tumorigenesis

DT-061, an orally bioavailable protein phosphatase 2A (PP2A) activator, may be used in the therapy of KRAS-mutant and MYC-driven tumorigenesis.

Broparestrol (E)- has antifertility activity and is a potent inhibitor of rodent mammary tumorigenesis.

Retinoic acid (Tretinoin), a metabolite of vitamin A, is a natural agonist of the retinoic acid receptor RAR and inhibits RARα β γ (IC50=14 nM). Retinoic acid induces cellular differentiation, reduces cellular proliferation, and inhibits tumorigenesis.

2-Undecanone (Methylnonylketone) inhibits DnaKJE-ClpB dione-dependent refolding of heat-inactivated bacterial fluorokinase. It has an inhibitory effect on lung tumorigenesis.

Bardoxolone (CDDO) is a synthetic oleanane triterpenoid that blocks the cellular synthesis of inducible nitric oxide synthase and inducible COX-2 in INF-γ-activated mouse macrophages with an IC50 value of 0.4 nM. By suppressing reactive oxygen and nitrogen species (ROS RNS) formation, it promotes the cellular control of ROS RNS levels that would lead to DNA damage associated with tumorigenesis. In various Y cell lines, Bardoxolone has been shown to specifically inhibit proliferation and induce apoptosis. Mechanism studies revealed that Bardoxolone is a ligand for peroxisome proliferator-activated receptor γ, and also that it induces genes regulated by Nrf2, including heme oxygenase-1 and eotaxin-1, which play a role in antioxidant response element signaling activity.

Liensinine is the active constituent of plumula nelambinis with anti-hypertension.

Copanlisib (BAY 80-6946) is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. By inhibiting the PI3K signaling pathway, Copanlisib may impede tumor cell growth and survival in certain tumor populations. Dysregulated PI3K signaling, often linked to tumorigenesis, may also contribute to tumor resistance to various antineoplastic agents.

3-Phenylpropyl isothiocyanate exhibits a potent inhibitory effect on N-nitrosomethyl-benzylamine (NMBA) tumorigenesis, thereby displaying strong chemopreventive properties [1] [2].

Cyproterone acetate (Cyproterone 17-O-acetate) binds the androgen receptor (AR), thereby preventing androgen-induced receptor activation in target tissues and inhibiting the growth of testosterone-sensitive tumor cells. Cyproterone acetate is the acetate salt of a synthetic steroidal antiandrogen with weak progestational and antineoplastic activities. This agent also exerts progestational agonist properties at the level of the pituitary that reduce luteinizing hormone (LH), resulting in reductions in testicular androgen secretion and serum testosterone levels. Treatment with cyproterone alone results in incomplete suppression of serum testosterone levels.Cyproterone binds the androgen receptor (AR), thereby preventing androgen-induced receptor activation in target tissues and inhibiting the growth of testosterone-sensitive tumor cells. Cyproterone Acetate is the acetate salt of a synthetic steroidal antiandrogen with weak progestational and antineoplastic activities. This agent also exerts progestational agonist properties at the level of the pituitary that reduce luteinizing hormone (LH), resulting in reductions in testicular androgen secretion and serum testosterone levels. Treatment with cyproterone alone results in incomplete suppression of serum testosterone levels.

PIM447 (LGH447) is an oral, selective pan-PIM kinase inhibitor with antitumor and bone-protective effects. It inhibits PIM1, PIM2, and PIM3, induces apoptosis, and decreases the viability, proliferation, and motility of HuH6 and COA67 cells. PIM447 suppresses tumorigenesis in hepatocellular carcinoma and can be used in the study of multiple myeloma.

ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities[1][2][3]. It positively modulates murine DCs, induces NSC proliferation, and constitutes a promising therapeutic agent for various neurologic disorders[4][5]. It also activates apoptotic proteins in human lymphoma U937 cells[3].

FAK-IN-22 (Compound 26) is an inhibitor of FAK, JAK3, and Aurora B, with IC50 values of 50.94 nM, 9.99 nM, and 0.49 nM, respectively, effectively suppressing tumorigenesis and metastasis in pancreatic ductal adenocarcinoma (PDAC). It inhibits proliferation in PANC-1 cells with an IC50 of 0.15 μM. FAK-IN-22 induces apoptosis and G2 M phase arrest in PANC-1 cells by inhibiting the FAK PI3K Akt signaling pathway.

MTH1 activator-1 is an MTH1 activator that enhances endogenous MTH1 activity and significantly reduces 8-oxo-dG levels in cellular DNA. It is useful for investigating the upregulation of oxidative damage repair in nucleotide pools and examining biological effects, as well as for studies aiming to delay or prevent tumorigenesis.

Ovatodiolide, a small molecule compound derived from fennel, has anti-inflammatory and potentially neuroprotective activity, inhibits colon tumorigenesis, and can be used in the study of neurological disorders.

ADP-Ribosylarginine can regulate cell proliferation and tumorigenesis.

Ochratoxin A-13C20is intended for use as an internal standard for the quantification of ochratoxin A by GC- or LC-MS. Ochratoxin A is a mycotoxin that has been found inAspergillusandPenicillium.1It increases lipid peroxide levels and the number of apoptotic cells, as well as reduces superoxide dismutase activity in rat kidney when administered at a dose of 120 μg/kg.2Topical application of ochratoxin A (80 μg/mouse) induces DNA damage, cell cycle arrest at the G0/G1phase, and apoptosis in mouse skin cells.1It also initiates tumor formation in a two-stage mouse skin tumorigenesis model. Ochratoxin A has been found as a contaminant in a variety of foods.3

(S)-GFB-12811 (compound 596) is a selective inhibitor of CDK5 (IC50<10 nM) and can be used in studies of cell cycle progression, neuronal development, and tumorigenesis.

NZ28, also known as NSC134754, is potent HSF1 inhibitor, which induced inhibition of HSF1, SP1 and NF-κB triggers the loss of the natural killer cell-activating ligands MICA B on human tumor cells. Heat-shock transcription factor HSF1 has a critical role in human epidermal growth factor receptor-2-induced cellular transformation and tumorigenesis.

LY2780301 is an orally bioavailable inhibitor of the serine threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor LY2780301 binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K Akt signaling pathway, thereby leading to inhibition of cell proliferation and the induction of apoptosis in tumor cells. Activation of the PI3K Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

GNE-8525 is a potent and selective pan-TRK inhibitor. GNE-8525 demonstrated potent antiproliferation activity with IC50 = 0.003 μM. In a tumor xenograft model derived from the KM12 cell line, GNE-8525 demonstrated in vivo antitumor efficacy when administered at ascending doses twice daily (bid) for 14 days in rats. Deregulated kinase activities of tropomyosin receptor kinase (TRK) family members have been shown to be associated with tumorigenesis and poor prognosis in a variety of cancer types. In particular, several chromosomal rearrangements involving TRKA have been reported in colorectal, papillary thyroid, glioblastoma, melanoma, and lung tissue that are believed to be the key oncogenic driver in these tumors.

PROTAC EZH2 Degrader-1 (Compound 150d) is a potent inhibitor that effectively suppresses EZH2 methyltransferase activity, with an IC50 of 2.7 nM. EZH2 plays a critical role in various tumorigenesis and development processes [1].

Phospholipase D (PLD), an enzyme within the phospholipase superfamily, is prevalent across bacteria, yeast, plants, animals, and viruses, serving roles in biochemical research. It catalyzes the hydrolysis of glycerophospholipids' phosphodiester bonds, generating phosphatidic acid and soluble choline. PLD is implicated in numerous disease-related pathways, such as diabetes, atherogenesis, obesity, tumorigenesis, immune responses, and neuroendocrine functions [1].

EB-3D is a potent and selective choline kinase alpha 1 (ChoKα1) inhibitor (IC50: 1 μM) with anti-cancer activity.

UNC9512 is a potent antagonist of the methyl-lysine reader protein 53BP1, which can be utilized to investigate the function of 53BP1 in DNA repair, gene editing, and tumorigenesis [1].