anticancer activity

Procarbazine hydrochloride (NSC-77213 HCl) is the hydrochloride salt of a methylhydrazine derivative with antineoplastic and mutagenic activities. Although the exact mode of cytotoxicity has not been elucidated, procarbazine, after metabolic activation, appears to inhibit the trans-methylation of methionine into transfer RNA (t-RNA), thereby preventing protein synthesis and consequently DNA and RNA synthesis. This agent may also undergo auto-oxidation, resulting in the formation of cytotoxic free radicals which damage DNA through an alkylation reaction.

Paeoniflorin (Peoniflorin) is a herbal constituent extracted from the root of Paeonia albiflora Pall.

HNHA is an inhibitor of HDAC.

Panaxadiol (20(R)-Panaxadiol) is a novel antitumor agent extracted from the Chinese medicinal herb Panax ginseng.

Trastuzumab deruxtecan (T-DXd) is an antibody-drug conjugate functioning as a HER2-targeted topoisomerase I inhibitor, with targeting capability and antitumor activity, employed in research on HER2-positive breast cancer and gastric cancer.

Ponsegromab (PF 06946860) is a selective and potent humanized anti-GDF15 antibody inhibitor with IC₅₀ values of 0.123 nM, 0.053 nM, and 0.102 nM for human, rhesus macaque, and mouse targets, respectively. Ponsegromab exhibits anti-cachexia activity by binding to GDF15 to prevent its interaction with GFRAL, thereby disrupting GDF15/GFRAL-mediated signaling. Ponsegromab possesses potential anticancer activity and may be used to treat cancer patients with cancer anorexia-cachexia syndrome. Ponsegromab acts as a chemopreparative agent, increasing intracellular reactive oxygen species levels and reducing glutathione levels.

Sacituzumab govitecan (IMMU-132) is a humanized ADC compound targeting Trop-2 with anticancer activity for the study of refractory, locally advanced or metastatic breast cancer and uroepithelial cancer.

RMC-7977 is a highly selective inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS with anticancer activity for the study of solid tumors with KRAS G12C mutations.

Simvastatin (MK 733) is an HMG-CoA reductase inhibitor (Ki=0.2 nM) with oral activity. Simvastatin has hypolipidemic activity, inhibits hepatic production of cholesterol, and is also used for the prevention of cardiovascular disease.

Cerivastatin sodium (BAY W 6228 sodium) is an orally active and highly potent HMG-CoA reductase inhibitor with lipid-lowering activity that can reduce low-density lipoprotein cholesterol levels. Cerivastatin sodium has anticancer effects and can be used to study primary hyperlipidemia.

EMD-503982 is an orally active, direct factor Xa (FXa) inhibitor that also exhibits inhibitory activity against factor VIIa, and has potential antithrombotic, anticancer, and neuroprotective effects. EMD-503982 can be used in research on thrombotic diseases.

Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis/erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.

CBL0137 hydrochloride (Curaxin-137 hydrochloride) is an inhibitor of the histone chaperone FACT, which also activates p53 and inhibits NF-κB with EC50 values ​​of 0.37 and 0.47 μM, respectively. CBL0137 hydrochloride functionally inactivates the complex that promotes chromatin transcription (FACT), thereby driving effects on p53 and NF-κB and promoting cancer cell death, and when used in combination with cisplatin, CBL0137 hydrochloride has potent anticancer activity against SCLC.

KDM4-IN-4 is a histone lysine demethylase 4 (KDM4) inhibitor that primarily targets the Tudor domain of KDM4A and exhibits anticancer activity. KDM4-IN-4 has an affinity for the KDM4A Tudor domain of approximately 80 μM. KDM4-IN-4 inhibits the binding of H3K4Me3 to the Tudor domain in cells, with an EC50 of 105 μM. KDM4-IN-4 can be used in cancer research.

Selvigaltin (GB1211) is an orally administered, highly selective small-molecule inhibitor of galectin-3 (Gal-3) with an IC₅₀ value of 12 nM in rabbits, exhibiting anticancer and anti-fibrotic activity. Selvigaltin reduces galectin-3 levels in the liver and decreases biomarkers of inflammation (cellular foci) and fibrosis (PSR, SHG), while simultaneously lowering the mRNA and protein expression of inflammatory and fibrotic biomarkers (IL-6, TGF-β3, SNAI2, collagen). Selvigaltin also restores T-cell activity and reduces tumor growth and metastasis. Selvigaltin is suitable for use in studies of liver fibrosis, non-alcoholic steatohepatitis (NASH), and tumors.

Zavondemstat (QC8222) is an orally active, selective inhibitor of the histone lysine demethylase 4 (KDM4) family, with an IC₅₀ of ≤ 0.08 μM against human KDM4A–D and a K₊₀ of 0.52 μM against human KDM4C. Zavondemstat activates tumor suppressor genes, induces apoptosis, causes S-phase cell cycle arrest, and inhibits cancer cell proliferation. In in vivo studies, Zavondemstat inhibits tumor growth and induces tumor regression. Zavondemstat can be used in cancer research.

Plogosertib (CYC140) is an orally active, selective, potent, and ATP-competitive PLK1 inhibitor with an IC50 value of 3 nM.Plogosertib exhibits antiproliferative and anticancer activity and can be used for the study of solid and hematologic tumors. and hematologic tumors.

H3B-8800 is a small-molecule inhibitor and an SF3B1-targeted inhibitor with oral bioactivity and cell permeability. This compound directly binds to the SF3b complex, exhibiting anticancer activity in transfusion-dependent myelodysplastic syndromes and SF3B1-mutant acute myeloid leukemia.

STC-15 is an orally active and potent METTL3 inhibitor with anticancer activity that inhibits cancer growth and induces anticancer immunity.

STX-478 is an orally active and selective PI3Kα inhibitor that penetrates the blood-brain barrier and has anticancer activity to inhibit tumor growth.STX-478 is indicated for the study of breast cancer and other cancers.

D-F07 belongs to fluorescent dye-class tricyclic chromone compounds and is an IRE1 inhibitor (prodrug form containing an aldehyde-masked group) with cell permeability. This compound induces tumor cell apoptosis through inhibition of the IRE1/XBP1 pathway, exhibiting significant antitumor activity, and is suitable for related mechanism research and antitumor drug development.

Calderasib (MK-1084) is a selective KRAS G12C inhibitor with an IC50 value of 1.2 nM . Calderasib (MK-1084) exhibits significant anticancer activity, and it can be employed either as a monotherapy or in combination with the PD-1 inhibitor Pembrolizumab, providing a versatile approach for the investigation of KRAS-mutant driven cancers.

Wighteone (Erythrinin B) is a small molecule compound derived from Genista ephedroides with potential antifungal and anticancer activity against EGFR L858R/T790M mutant non-small cell lung cancer.

ATM-3507 is a protomyosin inhibitor with anticancer activity that inhibits human melanoma and can be used to study ovarian cancer.