses CXCL12-induced intracellular calcium mobilisation in U87 glioma cells .
|
-
- HY-P1102
-
TC14012
3 Publications Verification
|
CXCR
HIV
|
Infection
Cancer
|
TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity .
|
-
- HY-P1102A
-
|
CXCR
HIV
|
Infection
Cancer
|
TC14012 TFA, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 TFA is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity .
|
-
- HY-10046S
-
-
- HY-10046R
-
AMD 3100 (Standard); JM3100 (Standard); SID791 (Standard)
|
Reference Standards
CXCR
HIV
|
Infection
Inflammation/Immunology
Endocrinology
Cancer
|
Plerixafor (Standard) is the analytical standard of Plerixafor. This product is intended for research and analytical applications. Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM .
|
-
- HY-D0976
-
|
P2X Receptor
HIV
|
Infection
|
NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC50 of 19 nM. NF279 displays good selectivity over P2X2, P2X3 (IC50=1.62 μM), P2X4 (IC50>300 μM). NF279 is a dual HIV-1 coreceptor inhibitor that interferes with the functional engagement of CCR5 and CXCR4 by Env .
|
-
- HY-122197
-
ML339
3 Publications Verification
|
CXCR
Apelin Receptor (APJ)
Arrestin
|
Cancer
|
ML339 is a selective CXCR6 antagonist with an IC50 of 140 nM. ML339 antagonizes β-arrestin recruitment and cAMP signaling pathway of human CXCR6 receptor induced by CXCL16, with IC50 of 0.3 μM and 1.4 μM, respectively. ML339 shows weaker activity against the recruitment of β-arrestin in mouse CXCR6 receptors, with an IC50 of 18 μM. ML339 has no inhibitory effect on CXCR5,CXCR4,CXCR6 and apelin receptor (APJ), with IC50 >79 μM. ML339 has the potential to promote the development of prostate cancer research .
|
-
- HY-P10971
-
|
CXCR
Apoptosis
VEGFR
GSK-3
Cadherin
Caspase
|
Cancer
|
Nef-M1 (Nef-Motif-1) is an antagonist peptide targeting CXCR4 and an apoptosis inducer derived from a myristoylated protein encoded by the nef gene in HIV. Nef-M1 inhibits tumor angiogenesis and epithelial-mesenchymal transition (EMT). Nef-M1 activates the apoptosis pathway by increasing the level of caspase-3 in cancer cells. Nef-M1 simultaneously inhibits VEGF-A, p-GSK-3β and vimentin, and enhances E-cadherin, thereby inhibiting angiogenesis and EMT processes. Nef-M1 can be used in the study of colorectal cancer and breast cancer .
|
-
- HY-123819
-
|
CXCR
|
Infection
|
KRH-1636 is a CXC chemokine receptor (CXCR) 4 antagonist. KRH-1636 can be used in HIV-1 research .
|
-
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-12488
-
LY2510924
Maximum Cited Publications
12 Publications Verification
|
CXCR
|
Endocrinology
Cancer
|
LY2510924 is a potent and selective CXCR4 antagonist that blocks SDF-1 binding to CXCR4 with an IC50 of 0.079 nM.
|
-
- HY-P1103
-
|
CXCR
|
Cancer
|
CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells .
|
-
- HY-P1104A
-
|
CXCR
HIV
|
Infection
|
FC131 TFA is a CXCR4 antagonist, inhibits [ 125I]-SDF-1 binding to CXCR4, with an IC50 of 4.5 nM. Anti-HIV activity .
|
-
- HY-168095
-
|
CXCR
|
Cancer
|
CXCR4 antagonist 10 (compound 21) is a potent antagonist of CXCR4, with the IC50 of 7.8 nM. CXCR4 antagonist 10 plays an important role in cancer research .
|
-
- HY-144285
-
|
CXCR
HIV
|
Inflammation/Immunology
|
CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM) .
|
-
- HY-P11011
-
Pep R54; CXCR4 antagonist peptide 19
|
CXCR
|
Cancer
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Peptide R54 (Pep R54; CXCR4 antagonist peptide 19) is an antagonistic peptide targeting CXCR4 with significant anticancer activity. Peptide R54 inhibits CXCR4-dependent cell migration, epithelial-mesenchymal transition, and lung metastasis development, with better serum stability and higher CXCR4 affinity than the lead compound (IC50=20 nM). Peptide R54 synergizes with anti-PD-1 therapy to exert anti-tumor activity in vivo, enhances granzyme activity, and reduces infiltration of Foxp3 cells. Peptide R54 can be used in the study of colon cancer, ovarian cancer, and melanoma .
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- HY-P1103A
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CXCR
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Cancer
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CTCE-9908 TFA is a potent and selective CXCR4 antagonist. CTCE-9908 TFA induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells .
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- HY-P10427A
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CXCR
HIV
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Infection
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DV1 TFA is a selective antagonist for CXC chemokine receptor 4 (CXCR4). DV1 TFA exhibits antiviral activity by blocking HIV-1 entry through the CXCR4 co-receptor .
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- HY-P1104
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CXCR
HIV
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Infection
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FC131 is a potent CXCR4 antagonist. FC131 inhibits [ 125I]-SDF-1 binding to CXCR4 with an IC50 of 4.5 nM. FC131 has anti-HIV activity .
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- HY-P10973
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CXCR
ERK
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Cancer
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Peptide R analogue 10 (compound 10) is an analog of the CXCR4 antagonist peptide Peptide R (HY-P4111) with stronger antagonistic potency, specificity and plasma stability. Peptide R analogue 10 can inhibit CXCL12-mediated cell migration, ERK phosphorylation and CXCR4 internalization. Peptide R analogue 10 can be used in the study of CXCR4 overexpressing leukemia and colon cancer .
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- HY-P0171
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BKT140 (4-fluorobenzoyl); BL-8040; TF14016
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CXCR
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Endocrinology
Cancer
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Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ~1 nM.
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- HY-P10427
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CXCR
HIV
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Infection
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DV1 is a selective antagonist for CXC chemokine receptor 4 (CXCR4). DV1 exhibits antiviral activity by blocking HIV-1 entry through the CXCR4 co-receptor. DV1 is stable in rat plasma and exhibits good pharmacokinetic characteristics in rat models .
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- HY-P10429
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CXCR
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Infection
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RCP168 is a highly selective and affinity CXCR4 receptor antagonist (IC50=5 nM). RCP168 has a stronger ability than natural chemical factors to inhibit the entry of HIV-1 (human immunodeficiency virus type 1) into host cells via CXCR4 receptors. RCP168 inhibits HIV-1 infection by blocking viral binding sites or inducing receptor internalization. RCP168 can be used to analyze the interaction between CXCR4 receptor and other chemical factor receptors .
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- HY-P7061A
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Apelin Receptor (APJ)
CXCR
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Infection
Endocrinology
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ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
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- HY-P7061
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CXCR
Apelin Receptor (APJ)
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Infection
Endocrinology
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ALX 40-4C is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
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- HY-P1682
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POL6326
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CXCR
Arrestin
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Cancer
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Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
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- HY-P4111
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CXCR
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Cancer
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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 .
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- HY-P10415
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EPI-X4
1 Publications Verification
hSA(408–423) peptide
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CXCR
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Infection
Inflammation/Immunology
Cancer
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EPI-X4 (hSA408–423 peptide) is an antagonist for C-X-C motif chemokine receptor 4 (CXCR4) with IC50 of 8.6 μM. EPI-X4 blocks the CXCL12-mediated signaling, inhibits chemokine-mediated migration and invasion of leukemia cell. EPI-X4 exhibits anti-inflammatory activity in mouse model. EPI-X4 exhibits antiviral activity against CXCR4-tropic HIV with IC50 of 8.6 μM .
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- HY-P1682A
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POL6326 TFA
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CXCR
Arrestin
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Cancer
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Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
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- HY-P4111A
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CXCR
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Cancer
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Peptide R (TFA) is a synthetic and specific CXCR4 antagonist. Peptide R (TFA) shows outstanding capacities to remodel the tumor stroma. Peptide R (TFA) can be used for solid tumor (glioblastoma, etc.) research .
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- HY-P1102
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TC14012
3 Publications Verification
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CXCR
HIV
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Infection
Cancer
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TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity .
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- HY-P1102A
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CXCR
HIV
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Infection
Cancer
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TC14012 TFA, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 TFA is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity .
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- HY-P10971
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CXCR
Apoptosis
VEGFR
GSK-3
Cadherin
Caspase
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Cancer
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Nef-M1 (Nef-Motif-1) is an antagonist peptide targeting CXCR4 and an apoptosis inducer derived from a myristoylated protein encoded by the nef gene in HIV. Nef-M1 inhibits tumor angiogenesis and epithelial-mesenchymal transition (EMT). Nef-M1 activates the apoptosis pathway by increasing the level of caspase-3 in cancer cells. Nef-M1 simultaneously inhibits VEGF-A, p-GSK-3β and vimentin, and enhances E-cadherin, thereby inhibiting angiogenesis and EMT processes. Nef-M1 can be used in the study of colorectal cancer and breast cancer .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P991656
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CXCR
Apoptosis
p38 MAPK
Akt
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Cancer
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LY-2624587 is a humanized IgG4 monoclonal antibody antagonist targeting CXCR4. LY-2624587 blocks SDF-1/CXCR4 interaction and SDF-1-induced GTP binding. LY-2624587 significantly inhibits cell migration and induces apoptosis in human lymphoma and leukemia cells. LY-2624587 also inhibits CXCR4 and SDF-1 mediated cell signaling including activation of MAPK and AKT. LY-2624587 can be used for human hematological malignancies like acute myeloid leukemia (AML) research .
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-10046S
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Plerixafor-d4 is the deuterium labeled Plerixafor. Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM .
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