tumorigenesis

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

DT-061 is an orally bioavailable protein phosphatase 2A (PP2A) activator. It could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis.

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

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.

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.

Copanlisib (BAY 80-6946) is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. Copanlisib inhibits the activation of the PI3K signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents.

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].

ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities[1][2][3]. ar-Turmerone ((+)-ar-Turmerone) exerts positive modulation on murine DCs, induces NSC proliferation.

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

Seribantumab (MM 121), a fully human IgG2 monoclonal antibody, specifically targets HER3, inhibiting the activation of the epidermal growth factor receptor (ErbB) family and its subsequent signaling. This action effectively blocks neuregulin 1 (NRG1) fusion-dependent tumorigenesis within in vitro and in vivo studies of patient-derived cancer models in breast, lung, and ovarian cancers [1].

HTH-02-006, a NUAK2 inhibitor (IC50 = 126 nM), decreases phosphorylated MYPT1 levels in HuCCT-1 cells and inhibits YAP-driven cell proliferation, hepatomegaly, and tumorigenesis. Additionally, it possesses an antifibrotic protective effect [1] [2].

Cdc25A (80-93) (human) is a polypeptide implicated in the regulation of cell proliferation and tumorigenesis through modulation of cyclin D1 expression and facilitation of the G1/S phase transition. This compound has applications in cancer research [1].

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

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

EN4 (EN4 MYC inhibitor) MYC inhibitor is a covalent ligand that targets cysteine 171 (C171) of MYC. It is selective for c-MYC over N-MYC and L-MYC, and inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis.

ADP-Ribosylarginine can regulate cell proliferation and 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.

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.

Torilin is an inhibitor of testosterone 5 alpha-reductase, it (IC50 = 31.7 +/- 4.23 microM) shows a stronger inhibition of 5 alpha-reductase than alpha-linolenic acid (IC50 = 160.3 +/- 24.62 microM) but is weaker than finasteride (IC50 = 0.38 +/- 0.06 microM). Torilin has immunomodulatory, hepatoprotective, and anti-inflammatory properties, it inhibits inflammation by limiting TAK1-mediated MAP kinase and NF-κB activation, it can attenuate arthritis severity, modify leukocyte activations in dLNs or joints, and restore serum and splenocyte cytokine imbalances. Torilin inhibits melanin production in alpha-melanocyte stimulating hormone-activated B16 melanoma cells, with an IC(50) value of 25 microM. Torilin shows excellent antimicrobial activity against Bacillus subtilis ATCC 6633 spores and vegetative cells. Torilin has a potent anti-angiogenic activity both in vivo and in vitro, and it may have a strong activity to suppress tumorigenesis by inhibition of tumor invasion, it reverses multidrug-resistance in cancer cells, it can potentiate the cytotoxicities of adriamycin, vinblastine, taxol and colchicine against multidrug-resistant KB-V1 and MCF7/ADR cells.

TPCK is an irreversible inhibitor of chymotrypsin-like proteases that affect cell proliferation, apoptosis, 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.

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].

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

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

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.

Ochratoxin α is a less toxic photolytic and thermal degradation product of Ochratoxin A.