Apoptose

SC 67655 is a peptidomimetic that specifically suppresses human leukocyte antigen DRB10401-restricted T cell proliferation.

Antitumor Agent-110 (Compound 13), an imidazotetrazine anticancer agent, exhibits excellent permeability.

Merodantoin induces apoptosis in KRAS-mutant cancer cells via ROS-autophagy and Akt pathway.

ICL-CCIC-0019 inhibits ChoKα, causes G1 arrest, ER stress, and cancer cell apoptosis.

MC2590 is a histone deacetylase (HDAC) inhibitor that inhibits HDAC1-3, -6, -8, and -10 activities, induces cell cycle arrest, and promotes apoptosis.

Artonin E, a prenylated flavonoid, induces apoptosis and S-phase arrest, disrupting the mitochondrial pathway for cancer research.

RET-IN-25 (compound 6b) is an anticancer RET kinase inhibitor that demonstrates efficacy against medullary thyroid carcinoma (MTC), exhibiting half-maximal

AAPK-25, a dual Aurora/PLK inhibitor, disrupts mitosis, induces apoptosis, and has antitumor properties.

Immunosuppressant-1 (Compound 31) suppresses T-cell proliferation triggered by anti-CD3/anti-CD28 co-stimulation and demonstrates immunosuppressive effects,

(S)-Sabutoclax ((S)-BI-97C1), an optically pure derivative of apogossypol, serves as a pan-active inhibitor of the antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins. It effectively blocks the binding of BH3 peptides to key proteins in the family, including Bcl-XL, Bcl-2, Mcl-1, and Bfl-1, displaying inhibitory concentration (IC50) values of 0.31, 0.32, 0.20, and 0.62 μM, respectively. Furthermore, (S)-Sabutoclax demonstrates potent efficacy in inhibiting the growth of various cancer cell lines, such as those from human prostate cancer, lung cancer, and lymphoma, with half-maximal effective concentration (EC50) values of 0.13, 0.56, and 0.049 μM, respectively. This compound is utilized in research focusing on apoptosis-based cancer therapies [1].

Thaspine: inhibits topoisomerase IB, reduces VEGF, stops endothelial cell growth via PI3K/MAPK pathways.

15-Deoxy-Δ12,14-Prostaglandin A1, a deoxyanalog of prostaglandins, inhibits NF-κB signaling and induces apoptosis. It also prevents TNF-α-induced upregulation of inflammatory endothelial cell adhesion molecules (CAM) and reduces monocyte arrest [1].

LSD1-IN-25: potent, selective oral LSD1 inhibitor; IC50=46 nM, Ki=30.3 nM; induces cancer cell apoptosis.

Sirt1/2-IN-2 (compound hsa55) serves as a dual inhibitor for SIRT1 with an IC50 of 1.8 μM and SIRT2 with an IC50 of 2.4 μM, respectively.

SM-433: Smac mimetic, blocks IAPs, strong XIAP BIR3 affinity (IC50 <1 μM). See patent WO2008128171A2.

eIF4A3-IN-9, a silvestrol analogue, disrupts eIF4F complex assembly; EC50s: 29/450/80 nM (myc/tub-LUC, MB-231 cells); for cancer research.

Bcl-2-IN-13 is a potent inhibitor of Bcl-2, exhibiting an IC50 of 17 nM, and holds potential for use in cancer research [1].

Mcl-1 Inhibitor 13 (Example 9), with a Ki of 8.2 nM, serves as an MCL-1 inhibitor suitable for cancer research [1].

JNJ-1013 is a selective IRAK1 PROTAC degrader with an IC50 of 72 nM ,antiproliferative and proapoptotic, increases cleaved-PARP expression.