Apoptosis

Trichostatin C, a natural glycosylated hydroxamate, is a histone deacetylase inhibitor with antifungal properties and can induce cell differentiation.

MS41 is a selective eleven-nineteen leukemia (ENL) PROTAC degrader, with DC50s values of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1). This compound effectively inhibits the growth of ENL-dependent leukemia cells, induces G1 cell cycle arrest, and increases cellular apoptosis (Apoptosis). Additionally, MS41 reduces chromatin occupancy related to ENL-mediated transcription elongation mechanisms and suppresses the expression of oncogenes and the progression of leukemia.

<p>Opamtistomig is a humanized monoclonal antibody immunoglobulin (H-γ1-scFv-L-κ) dimer targeting human programmed death-ligand 1 (PD-L1), CD274, and tumor necrosis factor receptor superfamily member 9 (TNFRSF9). It is anticipated for use in research on various solid tumors and hematologic malignancies.</p>

KB02-SLF, a molecular glue, degrades nuclear FKBP12 by modifying E3 ligase DCAF16 and extends protein degradation.

<p>QZ2135 (compound 20) is a PROTAC degrader that specifically targets RET and exhibits antitumor activity in vivo within a Ba/F3-KIF5B-RET-G810C xenograft mouse model. The compound demonstrates degradation activity with DC50 values of 4.7 nM (WT), 17.2 nM (V804M), and 73.8 nM (G810C) when targeting KIF5B-RET. QZ2135 is composed of the target protein ligand (red part) RETligand-3, the E3 ligase ligand (blue part) Lenalidomide-F, and the PROTAC Linker (black part) 7-Iodohept-1-yne, wherein the target protein ligand combined with the linker forms the conjugate RETLigand-Linker Conjugate-1.</p>

SBP-0636457: SMAC mimetic, IAP inhibitor, binds BIR-domains (Ki=0.27μM), potential in tumor/cancer research.

NA-Ir is a ferroptosis (Ferroptosis) inducer that targets mitochondrial DNA (mtDNA) and activates the cGAS-STING pathway to stimulate ferritin autophagy (). It also induces the production of reactive oxygen species (ROS) through photodynamic therapy (PDT), depletes glutathione (GSH), and downregulates glutathione peroxidase 4 (GPX4), thereby triggering lipid peroxidation and ferroptosis. NA-Ir exhibits enhanced anticancer activity under light exposure and selectively inhibits cancer cells with high H2S content.

PARP1/BRD4-IN-3 (compound HF4) is an effective inhibitor of BRD4 and PARP1, with IC50 values of 1210 nM and 2019 nM respectively. The compound exhibits antiproliferative activity, induces apoptosis (apoptosis) and cell cycle arrest at the G0/G1 phase. Additionally, PARP1/BRD4-IN-3 causes DNA damage and reduces the expression of the Rad51 protein, demonstrating anti-tumor activity.

Zigakibart (BION-1301) is a humanized monoclonal antibody targeting TNFSF13 with anti-inflammatory activity for the study of immunoglobulin A nephropathy (IgAN)

FAK-IN-24 (Compound 9f) is a potent FAK inhibitor with an IC50 of 0.815 nM. It induces DNA damage and apoptosis, and exhibits activity against glioblastoma. FAK-IN-24 effectively inhibits proliferation of glioblastoma cell lines U87-MG (IC50= 15 nM) and U251 (IC50= 20 nM), and suppresses tumor growth in U87-MG xenograft models.

L-threo-PPMP blocks GlcT, curbs glycosphingolipid creation, and triggers cell death, showing anti-cancer effects.

ARD-61: potent PROTAC, degrades AR/PR in AR+ cancers, triggers apoptosis, inhibits tumor growth in mice.

YF135 is a reversible-covalent KRAS G12C PROTAC that degrades its target via the VHL-proteasome pathway.

Compound 24a, an FPR1 antagonist, demonstrates potent inhibition of the formyl peptide receptor 1 (FPR1) with an IC50 value of 25 nM.

Tubulin/AKT1-IN-1 (Compound D1-1) serves as an inhibitor of both tubulin polymerization and AKT pathway activation, effectively suppressing proliferation and

Tebentafusp (IMCgp100) is a protein that targets gp100 with potential anti-tumor activity.

STAT3-D11-PROTAC-VHL (Compound D11-PROTAC) is a PROTAC degrader targeting signal transducer and activator of transcription 3 (STAT3). It demonstrates anti-tumor activity with IC50 values of 1335 nM in HeLa cells and 1973 nM in MCF-7 cells. The compound binds to the DNA binding domain of STAT3, recruits the E3 ligase VHL to form a ternary complex, leading to ubiquitination and subsequent proteasomal degradation of STAT3. Additionally, STAT3-D11-PROTAC-VHL inhibits tumor cell growth, induces cell cycle arrest and apoptosis (apoptosis), and suppresses tumor immune evasion.

<p>Sincalide ammonium, a CCK analog, stimulates bile release, gallbladder contraction, and sphincter relaxation, aiding in diagnoses.</p>

Irofulven is an agent of DNA-damaging and antitumor. It is used for the treatment of advanced solid tumors, including prostate, ovarian, and pancreatic cancers.

Topoisomerase II inhibitor 14: powerful anticancer agent that induces apoptosis, halts S phase, and lowers GSH, MDA, and NO levels.