i 49

I-49 free base (Pyrido[4,3-d]pyrimidin-7(6H)-one, 2-methyl-4-[[(1R)-1-[2-methyl-3-(trifluoromethyl)phenyl]ethyl]amino]-6-(tetrahydro-2H-pyran-4-yl)-) is a novel benzylamino substituted pyridopyrimidinone as SOS1 inhibitor.

IPI-493 (17-amino17demethoxy) is a novel HSP90 inhibitor with antitumor activity.

BI-4916 is a selective phosphoglycerate dehydrogenase (PHGDH) inhibitor that inhibits SSP and reduces the migration of cancer cells.BI-4916 can be used in the study of cancer and metabolic diseases.

BI-4924 is a selective and potent inhibitor of phosphoglycerate dehydrogenase (PHGDH) (IC50=3 nM) that disrupts serine biosynthesis by intracellular trapping, and can be used in the study of diseases caused by dysfunction.

JH-VIII-49 is an effective and selective inhibitor of CDK8.

ALW-II-49-7 is a selective and potent inhibitor of EphB2 kinase, with an EC50 value of 40 nM in cell.

NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor with significant affinity for various BRD4 and BRDT isoforms, as demonstrated by its Kd values of 0.095 nM for BRD4-1, 0.32 nM for BRD4-2, 0.29 nM for BRD4-T, 0.089 nM for BRDT-1, 5.5 nM for BRDT-2, and 0.058 nM for BRDT-T. Additionally, NC-III-49-1 exhibits antiproliferative effects and reduces the expression of c-Myc [1].

Palivizumab (MEDI 493) is a humanized RSV-specific monoclonal antibody that selectively inhibits epitopes at the F protein A antigenic site of RSV subtypes A and B for the prevention of respiratory syncytial virus infection (RSV).

Dazodalibep (MEDI 4920; VIB 4920) is a monoclonal antibody that specifically targets CD40LG/TNFSF5 and is fused to human serum albumin (ALB/HSA) [1].

E10i-494 is an ionizable cationic branched endosomal disruptor (BEND) lipid utilized in the formation of lipid nanoparticles (LNPs) for mRNA delivery in vitro. These LNPs, encapsulating mCherry or luciferase mRNA, trigger the expression of mCherry or luciferase in T cells.

diABZI-i functions as an orthogonal STING inhibitor, significantly suppressing cGAMP-induced IFNβ in PBMCs with an IC50 of 49 nM. Additionally, diABZI-i activates V155M SAVI constitutive signaling in a STINGV155M THP-1 cell model, demonstrating potent agonistic activity (EC50: 17 nM). This compound is applicable in researching monogenic autoinflammatory diseases such as SAVI.

3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite originally isolated from A. candidus that has diverse biological activities, including antioxidant, antiproliferative, antibacterial, and antiviral properties.1,2,3,4 It has a 96% scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals when used at a concentration of 100 μg/ml.2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells (IC50s = 23, 36, and 32 μM, respectively), as well as methicillin-resistant S. aureus (MRSA) and V. vulnificus bacteria (MIC = 31 μg/ml for both).3 It also inhibits HIV-1 integrase in both coupled and strand transfer assays (IC50s = 2.8 and 12.1 μM, respectively).4References1. Kurobane, I., Vining, L.C., McInnes, A.G., et al. 3-Hydroxyterphenyllin, a new metabolite of Aspergillus candidus. Structure elucidation by 1H and 13C nuclear magnetic resonance spectroscopy. J. Antibiot. (Tokyo) 32(6), 559-564 (1979).2. Yen, G.-C., Chang, Y.-C., Sheu, F., et al. Isolation and characterization of antioxidant compounds from Aspergillus candidus broth filtrate. J. Agric. Food Chem. 49(3), 1426-1431 (2001).3. Wang, W., Liao, Y., Tang, C., et al. Cytotoxic and antibacterial compounds from the coral-derived fungus Aspergillus tritici SP2-8-1. Mar. Drugs 15(11), E348 (2017).4. Singh, S.B., Jayasuriya, H., Dewey, R., et al. Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites. J. Ind. Microbiol. Biotechnol. 30(12), 721-731 (2003). 3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite originally isolated from A. candidus that has diverse biological activities, including antioxidant, antiproliferative, antibacterial, and antiviral properties.1,2,3,4 It has a 96% scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals when used at a concentration of 100 μg/ml.2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells (IC50s = 23, 36, and 32 μM, respectively), as well as methicillin-resistant S. aureus (MRSA) and V. vulnificus bacteria (MIC = 31 μg/ml for both).3 It also inhibits HIV-1 integrase in both coupled and strand transfer assays (IC50s = 2.8 and 12.1 μM, respectively).4 References1. Kurobane, I., Vining, L.C., McInnes, A.G., et al. 3-Hydroxyterphenyllin, a new metabolite of Aspergillus candidus. Structure elucidation by 1H and 13C nuclear magnetic resonance spectroscopy. J. Antibiot. (Tokyo) 32(6), 559-564 (1979).2. Yen, G.-C., Chang, Y.-C., Sheu, F., et al. Isolation and characterization of antioxidant compounds from Aspergillus candidus broth filtrate. J. Agric. Food Chem. 49(3), 1426-1431 (2001).3. Wang, W., Liao, Y., Tang, C., et al. Cytotoxic and antibacterial compounds from the coral-derived fungus Aspergillus tritici SP2-8-1. Mar. Drugs 15(11), E348 (2017).4. Singh, S.B., Jayasuriya, H., Dewey, R., et al. Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites. J. Ind. Microbiol. Biotechnol. 30(12), 721-731 (2003).

Heliquinomycin is a bacterial metabolite originally isolated fromStreptomycesthat has diverse biological activities.1It is active against a variety of Gram-positive bacteria, including strains ofB. anthracis, B. subtilis, and methicillin-sensitive or -resistantS. aureus(MICs = <0.05-0.39 μg/ml). Heliquinomycin inhibits the activity of DNA helicase with a Kivalue of 6.8 μM. It reduces the growth of L1210 leukemia, B16 melanoma, and FS-3 fibrosarcoma cells (IC50s = 0.97, 0.89, and 0.83 μg/ml, respectively). 1.Chino, M., Nishikawa, K., Umekita, M., et al.Heliquinomycin, a new inhibitor of DNA helicase, produced by Streptomyces sp. MJ929-SF2 I. Taxonomy, production, isolation, physico-chemical properties and biological activitiesJ. Antibiot. (Tokyo)49(8)752-757(1996)

PI3K Inhibitor ZSTK474 is an orally available, s-triazine derivative, ATP-competitive phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity.

PSB-SB1202 (Compound 21a), a phenyl coumarin compound, acts as a CB1/CB2 agonist. It demonstrates EC50 values of 56 and 14 nM and K i values of 32 and 49 nM for CB1 and CB2 receptors, respectively [1].

HPK1-IN-49 (Compound I-4) serves as an inhibitor of Hematopoietic Progenitor Kinase 1 (HPK1), exhibiting an IC50 value greater than 100 nM.

IGF-I is partly responsible for systemic GH activities although it possesses a wide number of own properties (anabolic, antioxidant, anti-inflammatory and cytoprotective actions).IGF-I (24-41) (TFA) is amino acids 24 to 41 fragment of Insulin-like Growth