various tumor cells

(20S)-Protopanaxadiol (20-Epiprotopanaxadiol) (20-Epiprotopanaxadiol), an apoptosis inducer, is an aglycon metabolic derivative of the protopanaxadiol-type ginseng saponin.

Cyclophosphamide is an alkylating agent type of anti-tumor drug, and its main target is DNA. Cyclophosphamide inhibits the proliferation of tumor cells by undergoing alkylation reactions with DNA, interfering with the replication and transcription processes of DNA.

(S)-Coriolic acid (13(S)-HODE) is an important intracellular signaling agent generated by the reaction of linoleic acid with plant and mammalian lipoxygenases. It is involved in cell proliferation and differentiation in various biological systems and inhibits the adhesion of tumor cells to the vascular endothelium, while down-regulating IRGpIIb/IIIa receptor expression at around 1 μM. Additionally, (S)-Coriolic acid is a metabolite of 15-lipoxygenase (15-LOX) and often acts as an endogenous ligand to activate PPARγ. It induces mitochondrial dysfunction and airway epithelial damage.

GDC-0425 (RG-7602) is a potent and highly selective inhibitor of Checkpoint kinase 1 (Chk1). This product blocks DNA damage-induced cell cycle arrest by inhibiting Chk1 activity, forcing damaged cells into mitosis and ultimately leading to apoptosis. Research indicates that the activity of GDC-0425 is modulated by the Ras-MEK signaling pathway, and it significantly enhances tumor regression when combined with DNA-damaging agents like Gemcitabine.

Geranylgeraniol (FT0626663) is an isoprenoid found in fruits, vegetables, and grains, including rice. Geranylgeraniol (FT0626663) inhibits growth and induces apoptosis of various tumor cells. Geranylgeraniol (FT0626663) protects monocytes against statin-induced cytotoxicity and suppresses the growth of Mycobacterium.

Okadaic acid is a potent polyether marine toxin that primarily accumulates in the digestive glands of marine mollusks. It is a highly effective and selective inhibitor of protein phosphatases (PPs). By inhibiting these phosphatases, okadaic acid increases the phosphorylation levels of various proteins, acts as a tumor promoter, and induces tau protein phosphorylation. It can be used to establish models of Alzheimer’s disease and skin cancer.

ER-076349 is a microtubule polymerization inhibitor that induces G2-M cell cycle arrest and disrupts mitotic spindles. This compound inhibits the growth of cancer cells and suppresses tumor growth in various human tumor xenograft mouse models. Additionally, ER-076349 is an analog of Halichondrin B.

SC428 acts as an inhibitor of the androgen receptor (AR), specifically targeting the N-terminal domain of AR. This compound effectively diminishes the transactivation of various AR forms, including AR-V7, ARv567es, full-length AR (AR-FL), and its LBD mutants. Additionally, SC428 significantly inhibits AR-FL nuclear translocation, chromatin binding, and AR-regulated gene transcription under androgen stimulation. In vitro, SC428 suppresses the proliferation of tumor cells. In vivo, it inhibits tumor growth in mice transplanted with 22Rv1 cells by inducing apoptosis.

DPP-21 is an inhibitor of microtubule protein polymerization (IC50: 2.4 μM). It exhibits antiproliferative activity against various cancer cell lines, with IC50 values of 0.38 nM (HCT116), 11.69 nM (B16), 5.37 nM (HeLa), 9.53 nM (MCF7), 8.94 nM (H23), and 9.37 nM (HepG2). DPP-21 induces cell cycle arrest at the G2/M phase of mitosis and subsequently triggers apoptosis in tumor cells by decreasing Bcl-2 while increasing pro-apoptotic protein Bax levels.

1-Stearoyl-sn-glycerol 3-phosphate sodium, a biologically active phospholipid, plays a crucial role in regulating cell motility, proliferation, invasion, survival, and the production of growth factors through interactions with G protein-coupled receptors (GPCR). Synthesized during the formation of membrane phospholipids, this compound typically has a low plasma concentration (approximately 100nM) and originates from various cell types, including activated platelets, epithelial cells, leukocytes, neuronal cells, and tumor cells. Its distinctive structure features stearic acid at the sn-1 position and a hydroxyl group at the sn-2 position.

PF-477736, also known as PF-00477736, is a potent CHK1 inhibitor with potential to enhance chemotherapy. This compound inhibits CHK1, an ATP-dependent serine/threonine kinase that is a crucial component of the S/G2 checkpoint system for DNA replication monitoring. By bypassing the final checkpoint defenses against DNA damage-induced lethal effects, PF-477736 may improve the antitumor efficacy of various chemotherapeutic agents in tumor cells with inherent checkpoint deficiencies.

NR-11c is a selective and potent p38α PROTAC degrader. It effectively degrades p38α in various tumor cells. When administered to mice via intraperitoneal or tail vein injection, NR-11c primarily acts in the liver. It is used for cancer research.

p53 Activator 14 (Compound 7A) is a derivative of Neratinib that can induce DNA damage and activate p53, thereby inhibiting the proliferation of various cancer cells, with an IC50 of 7.21 μM for HCT116 cells. This compound hinders adhesion, migration, and invasion of HCT116 cells, disrupts the cell cycle, and triggers apoptosis. In addition, p53 Activator 14 exhibits anti-tumor properties and inhibits angiogenesis in the chick embryo chorioallantoic membrane (CAM) model.

p38-α MAPK-IN-8 (Compound 13) is a lipophilic cationic derivative. It exhibits cytotoxicity toward various tumor cells, inducing cell cycle arrest and apoptosis, as well as increasing reactive oxygen species (ROS) production and causing mitochondrial membrane potential depolarization. Its antitumor activity may be related to the p38α MAPK pathway, making it a potential candidate for cancer research.

KRAS inhibitor-40 (Compound 41) is an inhibitor of KRAS, disrupting the KRAS G12C-BRAF complex and suppressing the phosphorylation of the downstream ERK signaling pathway. This compound also inhibits the proliferation of tumor cells with various KRAS mutations, exhibiting antitumor activity.

CD13-IN-1 (Compound 5f) is a CD13 inhibitor with an IC50 value of 1.71 μM. It effectively suppresses the proliferation of various tumor cells, demonstrating antitumor activity.

Antitumor agent-199 (Compound 4b) is an antitumor compound exhibiting significant antiproliferative activity against various tumor cell lines. It can induce autophagy (autophagy) in cancer cells through the ATG5/ATG7 pathway, making it useful for tumor research.

Aurora kinase inhibitor-14 (Compound 79) is an orally active and highly selective inhibitor of Aurora kinases, effectively inhibiting both Aurora A and Aurora B with IC50 values of 0.5 nM and 1.2 nM, respectively. It binds to the ATP binding site of Aurora kinases, blocking chromosome separation during mitosis and inducing apoptosis in tumor cells. Aurora kinase inhibitor-14 shows potential for research in various solid tumors and hematologic malignancies, such as non-small cell lung cancer, breast cancer, and acute myeloid leukemia.

DDO-6691 is an inhibitor of heat shock protein 90 (HSP90). It exhibits antiproliferative effects against various tumor cells, with the highest sensitivity observed in HCT-116 colon cancer cells (IC50: 1.08 μM). DDO-6691 also demonstrates potent tumor growth inhibition in HCT-116 xenograft mouse models.

PI3K/HDAC-IN-4 (Compound 31f) is a dual inhibitor targeting PI3K and HDAC, with an IC50 of 0.2μM. It demonstrates high selectivity for HDAC1-3, with IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively. As a potent pan-PI3K inhibitor, PI3K/HDAC-IN-4 has IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. This compound effectively induces apoptosis in tumor cells by concurrently inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. It shows significant antiproliferative activity across various tumor cell lines, such as MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively. PI3K/HDAC-IN-4 is applicable in the study of lymphoma and leukemia.

Anticanceragent 201 (Compound 2f) exhibits IC50 values in the low micromolar range across various tumor cell lines. It demonstrates high in vitro cytotoxicity against CCRF-CEM cells by inducing apoptosis through the activation of caspase-3 in the mitochondrial intrinsic pathway, cleavage of PARP, and reduced expression of Bcl-2 and Bcl-XL proteins. Anticanceragent 201 can be utilized in cancer research.

Elomotecan TFA is a potent inhibitor of topoisomerases I and II. As a camptothecin analogue belonging to the homocamptothecin family (hCPT), Elomotecan TFA demonstrates superior efficacy in reducing the proliferation of various tumor cells compared to other reference anticancer molecules targeting topoisomerases I and II.

PRMT5-MTA-IN-4 (Compound 30) is a potent irreversible inhibitor of protein arginine methyltransferase 5 (PRMT5) with an IC50 of 8 nM. It obstructs arginine methylation, hinders ribosomal RNA processing, and suppresses cell cycle-related protein expression. This compound shows antiproliferative activity in various tumor cell lines, exemplified by an IC50 of 0.3 μM in DLD-1 cells. PRMT5-MTA-IN-4 holds potential for research into hematological malignancies such as acute myeloid leukemia and diffuse large B-cell lymphoma.

HER2-IN-22 is a potent and selective HER2 inhibitor with an IC50 value of 215 μM. It exhibits cytotoxic activity against various tumor cells and can induce apoptosis. HER2-IN-22 significantly suppresses tumor growth in mice and can be utilized for research in HER2+ breast cancer and other tumors.