Apoptose

8-hydroxy Efavirenz, a main efavirenz metabolite by CYP2B6, causes apoptosis in rat neurons at 0.01 μM.

Apoptosis Inducer 13 (Compound Ru4) promotes apoptosis in cancer cells while also suppressing their migration and invasion.

2,5-Dimethylcyclohexa-2,5-diene-1,4-dione inhibits the viability of HL60 and K562 cells and exhibits antibacterial and anticancer properties.

ZC0109 inhibits IDO1 (50 nM) & TrxR1 (3.0 μM), induces ROS, arrests G1/S phase, causing cancer cell apoptosis.

EGFR/BRAFV600E-IN-3 is an inhibitor targeting EGFR, BRAFV600E, and EGFRT790M with IC50 values of 57 nM, 68 nM, and 9.70 nM, respectively.

U7D-1: First-class USP7 PROTAC degrader, DC50 33 nM, anticancer, induces apoptosis in Jeko-1.

A947 is a potent and selective SMARCA2 PROTAC that induces the degradation of SMARCA2, with significant antitumor activity in SMARCA4-mutant NSCLC cells.

VEGFR/PARP-IN-1 (Compound 14b) is a dual inhibitor of VEGFR and PARP with IC50 values of 191 nM and 60.9 nM, respectively.

Hexapeptide-11 is a novel proteostasis network modulator in human diploid fibroblasts.

Halenaquinone: PI3K inhibitor, stops RAD51 DNA binding & osteoclastogenesis, induces PC12 cell apoptosis.

Cell-permeable CaM agonist; activates phosphodiesterase, binds to Ca2+ channels, inhibits cytotoxicity (IC50=52μM), protects cells, reduces inflammation.

F1324: potent BCL6 inhibitor, IC50=1nM, binding t1/2=441s, strongly inhibits BCL6 PPI.

7-epi-Isogarcinol, a PPAP, hinders STAT3 to induce apoptosis and curbs cell migration with moderate antiproliferative effects.

Nauclefine, a plant alkaloid, triggers cancer cell death through PDE3A-SLFN12, binding but not inhibiting PDE3A.

BRD4 Inhibitor-38 (Compound 25) is an orally active BRD4 inhibitor, exhibiting IC50 values of 3.64 μM for BRD4 BD1 and 0.12 μM for BRD4 BD2. It also demonstrates anti-inflammatory properties, with an IC50 value of 1.98 μM for nitric oxide (NO) production.

HDSI-18 is an orally active selective inhibitor of HDAC6 with an IC50 of 1.6 nM. It exhibits cytotoxic effects against K562, MV4-11, MOLM-13, THP-1, and Jurkat cells with IC50 values of 0.48, 0.58, 0.91, 1.79, and 4.31 μM, respectively. HDSI-18 can activate Caspase-3, induce mitochondrial depolarization, and trigger apoptosis (Apoptosis), demonstrating antitumor activity.

PD-L1/LpxC-IN-1 (Compound 12b) is an inhibitor of PD-L1 and LpxC, with IC50 values of 5.2 μM and 0.081 μM, respectively. This compound disrupts bacterial lipopolysaccharide biosynthesis, leading to bacterial cell lysis and death. It effectively inhibits Gram-negative bacteria, exhibiting a minimum inhibitory concentration (MIC) of 0.25-0.5 μg/mL against K. pneumoniae ATCC 13883, E. coli ATCC 8739, S. typhimurium ATCC 14028, and P. aeruginosa ATCC 9027. Additionally, PD-L1/LpxC-IN-1 modulates the immune response by downregulating the expression of inflammatory cytokines IL-2 and IFN-γ, and upregulating CD4+ and CD8+ cells, thus activating the immune system and mitigating excessive inflammatory responses. In a mouse model of K. pneumoniae ATCC 13883 infection, PD-L1/LpxC-IN-1 demonstrated antibacterial activity.

Thalidomide-O-C8-Boc: CRBN ligand for PROTAC creation, derived from Thalidomide.