T7871

Calcium D-saccharate tetrahydrate (Calcium D-saccharate tetrahydrate) is an oxidized non-cyclic hexose sugar. It may inhibit carcinogenesis and proliferation of cancer cells.

Dim16 HCl is a dual inhibitor of PCSK9 and HMG-CoA reductase that exhibits an IC50 value of 19 nM for PCSK9, potently blocks PCSK9–LDLR binding with an IC50 of 0.8 nM, and increases LDL uptake in HepG2 cells, supporting its use in lipid metabolism and cardiovascular research.

AMX12006, a potent and selective EP4 antagonist, exhibits cytotoxic and antitumor activity, demonstrating oral activity with an IC50 of 4.3 nM [1].

A011, a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor, exhibits an IC50 of 1.0 nM and triggers apoptosis as well as G2/M phase cell cycle arrest when combined with CPT-11, displaying notable antitumor activity [1].

DNA Gyrase-IN-8 is a potent DNA gyrase inhibitor, exhibiting antimicrobial activity with an IC50 of 8.45 µM [1].

SARS-CoV-2-IN-40 (Compound 19) is a SARS-CoV-2 inhibitor that effectively suppresses the infection of Calu3 lung cells by the BA.1 and BA.5 variants, exhibiting half-maximal inhibitory concentrations (IC50s) of 100 nM and 160 nM, respectively [1].

PptT-IN-4 (Compound 3a) is a PptT inhibitor with an IC50 of 0.71 μM, demonstrating antimycobacterial activity against Mtb H37Rv with a MIC of 42 μM. It inhibits hERG, hCav1.2, and hNav1.5 channels with IC50 values of 11 μM, 8.1 μM, and 6.9 μM, respectively [1].

MS78, an acetylation targeting chimera (AceTAC), specifically acetylates the p53Y220C mutant by recruiting the histone acetyltransferase p300/CBP. This compound enhances the expression of TRAIL apoptotic genes while concurrently suppressing DNA damage response pathways. Its structure comprises a CBP/p300 binding domain, a p53Y220C targeting moiety, and a connecting linker [1].

MKA031 (compound 6y) is a non-competitive inhibitor of macrophage migration inhibitory factor (MIF) with an IC50 of 1.7 μM. It disrupts the MIF-aryl hydrocarbon receptor interacting protein (AIF) interaction, impedes MIF nuclear translocation, and mitigates N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced cell death. MKA031 is applicable in research on chronic hepatitis C virus infection [1].

Topoisomerase Inhibitor 2 (18C) is a broad-spectrum bacterial topoisomerase inhibitor effective against multidrug-resistant Gram-negative bacteria [1].

Dim16, a dual inhibitor of PCSK9/HMG-CoAR, demonstrates potent activity with an IC50 of 19 nM against PCSK9 and significantly impedes PCSK9-LDLR interaction with an IC50 of 0.8 nM, leading to an enhanced LDL uptake in HepG2 cells [1].

SARS-CoV-2-IN-47 (Compound 13), with IC50 values of 0.77 μM against Omicron BA.1 and 0.93 μM against the Delta strain, acts as an inhibitor of SARS-CoV-2 and is used in antiviral research [1].