cell cycle arrest

CAM 833 is an effective orthosteric inhibitor of the BRCA2-RAD51 interaction, inhibiting RAD51 aggregation, enhancing DNA damage-induced apoptosis, increasing 4N cell cycle arrest, and disrupting homologous DNA repair (HDR), and can be used for cancer therapy.

Ginsenoside C-K (Ginsenoside K) is a bacterial metabolite of G-Rb1 exhibiting anti-inflammatory effects by reducing iNOS and COX-2.

Imofinostat (MPT0E028) is a selective, orally available pan-HDAC inhibitor with IC₅₀ values of 53.0/106.2/29.5 nM against HDAC1/HDAC2/HDAC6 in HCT116 cells. In B-cell lymphoma, Imofinostat induces cell cycle arrest and apoptosis whilst inhibiting Akt phosphorylation, demonstrating anticancer activity across multiple tumour types.

2-O-β-D-Glucopyranosyl-L-ascorbic acid (AA-2βG) is a natural and stable vitamin C analog that induces apoptosis and cell cycle arrest in cancer cells by stabilizing p53 protein.

Trilaciclib is a short-acting, orally effective CDK4/6 inhibitor with IC₅₀ values of 1 nM and 4 nM respectively. It transiently and reversibly induces G1 cell cycle arrest, mitigates chemotherapy-induced myelosuppression, and enhances antitumour immunity, making it applicable across multiple cancers.

Devazepide is a competitive, selective, orally available non-peptide CCK1 (cholecystokinin 1) receptor antagonist that inhibits bladder cancer cell proliferation and migration while inducing apoptosis and cell cycle arrest.

Tubulin inhibitor 49 (Compound 18) is a tubulin polymerization inhibitor (IC50 = 48 μM) that disrupts the cellular microtubule network, arresting the cell cycle at G2 phase. It exhibits toxicity toward HeLa cells (IC50 = 8.8 μM).

Kaempferitrin (Lespenephryl) has antidepressant-like effect related to the serotonergic system, principally 5-HT1A. Kaempferitrin exerts cytotoxic and antitumor effects against HeLa cells. Kaempferitrin stimulates glucose-metabolizing enzymes, promotes glucose homeostasis. Kaempferitrin exerts immunostimulatory effects on immune responses mediated by splenocytes, macrophages, PBMC and NK cells. Kaempferitrin induces cytotoxic effects to include: cell cycle arrest in G1 phase and apoptosis via the intrinsic pathway in a caspase-dependent pathway.

PRLX-93936 is a selective Ras pathway protein inhibitor that modulates RAS/JNK pathway-associated protein phosphorylation, induces caspase-dependent apoptosis and cell cycle arrest, and exhibits anticancer activity.

Gracillin can induce cell cycle arrest, oxidative stress, and apoptosis in HL60 cells, and has the potential to be developed as an antitumor agent. Gracillin can be selected as lead compounds for the development of new drugs against I. multifiliis.

KS15 is a cryptochrome (CRY) inhibitor that promotes G1 cell cycle arrest, enhances drug sensitivity in MCF-7 cells, and exhibits antitumour activity against human breast cancer cells.

4-Oxofenretinide (3-Keto fenretinide) , a recently identified fenretinide metabolite, induces marked G2-M cell cycle arrest and apoptosis.

PI-103 Hydrochloride is a dual PI3K/Akt and mTOR inhibitor exhibiting nM-level inhibition of p110α, p110β, p110δ, p110γ, DNA-PK, mTORC1, and mTORC2. PI-103 induces autophagy, mitochondrial apoptosis, and cell cycle arrest, making it suitable for leukaemia research.

PLK1-IN-4 (compound 31) is a selective PLK1 inhibitor (IC50 < 0.51 nM) exhibiting antiproliferative activity against multiple cancer cell lines including A549, HT-29, and HCT-116. It induces cell cycle arrest and apoptosis, making it suitable for hepatocellular carcinoma research.

S)-(-)-Perillic acid is a terpenoid natural product capable of inhibiting protein pentosylisation and protein acylation. It exhibits anti-infective and anti-cancer activity, inducing cell cycle arrest and apoptosis in non-small cell lung cancer cells while increasing intracellular protein levels of Bax, p21, and caspase-3.

TH9619 is an effective inhibitor of both dehydrogenase and cyclohydrolase activities in MTHFD1 and MTHFD2 (IC50=47 nM). It induces folate trapping and cell cycle arrest, thereby selectively killing cancer cells expressing MTHFD2.

Schinifoline is a quinolone derivative extracted from Zanthoxylum schinifolium Sieb with cytotoxic activity that promotes radiosensitization of cancer cells, affects the cell cycle and apoptosis.

Glychionide A is a flavonoid glycoside discovered in Glycyrrhiza glabra that exhibits antitumor activity against PANC-1 cells by inducing autophagy, apoptosis, cell cycle arrest, and disruption of mitochondrial membrane potential.

Gypenoside LI is a natural product with anticancer activity that generates ROS, downregulates procaspase-8 and MMP-2/9, inhibits Wnt/β-catenin signaling, and induces cell cycle arrest and apoptosis.

Ribociclib hydrochloride (LEE011 HCl) is a selective, orally active cyclin-dependent kinase CDK4/6 inhibitor (IC50=10/39 nM) that blocks cell cycle progression and inhibits tumor cell proliferation.

YL-5092 is a YTHDC1 inhibitor (IC50=7.4 nM, KD=29.6 nM) that suppresses cancer cell proliferation, induces G0/G1 phase arrest and apoptosis, and can be used in studies of acute myeloid leukemia (AML).

MYF-03-69 (TEAD-IN-3) is a covalent and irreversible pan-TEAD inhibitor with IC₅₀ values of 385/143/558/173 nM for TEAD1/TEAD2/TEAD3/TEAD4, respectively. MYF-03-69 inhibits TEAD transcriptional activity (IC₅₀ = 56 nM), upregulates the pro-apoptotic gene BMF, and suppresses mesothelioma cancer cells with defective Hippo signaling, making it suitable for malignant pleural mesothelioma (MPM).

Picrasidine Q is an anticancer natural alkaloid that targets FGFR2, inducing apoptosis and G1 arrest in oesophageal squamous cell carcinoma (ESCC) cells.

S-trityl-L-Cysteine is a non-natural amino acid and an inhibitor of Eg5, also known as KSP and Kif11, a mitotic kinesin necessary for mitotic spindle formation. S-trityl-L-Cysteine inhibits the ATPase activity of Eg5 in basal and microtubule-stimulated states (IC50s = 1,000 and 140 nM, respectively). It is selective for Eg5 over nine other human kinesins in an enzyme-coupled assay. It reversibly inhibits Eg5-driven microtubule sliding velocity with an IC50 value of 500 nM using X. laevis recombinant Eg5. It induces cell cycle arrest in HeLa cells (IC50 = 700 nM), reversibly halting the cell cycle in the mitotic phase by inhibiting the separation of duplicated chromosomes and preventing bipolar spindle formation. S-trityl-L-Cysteine inhibits the growth of cancer cells in vitro when tested against the National Cancer Institute (NCI) 60 human cancer cell line panel (average GI50 = 1.3 μM) and in mouse xenograft models.