Apoptosi

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.

ZLMT-12: tacrine derivative, inhibits CDK2/CDK9, weak on AChE/BuChE, anti-proliferative, low toxicity, blocks S/G2/M phase, induces apoptosis.

TH-6, a potent HDAC inhibitor (IC50: HDAC1-0.115, 2-0.135, 3-0.242, 6-0.138, 8-2.120 μM), blocks cell migration, invasion, and has anti-tumor properties.

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

JNK-IN-19 (Compound Q8) is an inhibitor of c-Jun N-terminal kinase, utilized for the treatment and/or prevention of injuries prior to, during, or following surgery.

HER2-IN-11 is a psoralen derivative that induces apoptosis. HER2-IN-11 shows light-activated cytotoxicity and also exhibits anti-breast cancer activity [1].

SBI-0640726, an eIF4G1 inhibitor, exhibits antiproliferative activity against melanoma. It disrupts the eIF4F translation initiation complex by inhibiting the AKT and NF-kB signaling pathways. Additionally, SBI-0640726 inhibits the growth of melanoma with NRAS and BRAF mutations in vitro.

VNPP433-3β acts as a molecular glue degrader, targeting the androgen receptor (AR) and its splice variants (AR-Vs) as well as MAP kinase-interacting serine/threonine protein kinase Mnk1/2. It effectively inhibits the proliferation of cancer cells LNCaP, C4-2B, and CWR22Rv1, with GI50 values of 0.2, 0.3, and 0.31 μM, respectively. Additionally, VNPP433-3β shows favorable pharmacokinetics in CD-1 mice and suppresses tumor growth in the CWR22Rv1 xenograft mouse model.

Ac-DMLD-CMK is a peptide designed to target the caspase3-Gsdme signaling pathway in mice. It specifically inhibits the activation of caspase 3 and Gsdme, preventing the cleavage of Gsdme by caspase 3, which reduces pyroptosis. This process helps alleviate damage to renal tubular epithelial cells and decrease the secretion of inflammatory cytokines. Ac-DMLD-CMK can lower serum creatinine and blood urea nitrogen levels in mice induced by Cisplatin, thereby mitigating the progression of renal dysfunction. It holds potential for research into chemotherapy-induced nephrotoxicity.

Siphonaxanthin is a carotenoid found in green algae, known for targeting the death receptor 5 (DR5) on cancer cells to induce apoptosis. In human leukemia HL-60 cells, it increases DR5 expression, reduces Bcl-2 levels, and activates caspase-3. It also inhibits fibroblast growth factor receptor-1 (FGFR-1) signaling in endothelial cells. Siphonaxanthin suppresses the proliferation, migration, and tubular formation of human umbilical vein endothelial cells (HUVECs), as well as the growth of microvessels in rat aorta rings. Additionally, it has anti-inflammatory properties by blocking the translocation of high-affinity IgE receptors (FcεRI) to lipid rafts in mast cells. Siphonaxanthin shows potential for research into diseases such as cancer, diabetic retinopathy, and rheumatoid arthritis.

<p>eIF4E-IN-4 (Compound 33) is a selective inhibitor of the eukaryotic initiation factor 4E (eIF4E) with a biochemical activity value of 95 nM. It inhibits cap-dependent mRNA translation with an IC50 of 2.5 μM and is applicable in research on breast cancer, colon cancer, and head and neck cancer.</p>

KIRA9 inhibits IRE1 with a 4.8 μM IC50, blocking ER-stress-induced mRNA decay and apoptosis by fully binding IRE1's ATP site.

FAK-IN-4 (Compound 7d) has anticancer activities that can induce cell apoptosis. FAK-IN-4 is potential inhibitor of FAK [1].

TFCP2L1-IN-1 is a TFCP2L1 transcription factor inhibitor that regulates cell proliferation and promotes antitumor effect of Sorafenib by STAT3/NANOG pathway.

t9,t11,c15-CLNA is an isomer of conjugated linolenic acid (CLNA) produced by Lactobacillus plantarum ZS2058. It exhibits key activities including anti-inflammatory and antioxidant effects, as well as enhancement of intestinal barrier function. The regulatory mechanisms of t9,t11,c15-CLNA involve the upregulation of tight junction proteins, the inhibition of pro-inflammatory cytokines (such as TNF-α, IL-6), and the activation of antioxidant enzymes (such as SOD, CAT). t9,t11,c15-CLNA can be utilized in research on inflammatory bowel disease (like colitis).

LRRK2-IN-17 is an orally active LRRK2 inhibitor with IC50 values of 3.5 nM for WT and 3.3 nM for G2019S, and it also inhibits RET kinase with an IC50 of 59 nM. LRRK2-IN-17 is utilized in research related to cancer and Parkinson's disease (PD).

Soquelitinib (CPI-818) is a selective ITK inhibitor， inhibits tumor growth,T-cell, up-regulatCXCR3, IFNγ, TNFα, and CD107a expression in normal CD8 cells.

FGFR4-IN-7 is a covalent, reversible FGFR4 inhibitor (IC50: 0.42 μM) that blocks the FGFR4 signaling pathway, thereby inducing apoptosis.

<p>Thalidomide-NH-amido-PEG1-C2-NH2 hydrochloride is a synthetic E3 ligase ligand-linker conjugate that includes a thalidomide-based cereblon ligand and a linker, used in the synthesis of PROTAC.</p>

Akt/NF-κB/JNK-IN-1 (Compound 2i) is an inhibitor of Akt, NF-κB and JNK signalling pathways.Akt/NF-κB/JNK-IN-1 exhibits an inhibitory effect on nitric oxide