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MedChemExpress
frax597 Frax597, supplied by MedChemExpress, used in various techniques. Bioz Stars score: 94/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more https://www.bioz.com/result/frax597/product/MedChemExpress Average 94 stars, based on 1 article reviews
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MedChemExpress
frax486 ![]() Frax486, 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 https://www.bioz.com/result/frax486/product/MedChemExpress Average 93 stars, based on 1 article reviews
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Image Search Results
Journal: International Journal of Molecular Sciences
Article Title: Inhibition of NAMPT by PAK4 Inhibitors
doi: 10.3390/ijms251810138
Figure Lengend Snippet: PAK4 inhibitors inhibit NAMPT activity in a cell-free assay. ( A , B ) NAMPT activity in response to PAK4 inhibitors (KPT-9274, PF-3758309, GNE2861, and LCH7749944), group I (PAK1-3) inhibitors (IPA-3 and FRAX486), phloretin (a natural compound unrelated to kinase inhibitors), MEK inhibitors (BI-847325 and PD0325901), the solvent control (DMSO), and FX866, the positive control. ( C , D ) Absorption (A450), reflecting NAMPT activity for PAK4 inhibitors at 0 min and 30 min. The results indicate that all PAK4 inhibitors inhibited NAMPT.
Article Snippet: PF-3758309,
Techniques: Activity Assay, Cell-Free Assay, Solvent, Control, Positive Control
Journal: International Journal of Molecular Sciences
Article Title: Inhibition of NAMPT by PAK4 Inhibitors
doi: 10.3390/ijms251810138
Figure Lengend Snippet: Structure of PAK inhibitors and control drugs. ( A ). KPT-9274, bearing a pyridine core. ( B ) PF-3758309, bearing an imidazole and a pyrazole. ( C ) Other PAK4 inhibitors (GNE-2861 and LCH-7749944) bearing pyrimidines and their benzo derivative. ( D ) FRAX486, a group I PAK inhibitor that also partially inhibits PAK4, bears an imidazole. ( E ) PAK1 inhibitor IPA-3; ( F , G ) MEK inhibitors BI-847325 and PD0325901; ( H ) NAMPT inhibitor FK866; ( I ) Phloretin, a compound without imidazole and pyrazole, unlike PAK4 inhibitors. Based on the chemical structures, the pyrimidines or benzo derivatives in PAK4 inhibitors are predicted to bind to NAMPT or PAK4. The groups that interact with NAMPT are highlighted with green circles.
Article Snippet: PF-3758309,
Techniques: Control
Journal: International Journal of Molecular Sciences
Article Title: Inhibition of NAMPT by PAK4 Inhibitors
doi: 10.3390/ijms251810138
Figure Lengend Snippet: Ligand interactions report on PAK4 drugs with PAK4 protein.
Article Snippet: PF-3758309,
Techniques:
Journal: International Journal of Molecular Sciences
Article Title: Inhibition of NAMPT by PAK4 Inhibitors
doi: 10.3390/ijms251810138
Figure Lengend Snippet: Ligand interactions report on PAK4 drugs with NAMPT protein.
Article Snippet: PF-3758309,
Techniques:
Journal: International Journal of Molecular Sciences
Article Title: Inhibition of NAMPT by PAK4 Inhibitors
doi: 10.3390/ijms251810138
Figure Lengend Snippet: The predicted interactions between different drugs and the PAK4 protein. (1) PAK4 inhibitors: ( A ) KPT-9274, ( B ) PF-3758309, ( C ) GNE-2861, and ( D ) LCH-7749944. (2) PAK1 inhibitors: ( E ) FRAX486 and ( F ) IPA-3. (3) MEK inhibitors: ( G ) BI-847325 and ( H ) PD0325901 (mirdametinib). (4) Positive control ( I ) FK866 and negative control ( J ) phloretin.
Article Snippet: PF-3758309,
Techniques: Positive Control, Negative Control
Journal: International Journal of Molecular Sciences
Article Title: Inhibition of NAMPT by PAK4 Inhibitors
doi: 10.3390/ijms251810138
Figure Lengend Snippet: The predicted interactions between different drugs and the NAMPT protein. (1) PAK4 inhibitors: ( A ) KPT-9274, ( B ) PF-3758309, ( C ) GNE-2861, and ( D ) LCH-7749944. (2) PAK1 inhibitors: ( E ) FRAX486 and ( F ) IPA-3. (3) MEK inhibitors: ( G ) BI-847325 and ( H ) PD0325901 (mirdametinib). (4) Positive control ( I ) FK866 and negative control ( J ) phloretin. The results show that PAK4 inhibitors are predicted to interact with PAK4 via pyrimidines and their benzo derivatives. The different positions of nitrogen on the benzene will affect the electrostatic interactions with an -NH bond and may lead to varying levels of NAMPT inhibition. PAK1 inhibitors (IPA-3) do not have the same groups, which may explain why they are less efficient at inhibiting NAMPT.
Article Snippet: PF-3758309,
Techniques: Positive Control, Negative Control, Inhibition