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sch546738  (MedChemExpress)


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    Structured Review

    MedChemExpress sch546738
    Sch546738, supplied by MedChemExpress, used in various techniques. Bioz Stars score: 95/100, based on 23 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/product/sch546738/SCH+546738/pmc12786925-234-47-51
    Average 95 stars, based on 23 article reviews
    sch546738 - by Bioz Stars, 2026-09
    95/100 stars

    Images

    Related Articles

    Isolation:


    Article Title: NDRG1‐Driven Lactate Accumulation Promotes Lung Adenocarcinoma Progression Through the Induction of an Immunosuppressive Microenvironment
    Article Snippet: The T cell migration assay was conducted using a 24‐well Transwell system with 5.0 μm pore polycarbonate membrane inserts (Corning, 3421). .. Bone marrow‐derived macrophages (BMDMs) were co‐cultured with tumor cells or treated with tumor‐conditioned medium (TCM) for 12 h. CD8 + T cells were isolated from wild‐type mouse spleens using a CD8 + T Cell Isolation Kit (Miltenyi Biotec, 130‐095‐236), suspended in 200 μL of 1% FBS‐RPMI 1640 medium, and placed in the upper chamber with or without 100 nM SCH546738 (MedChemExpress, HY‐10017). ..

    Article Title: NDRG1-Driven Lactate Accumulation Promotes Lung Adenocarcinoma Progression Through the Induction of an Immunosuppressive Microenvironment.
    Article Snippet: See the T erm s and C onditions (https://onlinelibrary.w iley.com /term s-and-conditions) on W iley O nline L ibrary for rules of use; O A articles are governed by the applicable C reative C om m ons L icense inserts (Corning, 3421). .. Bone marrow-derived macrophages (BMDMs) were co-cultured with tumor cells or treated with tumor-conditioned medium (TCM) for 12 h. CD8+ T cells were isolated from wild-type mouse spleens using a CD8+ T Cell Isolation Kit (Miltenyi Biotec, 130-095-236), suspended in 200 μL of 1% FBS-RPMI 1640 medium, and placed in the upper chamber with or without 100 nM SCH546738 (MedChemExpress, HY-10017). ..

    Magnetic Beads:


    Cell Isolation:

    Article Title: NDRG1‐Driven Lactate Accumulation Promotes Lung Adenocarcinoma Progression Through the Induction of an Immunosuppressive Microenvironment
    Article Snippet: The T cell migration assay was conducted using a 24‐well Transwell system with 5.0 μm pore polycarbonate membrane inserts (Corning, 3421). .. Bone marrow‐derived macrophages (BMDMs) were co‐cultured with tumor cells or treated with tumor‐conditioned medium (TCM) for 12 h. CD8 + T cells were isolated from wild‐type mouse spleens using a CD8 + T Cell Isolation Kit (Miltenyi Biotec, 130‐095‐236), suspended in 200 μL of 1% FBS‐RPMI 1640 medium, and placed in the upper chamber with or without 100 nM SCH546738 (MedChemExpress, HY‐10017). ..

    Article Title: NDRG1-Driven Lactate Accumulation Promotes Lung Adenocarcinoma Progression Through the Induction of an Immunosuppressive Microenvironment.
    Article Snippet: See the T erm s and C onditions (https://onlinelibrary.w iley.com /term s-and-conditions) on W iley O nline L ibrary for rules of use; O A articles are governed by the applicable C reative C om m ons L icense inserts (Corning, 3421). .. Bone marrow-derived macrophages (BMDMs) were co-cultured with tumor cells or treated with tumor-conditioned medium (TCM) for 12 h. CD8+ T cells were isolated from wild-type mouse spleens using a CD8+ T Cell Isolation Kit (Miltenyi Biotec, 130-095-236), suspended in 200 μL of 1% FBS-RPMI 1640 medium, and placed in the upper chamber with or without 100 nM SCH546738 (MedChemExpress, HY-10017). ..

    Control:

    Article Title: CXCL9 and CXCL10 Induce Expression of Nociceptive Ion Channels in Primary Sensory Neurons in Models of HIV-Associated Distal Sensory Polyneuropathy
    Article Snippet: .. Exposure of iPSC-PSNs was performed by half media change with neuronal media (neuronal control), X-vivo 15 (X-vivo control), untreated MDM media (MDM control), IFNγ-treated MDM media, and LPS-treated MDM media and subsequently incubated for 24 h. CXCR3 antagonism was performed by preincubation of iPSC-PSNs with 12 μM SCH546738 for 15 min (MedChemExpress, Monmouth Junction, NJ, USA) prior to conditioned media treatment. ..

    Article Title: CXCL9 and CXCL10 Induce Expression of Nociceptive Ion Channels in Primary Sensory Neurons in Models of HIV-Associated Distal Sensory Polyneuropathy
    Article Snippet: .. Exposure of iPSC-PSNs was per- https://doi.org/10.3390/ijms27010523 formed by half media change with neuronal media (neuronal control), X-vivo 15 (X-vivo control), untreated MDM media (MDM control), IFNγ-treated MDM media, and LPStreated MDM media and subsequently incubated for 24 h. CXCR3 antagonism was performed by preincubation of iPSC-PSNs with 12 μM SCH546738 for 15 min (MedChemExpress, Monmouth Junction, NJ, USA) prior to conditioned media treatment. ..

    Incubation:

    Article Title: CXCL9 and CXCL10 Induce Expression of Nociceptive Ion Channels in Primary Sensory Neurons in Models of HIV-Associated Distal Sensory Polyneuropathy
    Article Snippet: .. Exposure of iPSC-PSNs was performed by half media change with neuronal media (neuronal control), X-vivo 15 (X-vivo control), untreated MDM media (MDM control), IFNγ-treated MDM media, and LPS-treated MDM media and subsequently incubated for 24 h. CXCR3 antagonism was performed by preincubation of iPSC-PSNs with 12 μM SCH546738 for 15 min (MedChemExpress, Monmouth Junction, NJ, USA) prior to conditioned media treatment. ..

    Article Title: CXCL9 and CXCL10 Induce Expression of Nociceptive Ion Channels in Primary Sensory Neurons in Models of HIV-Associated Distal Sensory Polyneuropathy
    Article Snippet: .. Exposure of iPSC-PSNs was per- https://doi.org/10.3390/ijms27010523 formed by half media change with neuronal media (neuronal control), X-vivo 15 (X-vivo control), untreated MDM media (MDM control), IFNγ-treated MDM media, and LPStreated MDM media and subsequently incubated for 24 h. CXCR3 antagonism was performed by preincubation of iPSC-PSNs with 12 μM SCH546738 for 15 min (MedChemExpress, Monmouth Junction, NJ, USA) prior to conditioned media treatment. ..

    Protease Inhibitor:

    Article Title: Structural insights into the activation and inhibition of CXC chemokine receptor 3
    Article Snippet: The only difference is that 4.2 μM PS372424 (MedChemExpress) or 0.72 μM VUF11222 (Tocris Bioscience) was added to all the buffers in protein purification. .. The cell pellets of CXCR3 κOR were thawed in 20 mM HEPES-Na, pH 7.5, 300 mM NaCl, 1% LMNG, 0.2% CHS, 10% glycerol, 0.1 μM SCH546738 (MedChemExpress) and complete protease inhibitor cocktail. ..



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    Molecular Dynamics Inc dynamics simulation of sch546738 binding
    a – c , Density maps and cartoon models of CXCR3–CXCL11–DNG i -scFv16 ( a ), CXCR3–PS372424–DNG i -scFv16 ( b ) and CXCR3–VUF11222–DNG i -scFv16 ( c ). Receptor, ligand, DNG αi , G β , G γ and scFv16 are colored violet, cyan, blue, green, orange and gray, respectively. PS372424 and VUF11222 are shown as spheres. d , Density map and cartoon model of CXCR3 κOR <t>–SCH546738-Nb6.</t> CXCR3, κOR fragment, SCH546738 and Nb6 are colored violet, orange, cyan and gray, respectively. SCH546738 is shown with spheres.
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    Image Search Results


    a – c , Density maps and cartoon models of CXCR3–CXCL11–DNG i -scFv16 ( a ), CXCR3–PS372424–DNG i -scFv16 ( b ) and CXCR3–VUF11222–DNG i -scFv16 ( c ). Receptor, ligand, DNG αi , G β , G γ and scFv16 are colored violet, cyan, blue, green, orange and gray, respectively. PS372424 and VUF11222 are shown as spheres. d , Density map and cartoon model of CXCR3 κOR –SCH546738-Nb6. CXCR3, κOR fragment, SCH546738 and Nb6 are colored violet, orange, cyan and gray, respectively. SCH546738 is shown with spheres.

    Journal: Nature Structural & Molecular Biology

    Article Title: Structural insights into the activation and inhibition of CXC chemokine receptor 3

    doi: 10.1038/s41594-023-01175-5

    Figure Lengend Snippet: a – c , Density maps and cartoon models of CXCR3–CXCL11–DNG i -scFv16 ( a ), CXCR3–PS372424–DNG i -scFv16 ( b ) and CXCR3–VUF11222–DNG i -scFv16 ( c ). Receptor, ligand, DNG αi , G β , G γ and scFv16 are colored violet, cyan, blue, green, orange and gray, respectively. PS372424 and VUF11222 are shown as spheres. d , Density map and cartoon model of CXCR3 κOR –SCH546738-Nb6. CXCR3, κOR fragment, SCH546738 and Nb6 are colored violet, orange, cyan and gray, respectively. SCH546738 is shown with spheres.

    Article Snippet: Fig. 6 Discovery of an allosteric site in the structure of CXCR3 occupied by SCH546738. a , The chemical structure of SCH546738. b , Molecular dynamics simulation of SCH546738 binding.

    Techniques:

    a Elution curve of CXCR3-CXCL11-DNG i -scFv16 complex on Superose 6 Increase column. b SDS-PAGE of CXCR3-CXCL11-DNG i -scFv16 complex after size-exclusion chromatography. c Cryo-EM image of CXCR3-CXCL11-DNG i -scFv16 particles (a representative of 5,500 micrographs). d Elution curve of CXCR3-PS372424-DNG i -scFv16 complex on Superose 6 Increase column. e SDS-PAGE of CXCR3-PS372424-DNG i -scFv16 complex after size-exclusion chromatography. f Cryo-EM image of CXCR3-PS372424-DNG i -scFv16 particles (a representative of 3,185 micrographs). g Elution curve of CXCR3-VUF11222-DNG i -scFv16 complex on Superose 6 Increase column. h SDS-PAGE of CXCR3-VUF11222-DNG i -scFv16 complex after size-exclusion chromatography. i Cryo-EM image of CXCR3-VUF11222-DNG i -scFv16 particles (a representative of 2,891 micrographs). j Elution curve of CXCR3 κOR -SCH546738-Nb6 complex on Superose 6 Increase column. k SDS-PAGE of CXCR3 κOR -SCH546738-Nb6 complex after size-exclusion chromatography. l Cryo-EM image of CXCR3 κOR -SCH546738-Nb6 particles (a representative of 12,944 micrographs). In b, e, h, and k, data shown are representative of two independent experiments.

    Journal: Nature Structural & Molecular Biology

    Article Title: Structural insights into the activation and inhibition of CXC chemokine receptor 3

    doi: 10.1038/s41594-023-01175-5

    Figure Lengend Snippet: a Elution curve of CXCR3-CXCL11-DNG i -scFv16 complex on Superose 6 Increase column. b SDS-PAGE of CXCR3-CXCL11-DNG i -scFv16 complex after size-exclusion chromatography. c Cryo-EM image of CXCR3-CXCL11-DNG i -scFv16 particles (a representative of 5,500 micrographs). d Elution curve of CXCR3-PS372424-DNG i -scFv16 complex on Superose 6 Increase column. e SDS-PAGE of CXCR3-PS372424-DNG i -scFv16 complex after size-exclusion chromatography. f Cryo-EM image of CXCR3-PS372424-DNG i -scFv16 particles (a representative of 3,185 micrographs). g Elution curve of CXCR3-VUF11222-DNG i -scFv16 complex on Superose 6 Increase column. h SDS-PAGE of CXCR3-VUF11222-DNG i -scFv16 complex after size-exclusion chromatography. i Cryo-EM image of CXCR3-VUF11222-DNG i -scFv16 particles (a representative of 2,891 micrographs). j Elution curve of CXCR3 κOR -SCH546738-Nb6 complex on Superose 6 Increase column. k SDS-PAGE of CXCR3 κOR -SCH546738-Nb6 complex after size-exclusion chromatography. l Cryo-EM image of CXCR3 κOR -SCH546738-Nb6 particles (a representative of 12,944 micrographs). In b, e, h, and k, data shown are representative of two independent experiments.

    Article Snippet: Fig. 6 Discovery of an allosteric site in the structure of CXCR3 occupied by SCH546738. a , The chemical structure of SCH546738. b , Molecular dynamics simulation of SCH546738 binding.

    Techniques: SDS Page, Size-exclusion Chromatography, Cryo-EM Sample Prep

    a Cryo-EM data processing of CXCR3-CXCL11-DNG i -scFv16. The local resolution map and the FSC curve are presented as well. b Cryo-EM data processing of CXCR3-PS372424-DNG i -scFv16. The local resolution map and the FSC curve are presented as well. c Cryo-EM data processing of CXCR3-VUF11222-DNG i -scFv16. The local resolution map and the FSC curve are presented as well. d Cryo-EM data processing of CXCR3 κOR -SCH546738-Nb6. The local resolution map and the FSC curve are presented as well.

    Journal: Nature Structural & Molecular Biology

    Article Title: Structural insights into the activation and inhibition of CXC chemokine receptor 3

    doi: 10.1038/s41594-023-01175-5

    Figure Lengend Snippet: a Cryo-EM data processing of CXCR3-CXCL11-DNG i -scFv16. The local resolution map and the FSC curve are presented as well. b Cryo-EM data processing of CXCR3-PS372424-DNG i -scFv16. The local resolution map and the FSC curve are presented as well. c Cryo-EM data processing of CXCR3-VUF11222-DNG i -scFv16. The local resolution map and the FSC curve are presented as well. d Cryo-EM data processing of CXCR3 κOR -SCH546738-Nb6. The local resolution map and the FSC curve are presented as well.

    Article Snippet: Fig. 6 Discovery of an allosteric site in the structure of CXCR3 occupied by SCH546738. a , The chemical structure of SCH546738. b , Molecular dynamics simulation of SCH546738 binding.

    Techniques: Cryo-EM Sample Prep

    Statistics of data collection, data processing, model refinement and validation

    Journal: Nature Structural & Molecular Biology

    Article Title: Structural insights into the activation and inhibition of CXC chemokine receptor 3

    doi: 10.1038/s41594-023-01175-5

    Figure Lengend Snippet: Statistics of data collection, data processing, model refinement and validation

    Article Snippet: Fig. 6 Discovery of an allosteric site in the structure of CXCR3 occupied by SCH546738. a , The chemical structure of SCH546738. b , Molecular dynamics simulation of SCH546738 binding.

    Techniques: Biomarker Discovery

    a Density maps of the transmembrane helixes and CXCL11 in the structure of CXCR3-CXCL11-DNG i -scFv16. b Density maps of the transmembrane helixes and PS372424 in the structure of CXCR3- PS372424 -DNG i -scFv16. c Density maps of the transmembrane helixes and VUF11222 in the structure of CXCR3- VUF11222 -DNG i -scFv16. d Density maps of the transmembrane helixes and SCH546738 in the structure of CXCR3 κOR - SCH546738-Nb6.

    Journal: Nature Structural & Molecular Biology

    Article Title: Structural insights into the activation and inhibition of CXC chemokine receptor 3

    doi: 10.1038/s41594-023-01175-5

    Figure Lengend Snippet: a Density maps of the transmembrane helixes and CXCL11 in the structure of CXCR3-CXCL11-DNG i -scFv16. b Density maps of the transmembrane helixes and PS372424 in the structure of CXCR3- PS372424 -DNG i -scFv16. c Density maps of the transmembrane helixes and VUF11222 in the structure of CXCR3- VUF11222 -DNG i -scFv16. d Density maps of the transmembrane helixes and SCH546738 in the structure of CXCR3 κOR - SCH546738-Nb6.

    Article Snippet: Fig. 6 Discovery of an allosteric site in the structure of CXCR3 occupied by SCH546738. a , The chemical structure of SCH546738. b , Molecular dynamics simulation of SCH546738 binding.

    Techniques:

    a , Comparison of the insertion depth of the three agonists. The receptors are shown as cartoons and the ligands are shown as sticks. CXCL11, PS372424 and VUF11222 are colored violet, yellow and blue, respectively. b , Superposition of CXCL11-activated CXCR3 (violet) and PS372424-activated CXCR3 (yellow). c , Superposition of CXCL11-activated CXCR3 (violet) and VUF11222-activated CXCR3 (blue). d , The residues in CXCR3 involved in the interactions with CXCL11 (violet), PS372424 (yellow) and VUF11222 (blue). The residues are shown as sticks, and the CXCL11-activated CXCR3 are shown as cartoons. e , Comparison of CXCL11-activated CXCR3 (violet) and SCH546378-inhibited CXCR3 (green). f , The packing between TM3 and TM6 in the CXCR3 inhibited by antagonist SCH546738. CXCR3 is shown as a cartoon model and colored green and residues involved in TM packing are shown as sticks. g , The packing between TM5 and TM6 in the CXCR3 activated by chemokine CXCL11. CXCR3 is shown as a cartoon model and colored violet, and residues involved in TM packing are shown as sticks. h , Outward displacement of TM6 on CXCL11 binding leads to the exposure of the G αi binding pocket. The CXCL11-activated CXCR3, SCH546378-inhibited CXCR3 and G αi are shown as cartoon and colored violet, green and gray, respectively.

    Journal: Nature Structural & Molecular Biology

    Article Title: Structural insights into the activation and inhibition of CXC chemokine receptor 3

    doi: 10.1038/s41594-023-01175-5

    Figure Lengend Snippet: a , Comparison of the insertion depth of the three agonists. The receptors are shown as cartoons and the ligands are shown as sticks. CXCL11, PS372424 and VUF11222 are colored violet, yellow and blue, respectively. b , Superposition of CXCL11-activated CXCR3 (violet) and PS372424-activated CXCR3 (yellow). c , Superposition of CXCL11-activated CXCR3 (violet) and VUF11222-activated CXCR3 (blue). d , The residues in CXCR3 involved in the interactions with CXCL11 (violet), PS372424 (yellow) and VUF11222 (blue). The residues are shown as sticks, and the CXCL11-activated CXCR3 are shown as cartoons. e , Comparison of CXCL11-activated CXCR3 (violet) and SCH546378-inhibited CXCR3 (green). f , The packing between TM3 and TM6 in the CXCR3 inhibited by antagonist SCH546738. CXCR3 is shown as a cartoon model and colored green and residues involved in TM packing are shown as sticks. g , The packing between TM5 and TM6 in the CXCR3 activated by chemokine CXCL11. CXCR3 is shown as a cartoon model and colored violet, and residues involved in TM packing are shown as sticks. h , Outward displacement of TM6 on CXCL11 binding leads to the exposure of the G αi binding pocket. The CXCL11-activated CXCR3, SCH546378-inhibited CXCR3 and G αi are shown as cartoon and colored violet, green and gray, respectively.

    Article Snippet: Fig. 6 Discovery of an allosteric site in the structure of CXCR3 occupied by SCH546738. a , The chemical structure of SCH546738. b , Molecular dynamics simulation of SCH546738 binding.

    Techniques: Comparison, Binding Assay

    a , The chemical structure of SCH546738. b , Molecular dynamics simulation of SCH546738 binding. Shown are the cryo-EM structure and the top three cluster centroids. The size of each cluster is represented as the percentage of the total number of frames in the trajectories. c , A general view of the SCH546738 binding pocket in CXCR3. SCH546738 and CXCR3 are shown as a stick model (colored gray) and surface model (colored by electronic potential), respectively. d , Interactions between SCH546738 (gray) and CXCR3 (green). SCH546738 and the residues involved in interactions are shown as sticks. e , cAMP responses of CXCR3 to CXCL11 in the presence of SCH546738 at different concentrations. f , cAMP responses of CXCR3 V261F to CXCL11 in the presence of SCH546738 at different concentrations. g , cAMP responses of CXCR3 A265F to CXCL11 in the presence of SCH546738 at different concentrations. In e – g , the data represent means ± s.e.m. ( n = 6 independent experiments). h , Comparison of the allosteric binding sites outside the TMs in class A GPCR. The receptors are shown as cartoons and the antagonists are shown as spheres. Allosteric binding sites are indicated by red circles.

    Journal: Nature Structural & Molecular Biology

    Article Title: Structural insights into the activation and inhibition of CXC chemokine receptor 3

    doi: 10.1038/s41594-023-01175-5

    Figure Lengend Snippet: a , The chemical structure of SCH546738. b , Molecular dynamics simulation of SCH546738 binding. Shown are the cryo-EM structure and the top three cluster centroids. The size of each cluster is represented as the percentage of the total number of frames in the trajectories. c , A general view of the SCH546738 binding pocket in CXCR3. SCH546738 and CXCR3 are shown as a stick model (colored gray) and surface model (colored by electronic potential), respectively. d , Interactions between SCH546738 (gray) and CXCR3 (green). SCH546738 and the residues involved in interactions are shown as sticks. e , cAMP responses of CXCR3 to CXCL11 in the presence of SCH546738 at different concentrations. f , cAMP responses of CXCR3 V261F to CXCL11 in the presence of SCH546738 at different concentrations. g , cAMP responses of CXCR3 A265F to CXCL11 in the presence of SCH546738 at different concentrations. In e – g , the data represent means ± s.e.m. ( n = 6 independent experiments). h , Comparison of the allosteric binding sites outside the TMs in class A GPCR. The receptors are shown as cartoons and the antagonists are shown as spheres. Allosteric binding sites are indicated by red circles.

    Article Snippet: Fig. 6 Discovery of an allosteric site in the structure of CXCR3 occupied by SCH546738. a , The chemical structure of SCH546738. b , Molecular dynamics simulation of SCH546738 binding.

    Techniques: Binding Assay, Cryo-EM Sample Prep, Comparison

    Journal: Nature Structural & Molecular Biology

    Article Title: Structural insights into the activation and inhibition of CXC chemokine receptor 3

    doi: 10.1038/s41594-023-01175-5

    Figure Lengend Snippet: The potencies of CXCL11 with the receptor or its mutants in the present of different concentrations of SCH546738

    Article Snippet: Fig. 6 Discovery of an allosteric site in the structure of CXCR3 occupied by SCH546738. a , The chemical structure of SCH546738. b , Molecular dynamics simulation of SCH546738 binding.

    Techniques: