Apoptosi

PROTAC EZH2 Degrader-3 (compound ZJ-20) is a potent EZH2 degrader that exhibits strong inhibitory effects not only on EZH2 protein expression but also on the levels of other PRC2 subunits and H3k27me3 protein. Additionally, PROTAC EZH2 Degrader-3 demonstrates antiproliferative activity by blocking the cell cycle at the G0-G1 phase and inducing apoptosis (cell death). At a concentration of 5 μM and over a period of 24 hours, it effectively suppresses the expression of these critical proteins involved in cell regulation and growth.

FGFR1/VEGFR2-IN-3 (Compound 8m) acts as a dual inhibitor of FGFR1 and VEGFR2. This compound exhibits both anti-cancer cell proliferation and anti-migration activities, and it also has the capability to induce cell apoptosis (apoptosis).

IDH1/2-IN-1 (Compound 6b) is a dual inhibitor of IDH1(R132H)/IDH2(R140Q) with IC50 values of 0.22 μM and 1.6 μM, respectively. This compound effectively inhibits tumor growth by suppressing tumor cell proliferation and activating antioxidative enzymes to enhance host defense. Additionally, IDH1/2-IN-1 reduces inflammation and promotes apoptosis, demonstrating significant anti-tumor activity. It is also utilized in leukemia research.

ROS inducer 5 (compound 6e) induces intracellular ROS accumulation and subsequent nuclear fragmentation. It can provoke apoptosis in MCF-7 cells with an IC50 of 3.85 μM. ROS inducer 5 is useful for cancer research applications.

PD-L1 inhibitor IV, a polypeptide, competitively blocks hPD-1 with a Kd of 1.38 μM, preventing hPD-1/hPD-L1 interaction.

CDK2-IN-32 (Compound 5g) is a selective CDK2 inhibitor with an IC50 of 0.21 μM. It exhibits cytotoxicity towards Vero cells with an IC50 of 28.52 μM.

PRMT5-IN-45 (compound 36) is a potent and selective inhibitor of PRMT5, exhibiting an IC50 value of 3 nM. This compound effectively reduces the levels of symmetrical dimethylarginine (sDMA) and inhibits the proliferation of the MOLM-13 cell line by inducing apoptosis and causing cell cycle arrest.

EGFR-IN-131 (compound 3a) is an efficacious EGFR inhibitor capable of crossing the blood-brain barrier, with an IC50 value of 272.9 nM. This compound exhibits anti-proliferative activity, induces cellular apoptosis (apoptosis), and causes cell cycle arrest in the G0/G1 phase. Additionally, EGFR-IN-131 reduces the protein expression of p-EGFR.

Asaretoclax is an effective inhibitor of B-cell lymphoma 2 (Bcl-2), demonstrating potential for use in cancer research.

PLD-IN-1 (Compound 3r) is an orally effective inhibitor of phospholipase D (phospholipaseD) with an IC50 of 1.97 μM. It reduces the expression of CD24, CD47, and PD-L1 while enhancing the expression of calreticulin, thereby modulating the immune evasion mechanisms of lung cancer cells by promoting the phagocytosis of cancer cells by macrophages. PLD-IN-1 inhibits the viability of lung cancer cell lines A549, HCC44, H460, and HCC15 with IC50 values of 18.44, 22.31, 24.85, and 21.45 μM, respectively. It induces apoptosis (apoptosis) in A549 cells and inhibits cell migration. Additionally, PLD-IN-1 increases pro-inflammatory M1 macrophage levels and decreases anti-inflammatory M2 macrophage levels, exhibiting anti-tumor activity in mouse models.

PAR4 antagonist8 (Compound 20f) is an effective oral and selective PAR4 antagonist with an IC50 of 15.32 nM, boasting favorable pharmacokinetic properties. It effectively inhibits human platelet aggregation induced by PAR4 agonists (IC50=6.39 nM) and also suppresses platelet aggregation in mice. PAR4 antagonist8 is utilized in anti-thrombotic research.

MD-265 is a PROTAC degrader that targets and degrades MDM2, leading to the activation of p53 in cancer cells with wild-type p53. MD-265 achieves complete tumor regression and enhances long-term survival in leukemic mice.

Sarglaroids F (compound 6), an anti-inflammatory agent extracted from the roots of Grass Coral, suppresses LPS/ATP-induced IL-1β secretion by modulating K+

WKYMVm is a selective FPR2 agonist with high affinity, which was identified through screening of a synthetic peptide library.

5,10,15,20-Tetrakis(4-methoxyphenyl)porphyrin is a capable of forming complexes with metal ions and exhibit phototoxicity towards Hep-2 cells.

Acetyl tetrapeptide-2 is a skin conditioner, by soothing and nourishing the skin through similar mechanisms as other peptides.

WK369 is an innovative small molecule inhibitor of BCL6, demonstrating remarkable bioactivity against ovarian cancer by inducing cell cycle arrest and triggering apoptosis. It binds directly to the BCL6-BTB domain, obstructing the interaction between BCL6 and SMRT, which results in the reactivation of p53, ATR, and CDKN1A.

Antitumor photosensitizer-5 (Ru2) is an effective photosensitizing agent that targets tumor mitochondria, with an IC50 of 0.3 μM for phototoxicity against A549 cells. Upon exposure to 460 nm light, it induces reactive oxygen species production and NADH depletion, leading to mitochondrial damage, caspase-3 activation, apoptosis induction, and inhibition of cell migration. Antitumor photosensitizer-5 shows potential for preventing malignant tumor growth and may be applicable in photodynamic therapy.