Chromatin/Epigenetics

<p>PRMT5 IN-1 hydrochloride is a potent PRMT5 inhibitor (IC50: 11 nM), forms covalent adduct with C449, and converts to an aldehyde in vivo.</p>

<p>DS17701585: Oral EP300/CBP inhibitor; potent on CBP, EP300, H3K27, &amp; SOX2; useful for cancer research.</p>

<p>Tyk2-IN-15 (Compound 97) is a selective inhibitor of tyrosine kinase 2 (Tyk2) with an IC50 value ≤ 10 nM for Tyk2-JH2. It is utilized in the research of inflammatory and autoimmune diseases [1].</p>

<p>BRD4-BD1/2-IN-2 inhibits BRD4 BD1/BD2 with IC50 &lt;300 nM/&lt;0.5 nM (WO2021233371A1).</p>

<p>HDAC2-IN-1 is an oral HDAC2 inhibitor (IC50: 0.5 μM), crosses the blood-brain barrier, and inhibits HDAC1 and HDAC8.</p>

<p>PRMT5-IN-18 (Compound 002) is a potent inhibitor of PRMT5 and can be used in the study of PRMT5-mediated diseases, such as tumours.</p>

<p>HDAC-IN-33 inhibits HDAC1/2/6 (IC50: 24/46/47 nM), exhibits potent antitumor activity in vitro and in vivo, and activates antitumor immunity.</p>

<p>MTL-CEPBA is a small activating RNA that targets C/EBPα upregulation and exhibits anti-inflammatory and anti-cancer effects.</p>

<p>Aurora A inhibitor 1: potent, selective, targets cancer-linked Aurora A overexpression, potential for cancer research. (WO2021147974A1, 49)</p>

<p>ORIC-944 is an orally available, selective variant of PRC2 with anticancer activity for the study of prostate cancer.</p>

<p>Pocenbrodib (FT-7051) is a potent inhibitor of the bromodomain of the CBP/p300 family with potential antitumour activity and is palatable for cancer research.</p>

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

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

<p>DN02: a potent, selective BRD8(1) bromodomain probe; Ki=32 nM; 30x more affine than BRD8(2).</p>

<p>EZM0414 is a potent, selective, orally bioavailable inhibitor of SETD2 with IC50 of 18 nM in SETD2 biochemical assay and IC50 of 34 nM in a cellular assay.</p>

<p>INCB054329 is a BET inhibitor targeting BRD2/3/4 and BRDT with IC50s ranging from 1-119 nM.</p>

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

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

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

<p>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.</p>