anti-cancer activity

HNHA is an inhibitor of HDAC.

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.

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

5-Aminosalicylic Acid (5-ASA) is a specific PPARγ agonist and also inhibits P21-activated kinase 1(PAK1) and NF-Κb. 5-Aminosalicylic Acid has anti-cancer and anti-inflammatory activities. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead

Ifebemtinib (BI-853520) is an orally active and potent inhibitor of adhesion plaque kinase (FAK) (IC50=1 nM) with anti-tumour activity that inhibits globule formation and in situ tumour growth in malignant pleural mesotheliomas, and may be useful for the study of breast and ovarian cancer.

Antitumor agent-2 has anti-inflammatory and anti-tumor activity and can be used to study cancer.

GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity.

OXFBD04 is a potent and selective BRD4 inhibitor (IC50= 166 nM), a BET bromodomain ligand with modest affinity for the CREBBP bromodomain, and exhibits anti-cancer activity.

SR-318 is a potent and highly selective inhibitor of p38 MAPK, demonstrating IC50 values of 5 nM for p38α, 32 nM for p38β, and 6.11 μM for p38α/β. It possesses both anti-cancer and anti-inflammatory activity.

β-NETA (α-NETA) is a stable, noncompetitive, slowly reversible choline acetyltransferase (ChAT) inhibitor with an IC50 of 9 μM and is a potent chemokine-like receptor-1 (CMKLR1) antagonist. β-NETA has anti-cancer activity[1][2]. β-NETA weakly inhibits cholinesterase (IC50=84 µM) and acetylcholinesterase (IC50=300 µM).

Zindoxifene (D 16726) is an anti-estrogenic compound with antitumor activity that can be used in studies of breast and prostate cancer.

BMS-960 is an S1P agonist with potential anti-tumour activity for cancer research.

Pyrazoloacridine (PD 115934) is a nucleic acid binding agent that inhibits the activity of topo I and II with an IC50 of 1.25 μM in K562 cells. Pyrazoloacridine shows anti-cancer activity.

rac-CCT-250863 HCl is a selective and reversible inhibitor of NEK 2. rac-CCT-250863 HCl induces cell cycle arrest and has good anti-proliferative activity against cancer cells. rac-CCT-250863 HCl can be used in combination with Pomalidomide to induce apoptosis and can be used in combined anti-cancer studies.

VPC-13163 (NSC-52361) has strong anti-proliferative activity against LNCaP and Enzalutamide-resistant prostate cancer cell lines (MR49F) whereas it did not affect the growth of AR independent PC3 cell line. It also inhibits Prostate Specific Antigen (PSA) in both LNCaP and MR49F and reduces expression of AR target genes, PSA and TMPRSS2. These findings suggest that VPC-13566 exhibits AR BF3 specific mechanism of action.

Panomifene HCl is a selective anti-estrogenic compound with antitumor activity for the treatment of breast cancer.

PBRM1-BD2-IN-8 (compound 34) is a potent PBRM1 Bromodomain inhibitor with PBRM1-BD2 Kd of 4.4 μM, PBRM1-BD2 IC50 of 0.16 μM, and PBRM1-BD5 Kd of 25 μM; PBRM1-BD2-IN-8 shows anti-cancer activity.

BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor with an IC50 of 0.3 nM, exhibiting anti-tumor activity and potential applications in cancer and polycystic kidney disease research [1] [2].

MPT0G211 is a highly selective and orally active HDAC6 inhibitor (IC50=0.291 nM) that has neuroprotective effects and has shown anti-metastatic activity in human breast cancer cells. MPT0G211 has 1,000 times more affinity for HDAC6 than other HDAC subtypes. MPT0G211 can cross the blood-brain barrier and could be used to improve tau phosphorylation and cognitive deficits in Alzheimer's disease models.

L82 is a DNA ligase 1 (DNA Lig1) inhibitor (hLig1 IC50=12 μM) that is selective and non-competitive.L82 expresses anti-proliferative activity against breast cancer cells.

Tilomisole (Wy 18251) is an orally available benzimidazole thiazole with anti-inflammatory activity and immunomodulatory activity.Tilomisole is used in the study of cancer and inflammation.

USP1-IN-2 is a potent USP1 inhibitor with potential anti-tumor activity for the study of cancer.