Apoptosis

WEHI-539 is a selective Bcl-XL inhibitor (IC50: 1.1 nM).

Samuraciclib (CT7001) is a potent oral CDK7 inhibitor (IC50: 41 nM) with anti-breast cancer properties.

RIPK2-IN-6 (Compound 15a) is an inhibitor of RIPK that specifically targets the phosphorylation of RIPK2, thereby suppressing the NF-κB and MAPK signaling pathways. It has demonstrated anti-inflammatory and anti-fibrotic activities in a mouse model of colitis induced by Dextran sodium sulfate.

ST-899 is an innovative platelet-activating factor (PAF) receptor antagonist. It significantly reduces the mortality rate in mice experiencing shock induced by endotoxins (LPS). The compound markedly inhibits the LPS-induced increase in serum tumor necrosis factor (TNF) levels while leaving interleukin-6 (IL-6) unaffected. The mechanism by which ST-899 operates involves disrupting the positive feedback loop between PAF and TNF, thereby mitigating inflammatory responses. ST-899 is applicable for studies related to inflammatory diseases such as septic shock.

sEH-IN-21 is an orally active inhibitor of sEH, exhibiting IC50 values of 0.1 nM for both hsEH and msEH. It significantly suppresses the NF-κB signaling pathway. sEH-IN-21 demonstrates potent anti-inflammatory activity by reducing IL-6 and TNF-α release and maintaining intestinal barrier integrity. It is applicable in research on inflammatory bowel disease (IBD).

SF-9-2 is a PD-L1/PD-1 binding inhibitor with an IC50 of 24.9 nM. It suppresses epithelial-mesenchymal transition, migration, invasion, and proliferation of SK-N-SH cells, while also inducing apoptosis and causing cell cycle arrest. SF-9-2 blocks PD-L1-induced growth of SK-N-SH cells via the MAPK signaling pathway. It restores GSK-3β activity and enhances PD-L1 degradation through the ubiquitin-proteasome pathway. In the SK-N-SH NOG mouse model, SF-9-2 inhibits tumor growth without notable toxicity. Additionally, SF-9-2 acts as an immune checkpoint inhibitor, blocking PD-L1 to restore T cell function and is applicable to neuroblastoma research.

PD-L1-IN-1, potent PD-L1 inhibitor with 115 nM IC50, suppresses tumors, boosts immune response, and spares healthy cells.

DC-U4106: USP8 inhibitor, Kd 4.7μM, IC50 1.2μM, degrades Erα, low-toxicity tumor suppressor for breast cancer research.

JH-XVII-10: potent, oral DYRK1A/B inhibitor (IC50: 3/5 nM), shows antitumor activity in HNSCC.

Minnelide is a prodrug of triptolide,and shows potent antitumor activity in a number of tumor types.

HAC-Y6 exerts its anticancer effects by inducing cell cycle arrest. It prompts apoptosis in COLO 205 cells with an IC50 of 0.52 µM.

PBX-7011, an active camptothecin derivative, binds to the DDX5 protein in cells and induces cell death through DDX5 protein degradation [1].

JAK2/FLT3-IN-1 (TFA), an oral JAK2/FLT3 inhibitor, shows anticancer properties; IC50: JAK2 (0.7 nM), FLT3 (4 nM), JAK1 (26 nM), JAK3 (39 nM).

Antitumor agent-43 (Compound 4B) is a potent antitumor agent that induces cell cycle arrest at G2/M phase.

Antitumor Agent-184 (compound 12aa) triggers apoptosis in various cell lines, exhibiting IC50 values of 2.35 μM in B16-F10 cells, 7.32 μM in 4T1 cells, and 10.31 μM in CT26 cells.

Compound 5f, a potent tubulin polymerization inhibitor (IC50 = 1.09 μM), blocks cell migration, tube formation, and has anti-angiogenic effects.

Compound 14 is a peptidomimetic that significantly lowers TNFα, NO, CD40, and CD86, showcasing strong anti-inflammatory effects.

eIF4A-IN-1 is an eIF4A inhibitor used in tumor research.

Casuarinin, an ellagitannin found in pomegranates and certain Casuarina/Stachyurus plants, is a carbonic anhydrase inhibitor and astringent.

LSD1/ER-IN-1 inhibits ER & LSD1 (IC50: 1.55 μM), and fights MCF-7 breast cancer (IC50: 8.79 μM).