Cromatina/Epigenetica

Aldometanib (LXY-05-029) is an oral aldolase inhibitor that maintains metabolic balance by blocking FBP and activating lysosomal AMPK.

LLY-283, PRMT5 inhibitor, IC50 22 nM, Kd 6 nM, oral, selective, with antitumor effects.

AMG-193 is an inhibitor of the MTA-PRMT5 complex and is used in the study of cancer, respiratory diseases and digestive disorders.

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is a PRMTs inhibitor , with anticancer activity, for the study of advanced solid tumors.

JDTic, a 4-phenylpiperidine derivative distantly related to analgesics like meperidine and ketobemidone and more closely to the mu opioid antagonist alvimopan, exhibits a notably long duration of action, maintaining effects in animals for weeks following a single dose. This duration is not due to irreversible binding to the kappa opioid receptor but rather to altered activity of c-Jun N-terminal kinases. As a highly selective antagonist for the κ-opioid receptor, without influencing the μ- or δ-opioid receptors, JDTic has shown potential in animal studies for producing antidepressant and anxiolytic effects. It also demonstrates promise in treating addiction to substances such as cocaine and morphine, distinguishing itself structurally from other kappa antagonists like norbinaltorphimine.

Sinefungin (Adenosyl-Ornithine) is an effective inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral

BRD0639 is a first-in-class PRMT5-substrate interaction inhibitor for PBM-dependent PRMT5 activity studies.

EHMT2-IN-2 Used in the research of blood disease or cancer. EHMT2-IN-2 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2.

(8R,9S)-Talazoparib is Talazoparib enantiomer , less active than Talazoparib on the inhibition of PARP1 (IC50: 144 nM).

<p>PLK1-IN-6: potent, selective PLK1 inhibitor, IC50 = 0.45 nM, hinders cancer cell growth.</p>

Cercosporin, produced by the plant pathogen Cercospora kikuchii and the elsinochromes, is a potent photosensitizer with a short activation wavelength. Cercosporin contains perylene quinone structural features essential for PKC activity (IC50: 0.6-1.3 μM).

HJB97 is used for the design of potential PROTAC BET degrader. It also has antitumor activity. HJB97 is a high-affinity inhibitor of BET (Kis: 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), 1.0 nM (BRD4 BD2), respectively).

CARM1-IN-1 hydrochloride is a potent and selective inhibitor of CARM1 (IC50: 8.6 μM) with minimal inhibition of PRMT1 and SET7.

YF-2 hydrochloride is a potent histone acetyltransferase activator that exhibits high selectivity and can pass through the blood-brain barrier. It specifically acetylates H3 in the hippocampus, with EC50 values of 2.75 μM, 29.04 μM, and 49.31 μM for CBP, PCAF, and GCN5, respectively. Notably, it does not affect HDAC activity. Moreover, YF-2 hydrochloride demonstrates promising anti-cancer and anti-Alzheimer's disease properties.

(3R,4S)-Tofacitinib, the less active enantiomer of Tofacitinib, is a JAK3 inhibitor with an IC50 of 1 nM.

Amredobresib is a potent BET inhibitor that impedes the interaction between bromodomains and acetylated lysines on histone H3 and H4, thereby serving as crucial regulators of gene transcription. It proves valuable in the investigation of acute myeloid leukemia (AML) and cancer.

BD-9136, a highly selective BRD4 degrader, demonstrates the capability to inhibit tumor growth without inducing adverse effects in mice, showing potential for

HIF-PHD-IN-1 is a pharmacological compound that acts as an orally active inhibitor of the hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), displaying an IC50 of 54 nM for hHIF-PHD2. Its potential as a therapeutic agent for renal anemia is highly promising.

<p>20-HETE is a CYP450 product, vasoconstrictor, modulates K+ channels, affects NADPH, ROS, NF-κB, NO synthase, and cell apoptosis/proliferation.</p>

<p>CTB (Cholera Toxin B subunit) is an activator of p300 histone acetyltransferase and induces apoptosis in MCF-7 cells.</p>