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gsk 3β inhibitor ii  (MedChemExpress)
93
MedChemExpress gsk 3β inhibitor ii
Gsk 3β Inhibitor Ii, supplied by MedChemExpress, used in various techniques. Bioz Stars score: 93/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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Average 93 stars, based on 1 article reviews
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tlr7 8 agonists  (MedChemExpress)
92
MedChemExpress tlr7 8 agonists
Design, synthesis, and evaluation of novel <t>TLR7/8</t> agonists through HEK-Blue cell lines expressing either hTLR7 or hTLR8 receptor. (A) The design flowchart and chemical structures of novel TLR7/8 agonists with single TLR8 or dual TLR7/8 agonistic activity. Superimposition of MmTLR7-R848 cocrystal (5GMH, brown) and hTLR8-R848 cocrystal (3W3N, bottle green) was performed by Maestro software (v9.1). (B,C) Activity evaluation of TLR7/8 agonists through HEK-Blue cell lines expressing either hTLR7 (B) or hTLR8 (C) receptor, measured by the secreted embryonic alkaline phosphatase (SEAP) in the culture supernatant. Commercially available GS9620 (TLR7 agonist), VTX-2337 (TLR8 agonist), and R848 (TLR7/8 dual agonist) labeled unfilled triangle are reference compounds. (D) TLR7/8 agonists were divided into 4 categories, exhibiting the molecular structure (R1,R2,R3,R4,X refer to the functional group in A ), molecular weight (MW), cpKa, cLogP, as well as EC50 values for hTLR7 and hTLR8. Commercially available GS9620 (TLR7 agonist), VTX-2337 (TLR8 agonist), and R848 (TLR7/8 dual agonist) labeled as underlined are reference compounds.
Tlr7 8 Agonists, supplied by MedChemExpress, used in various techniques. Bioz Stars score: 92/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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Average 92 stars, based on 1 article reviews
tlr7 8 agonists - by Bioz Stars, 2026-02
92/100 stars
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Design, synthesis, and evaluation of novel TLR7/8 agonists through HEK-Blue cell lines expressing either hTLR7 or hTLR8 receptor. (A) The design flowchart and chemical structures of novel TLR7/8 agonists with single TLR8 or dual TLR7/8 agonistic activity. Superimposition of MmTLR7-R848 cocrystal (5GMH, brown) and hTLR8-R848 cocrystal (3W3N, bottle green) was performed by Maestro software (v9.1). (B,C) Activity evaluation of TLR7/8 agonists through HEK-Blue cell lines expressing either hTLR7 (B) or hTLR8 (C) receptor, measured by the secreted embryonic alkaline phosphatase (SEAP) in the culture supernatant. Commercially available GS9620 (TLR7 agonist), VTX-2337 (TLR8 agonist), and R848 (TLR7/8 dual agonist) labeled unfilled triangle are reference compounds. (D) TLR7/8 agonists were divided into 4 categories, exhibiting the molecular structure (R1,R2,R3,R4,X refer to the functional group in A ), molecular weight (MW), cpKa, cLogP, as well as EC50 values for hTLR7 and hTLR8. Commercially available GS9620 (TLR7 agonist), VTX-2337 (TLR8 agonist), and R848 (TLR7/8 dual agonist) labeled as underlined are reference compounds.

Journal: Frontiers in Microbiology

Article Title: Novel TLR7/8 agonists promote activation of HIV-1 latent reservoirs and human T and NK cells

doi: 10.3389/fmicb.2023.1033448

Figure Lengend Snippet: Design, synthesis, and evaluation of novel TLR7/8 agonists through HEK-Blue cell lines expressing either hTLR7 or hTLR8 receptor. (A) The design flowchart and chemical structures of novel TLR7/8 agonists with single TLR8 or dual TLR7/8 agonistic activity. Superimposition of MmTLR7-R848 cocrystal (5GMH, brown) and hTLR8-R848 cocrystal (3W3N, bottle green) was performed by Maestro software (v9.1). (B,C) Activity evaluation of TLR7/8 agonists through HEK-Blue cell lines expressing either hTLR7 (B) or hTLR8 (C) receptor, measured by the secreted embryonic alkaline phosphatase (SEAP) in the culture supernatant. Commercially available GS9620 (TLR7 agonist), VTX-2337 (TLR8 agonist), and R848 (TLR7/8 dual agonist) labeled unfilled triangle are reference compounds. (D) TLR7/8 agonists were divided into 4 categories, exhibiting the molecular structure (R1,R2,R3,R4,X refer to the functional group in A ), molecular weight (MW), cpKa, cLogP, as well as EC50 values for hTLR7 and hTLR8. Commercially available GS9620 (TLR7 agonist), VTX-2337 (TLR8 agonist), and R848 (TLR7/8 dual agonist) labeled as underlined are reference compounds.

Article Snippet: The TLR7/8 agonists, D018, C008, 199–1, WA86, C142, B-130a, B-130b, WA175, C163 were synthesized by Zhisong Wang in Xuebin Liao’s Lab. R848, GS9620, and VTX2337 were purchased from MedChemExpress (MCE).

Techniques: Expressing, Activity Assay, Software, Labeling, Functional Assay, Molecular Weight

TLR7/8 agonists activate latent HIV-1 and inflammatory cytokines from PBMCs of infected individuals. (A) HIV-1 RNA copies in the supernatant were measured by RT-qPCR 4 days after stimulation ( n = 6). (B–I) Concentrations of inflammatory cytokines in the culture supernatant 2 days after stimulation by TLR7/8 agonists, including IL-1β (B) , IL-6 (C) , IL-10 (D) , IL-18 (E) , IL-23 (F) , IFN-α (G) , IFN-γ (H) , and TNF-α (I) . DMSO was negative control whereas PMA plus Ionomycin were positive control. PBMC from each HIV-1 infected patient ( n = 6) with different shape was filled and PBMC from each normal control ( n = 2) with different shape was an open symbol. Data are shown as the mean of two replicates for each donor. Statistical difference between various TLR7/8 agonists and DMSO group analyzed by paired- t -test. **** p < 0.0001, *** p < 0.001, ** p < 0.01, * p < 0.05, n.s. not significant.

Journal: Frontiers in Microbiology

Article Title: Novel TLR7/8 agonists promote activation of HIV-1 latent reservoirs and human T and NK cells

doi: 10.3389/fmicb.2023.1033448

Figure Lengend Snippet: TLR7/8 agonists activate latent HIV-1 and inflammatory cytokines from PBMCs of infected individuals. (A) HIV-1 RNA copies in the supernatant were measured by RT-qPCR 4 days after stimulation ( n = 6). (B–I) Concentrations of inflammatory cytokines in the culture supernatant 2 days after stimulation by TLR7/8 agonists, including IL-1β (B) , IL-6 (C) , IL-10 (D) , IL-18 (E) , IL-23 (F) , IFN-α (G) , IFN-γ (H) , and TNF-α (I) . DMSO was negative control whereas PMA plus Ionomycin were positive control. PBMC from each HIV-1 infected patient ( n = 6) with different shape was filled and PBMC from each normal control ( n = 2) with different shape was an open symbol. Data are shown as the mean of two replicates for each donor. Statistical difference between various TLR7/8 agonists and DMSO group analyzed by paired- t -test. **** p < 0.0001, *** p < 0.001, ** p < 0.01, * p < 0.05, n.s. not significant.

Article Snippet: The TLR7/8 agonists, D018, C008, 199–1, WA86, C142, B-130a, B-130b, WA175, C163 were synthesized by Zhisong Wang in Xuebin Liao’s Lab. R848, GS9620, and VTX2337 were purchased from MedChemExpress (MCE).

Techniques: Infection, Quantitative RT-PCR, Negative Control, Positive Control, Control

TLR7/8 agonists directly activate latent HIV-1 from monocytic U1 cell line. (A) Dose–response curves for HIV-1 activation in U1 cell line by the selected novel and control TLR7/8 agonists. Data are shown as mean ± SD ( n = 4). (B,C) The p24 concentration in the supernatant of U1 cell line stimulated by D018 (TLR7/8), B-130a (TLR8), or GS9620 (TLR8) before and after (B) TLR8-shRNA silencing or (C) MyD88-shRNA silencing compared with control shRNA silencing. Data are shown as mean ± SD ( n = 4). Statistical difference between various TLR7/8 agonists was analyzed by two-way ANOVA. **** p < 0.0001, *** p < 0.001, ** p < 0.01, * p < 0.05, n.s. not significant.

Journal: Frontiers in Microbiology

Article Title: Novel TLR7/8 agonists promote activation of HIV-1 latent reservoirs and human T and NK cells

doi: 10.3389/fmicb.2023.1033448

Figure Lengend Snippet: TLR7/8 agonists directly activate latent HIV-1 from monocytic U1 cell line. (A) Dose–response curves for HIV-1 activation in U1 cell line by the selected novel and control TLR7/8 agonists. Data are shown as mean ± SD ( n = 4). (B,C) The p24 concentration in the supernatant of U1 cell line stimulated by D018 (TLR7/8), B-130a (TLR8), or GS9620 (TLR8) before and after (B) TLR8-shRNA silencing or (C) MyD88-shRNA silencing compared with control shRNA silencing. Data are shown as mean ± SD ( n = 4). Statistical difference between various TLR7/8 agonists was analyzed by two-way ANOVA. **** p < 0.0001, *** p < 0.001, ** p < 0.01, * p < 0.05, n.s. not significant.

Article Snippet: The TLR7/8 agonists, D018, C008, 199–1, WA86, C142, B-130a, B-130b, WA175, C163 were synthesized by Zhisong Wang in Xuebin Liao’s Lab. R848, GS9620, and VTX2337 were purchased from MedChemExpress (MCE).

Techniques: Activation Assay, Control, Concentration Assay, shRNA

TLR7/8 agonists indirectly activate latent HIV-1 from the J-Lat CD4 T cell line through TNF-α. (A) Dose–response curves for HIV-1 activation in J-Lat CD4 T cell line by the selected novel and control TLR7/8 agonists. The GFP+ percentage indicated the proportion of J-Lat activated. Data are shown as mean ± SD of 2 independent experiments). (B) Dose–response curves for HIV-1 activation and TNF-α release in the J-Lat and mDDC co-culture system 48 h after stimulation by D018, B130-a, GS9620, and DMSO. Data are shown as mean ± SD ( n = 4). (C) Dose–response curves for HIV-1 activation of J-Lat CD4 T cells with varying concentrations of anti-TNF-α monoclonal antibody compared with that of irrelevant IgG1 antibody control, 48 h after stimulation by D018, B130-a, GS9620, and DMSO. The GFP+ percentage indicated the proportion of J-Lat activated. Data are shown as mean ± SD ( n = 4).

Journal: Frontiers in Microbiology

Article Title: Novel TLR7/8 agonists promote activation of HIV-1 latent reservoirs and human T and NK cells

doi: 10.3389/fmicb.2023.1033448

Figure Lengend Snippet: TLR7/8 agonists indirectly activate latent HIV-1 from the J-Lat CD4 T cell line through TNF-α. (A) Dose–response curves for HIV-1 activation in J-Lat CD4 T cell line by the selected novel and control TLR7/8 agonists. The GFP+ percentage indicated the proportion of J-Lat activated. Data are shown as mean ± SD of 2 independent experiments). (B) Dose–response curves for HIV-1 activation and TNF-α release in the J-Lat and mDDC co-culture system 48 h after stimulation by D018, B130-a, GS9620, and DMSO. Data are shown as mean ± SD ( n = 4). (C) Dose–response curves for HIV-1 activation of J-Lat CD4 T cells with varying concentrations of anti-TNF-α monoclonal antibody compared with that of irrelevant IgG1 antibody control, 48 h after stimulation by D018, B130-a, GS9620, and DMSO. The GFP+ percentage indicated the proportion of J-Lat activated. Data are shown as mean ± SD ( n = 4).

Article Snippet: The TLR7/8 agonists, D018, C008, 199–1, WA86, C142, B-130a, B-130b, WA175, C163 were synthesized by Zhisong Wang in Xuebin Liao’s Lab. R848, GS9620, and VTX2337 were purchased from MedChemExpress (MCE).

Techniques: Activation Assay, Control, Co-Culture Assay

TLR7/8 agonists indirectly activate latent-infected cells derived from HIV-1 positive patients through TNF-α. (A,B) The PBMCs derived from HIV-1 viremic patients were stimulated by D018 (TLR7/8), B-130a (TLR8), GS9620 (TLR8) with anti-TNF-α monoclonal antibody compared with that of irrelevant IgG1 antibody control. (A) The HIV-1 RNA copies and (B) TNF-α concentrations in the supernatant were measured after stimulation. Data are shown as mean ± SD ( n = 7). Statistical difference was analyzed by paired t -test. **** p < 0.0001, *** p < 0.001, ** p < 0.01, * p < 0.05, n.s. not significant.

Journal: Frontiers in Microbiology

Article Title: Novel TLR7/8 agonists promote activation of HIV-1 latent reservoirs and human T and NK cells

doi: 10.3389/fmicb.2023.1033448

Figure Lengend Snippet: TLR7/8 agonists indirectly activate latent-infected cells derived from HIV-1 positive patients through TNF-α. (A,B) The PBMCs derived from HIV-1 viremic patients were stimulated by D018 (TLR7/8), B-130a (TLR8), GS9620 (TLR8) with anti-TNF-α monoclonal antibody compared with that of irrelevant IgG1 antibody control. (A) The HIV-1 RNA copies and (B) TNF-α concentrations in the supernatant were measured after stimulation. Data are shown as mean ± SD ( n = 7). Statistical difference was analyzed by paired t -test. **** p < 0.0001, *** p < 0.001, ** p < 0.01, * p < 0.05, n.s. not significant.

Article Snippet: The TLR7/8 agonists, D018, C008, 199–1, WA86, C142, B-130a, B-130b, WA175, C163 were synthesized by Zhisong Wang in Xuebin Liao’s Lab. R848, GS9620, and VTX2337 were purchased from MedChemExpress (MCE).

Techniques: Infection, Derivative Assay, Control

TLR7/8 agonists prefer to induce the NK cells and T cells activation and IFN-γ expression. (A–D) PBMCs from healthy donors were stimulated by different TLR7/8 agonists or DMSO for 24 h, and different activated markers in several immune cells were analyzed by flow cytometry. The percentage of (A) CD69 positive CD56 bright NK cells and (B) CD56 dim NK cells, (C) NKG2D positive CD56 bright NK cells, and (D) CD56 dim NK cells. (E–H) The percentage of (E) CD69 positive CD4 T cells and (F) CD8 T cells, (G) CD25 positive CD4 T cells, and (H) CD8 T cells. (I,J) The percentage of (I) CD40 positive and (J) HLA-DR positive monocytes. (K,L) The percentage of (K) CD80 positive and (L) CD86 positive dendritic cells. Each different shaped point represents one donor and data is shown as the mean of 8 donors. Statistical difference between various TLR7/8 agonists and DMSO group was analyzed by paired t -test. **** p < 0.0001, *** p < 0.001, ** p < 0.01, * p < 0.05, n.s. not significant.

Journal: Frontiers in Microbiology

Article Title: Novel TLR7/8 agonists promote activation of HIV-1 latent reservoirs and human T and NK cells

doi: 10.3389/fmicb.2023.1033448

Figure Lengend Snippet: TLR7/8 agonists prefer to induce the NK cells and T cells activation and IFN-γ expression. (A–D) PBMCs from healthy donors were stimulated by different TLR7/8 agonists or DMSO for 24 h, and different activated markers in several immune cells were analyzed by flow cytometry. The percentage of (A) CD69 positive CD56 bright NK cells and (B) CD56 dim NK cells, (C) NKG2D positive CD56 bright NK cells, and (D) CD56 dim NK cells. (E–H) The percentage of (E) CD69 positive CD4 T cells and (F) CD8 T cells, (G) CD25 positive CD4 T cells, and (H) CD8 T cells. (I,J) The percentage of (I) CD40 positive and (J) HLA-DR positive monocytes. (K,L) The percentage of (K) CD80 positive and (L) CD86 positive dendritic cells. Each different shaped point represents one donor and data is shown as the mean of 8 donors. Statistical difference between various TLR7/8 agonists and DMSO group was analyzed by paired t -test. **** p < 0.0001, *** p < 0.001, ** p < 0.01, * p < 0.05, n.s. not significant.

Article Snippet: The TLR7/8 agonists, D018, C008, 199–1, WA86, C142, B-130a, B-130b, WA175, C163 were synthesized by Zhisong Wang in Xuebin Liao’s Lab. R848, GS9620, and VTX2337 were purchased from MedChemExpress (MCE).

Techniques: Activation Assay, Expressing, Flow Cytometry

The mechanism diagram of TLR7/8 agonists activating HIV latent reservoirs.

Journal: Frontiers in Microbiology

Article Title: Novel TLR7/8 agonists promote activation of HIV-1 latent reservoirs and human T and NK cells

doi: 10.3389/fmicb.2023.1033448

Figure Lengend Snippet: The mechanism diagram of TLR7/8 agonists activating HIV latent reservoirs.

Article Snippet: The TLR7/8 agonists, D018, C008, 199–1, WA86, C142, B-130a, B-130b, WA175, C163 were synthesized by Zhisong Wang in Xuebin Liao’s Lab. R848, GS9620, and VTX2337 were purchased from MedChemExpress (MCE).

Techniques: