transformation

OSI-906 (Linsitinib (OSI-906)) is an orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Linsitinib selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGF-1R stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis.

KW-2450 free base is an orally bioavailable inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR) tyrosine kinases with potential antineoplastic activity. IGF-1R IR inhibitor KW-2450 free base selectively binds to and inhibits the activities of IGF-1R and IR, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-R1 and IR tyrosine kinases, overexpressed in a variety of human cancers, play significant roles in the stimulation of cellular proliferation, oncogenic transformation, and suppression of apoptosis.

(-)-Epigallocatechin, the predominant flavonoid in green tea, possesses the unique ability to attach to unfolded native polypeptides, thereby inhibiting their transformation into amyloid fibrils.

(2-Aminoethyl)phosphonic acid (2-Aminoethylphosphonic acid) is primarily detected in urine. (2-Aminoethyl)phosphonic acid participates in many enzymatic reactions and is also the parent compound of other transformation products, including but not limited to ceramide 2-(methylamino)ethylphosphonate, N-(2-phosphineethyl)cholamide and CMP-2-aminoethylphosphonate.

Trans-Aconitic acid is normally present in normal human urine, and it has been suggested that is present in larger amounts with Reye's syndrome and organic aciduria. trans-Aconitic acid is a substrate of enzyme trans-aconitate 2-methyltransferase (EC 2.1.

o-Phenanthroline (1,10-Phenanthroline) , a metal chelator, prevents the induction of chromosomal aberrations in streptozotocin-treated cells.o-Phenanthroline protects mammalian cells from hydrogen peroxide-induced gene mutation and morphological transformation.

1. Ethyl trans-caffeate (Caffeic Acid Ethyl Ester) has anti-inflammatory activity. 2. Ethyl trans-caffeate may as a promising natural compound for future application in chronic liver disease. 3. Ethyl trans-caffeate is a potent chemopreventive compound against skin carcinogenesis caused by solar UV exposure. 4. Ethyl trans-caffeate is the high-resolution structures of representative inhibitors in complex with human pancreatic α-amylase. 5. Ethyl trans-caffeate strongly inhibits neoplastic transformation of JB6 Cl41 cells without toxicity. PI3K, ERK1 2, and p38 kinase activities were suppressed by direct binding with HOEC in vitro.

1. Betulonic acid (Liquidambaric acid) amide stimulated the regenerative response in hepatocytes under conditions of combined toxic exposure and promoted recovery of their qualitative and quantitative characteristics, which was accompanied by a significant decrease in the severity of liver fibrosis and the absence of cirrhotic transformation of the liver. 2. Betulonic acid derivatives have a promising cytostatic activity in vitro and could be used as potential leads for the development of new type of anti-cancer agents. 3. Betulonic acid has antiholestatic effects in mice.

EHT 1864 (EHT 1864 2HCl) is a Rac family GTPase inhibitor that blocks activation by direct binding to Rac1, Rac1b, Rac2, and Rac3 (Kd=40 50 60 250 nM). EHT 1864 inhibits Rac, Ras, and Tiam-induced growth transformation of NIH-3T3 fibroblasts.

Dibenz[a,h]anthracene (CCRIS 208) has induced DNA damage and gene mutations in bacteria and gene mutations and transformation in several types of mammalian cell cultures.

TK216 is a potent inhibitor of E26 transformation-specific (ETS) with anticancer activity.

Antipain, a protease inhibitor isolated from Actinomycetes, inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations[1][2].

sAJM589 is a Myc inhibitor that dose-dependently disrupts Myc-Max heterodimers, thereby decreasing Myc protein levels. Myc is a multifunctional nuclear phosphoprotein that plays a key role in cell cycle progression, apoptosis, and cellular transformation. sAJM589 inhibits the cellular proliferation of a variety of Myc-dependent cancer cell lines and the adherent, non-dependent growth of Raji cells’ Growth.

Mevalonic acid lithium salt (MVA lithium salt) is a precursor of the mevalonic acid pathway, an initiator of cell growth, a key substance in cholesterol synthesis, and stimulates DNA synthesis, morphology transformation, and cell cycling in human lymphocytes from peripheral blood.

CYP51-IN-20 (compound 5b), an antifungal agent, effectively inhibits CYP51 and exhibits significant activity against Candida albicans ATCC 10231. It suppresses the ERG11 (Cyp51) gene expression and markedly curtails the morphological transformation from yeast to hyphae. Furthermore, when combined with Voriconazole, CYP51-IN-20 synergistically occupies the entire CYP51 binding site, enhancing its inhibitory impact in the Glechoma moth model.

LENNOXAMINE is an alkaloid synthesized through an intramolecular addition of an aryl radical to (trimethylsilyl)acetylene, resulting in a ten-membered lactone, followed by internal cyclization. This process involves a molecular structural transformation from the ten-membered lactone to LENNOXAMINE.

Pulcherosine, a compound formed through the oxidative coupling of isodityrosine and tyrosine, features a biphenyl linkage that creates a 2,2'-dihydroxy-3-phenoxybiphenyl aromatic core. It functions as an intermediate in the transformation of isodityrosine into the tetramer di-isodityrosine. Additionally, Pulcherosine contributes to the formation of inter-polypeptide cross-links and or extensive intra-polypeptide loops.

Trimegestone, a highly effective oral progestogen, is used for endometrial protection, all doses inducing secretory endometrial transformation.

SCH 51344 inhibits Ras-induced malignant transformation and prevents anchorage-independent growth of oncogene-transformed fibroblasts [1].

AD57, as polypharmacological cancer therapeutic, is designed to regulate multiple targets related to cancer blocks the receptor tyrosine kinase RET in Drosophila (IC50: 2 nM). AD57 effectively suppresses tyrosine kinase RET, weakens the activity of numero

MYRA-A is an inducer of apoptosis in a Myc-dependent manner that acts by inhibiting Myc-driven transformation and disrupting MYC-Max interaction.

DAC-2-25 is a Hydra head regeneration modulator. It acts by inducing a homeotic transformation in Hydra.

BLL5 Maleate is a first-in-class selective PRMT5 inhibitor, it blocks EBV-driven B lymphocyte transformation and survival while leaving normal B cells unaffected.

L 685487 is produced by microbial transformation of FR 900520.