Chromatin/Epigenetics

<p>CARM1-IN-3 dihydrochloride (17b) is a potent CARM1 inhibitor (IC50: 0.07 μM) with selectivity over CARM3 (IC50 &gt;25 μM).</p>

<p>KDOAM-25 trihydrochloride selectively inhibits KDM5 enzymes, boosts H3K4 methylation, and suppresses MM1S cell growth.</p>

<p>LSD1-IN-19 is a potent, selective LSD1 inhibitor with Ki of 0.108 μM and 72h IC50 values of 0.17-0.40 μM.</p>

<p>CFT8634 degrades BRD9, for synovial sarcoma and SMARCB1 tumor research, from patent WO2021178920A1.</p>

<p>P300 bromodomain-IN-1 blocks c-Myc, induces G1/G0 arrest, apoptosis. Potent EP300 inhibitor (IC50: 49 nM).</p>

<p>SCH-1473759 is an inhibitor of the aurora (IC50s: 4 and 13 nM for Aurora A and B, respectively).</p>

<p>QCA570 is an effective BET degrader based on PROTAC (IC50: 10 nM for BRD4 BD1 Protein).</p>

<p>Londamocitinib (JAK1-IN-7) is a selective and potent JAK1 inhibitor with anti-inflammatory activity.</p>

<p>MAO A/HDAC-IN-1 is an effective monoamine oxidase A (MAO A) and HDAC dual inhibitor, which can be used for glioma research.</p>

<p>BRD4 D1-IN-2 (compound 26), a BRD4 D1 inhibitor, IC50 &lt;0.092 μM, 15 nM affinity, &gt;500x selectivity over BRD2 D1/BRD4 D2.</p>

<p>HDAC6-IN-12 is a potent inhibitor of HDAC6 that binds in the DNA chain, causing DNA damage and exhibiting anticancer effects that can be used in cancer research</p>

<p>Balanol is an ATP-competitive Protein Kinase C and Protein Kinase A inhibitor.</p>

<p>Tyk2-IN-17 (compound 185) effectively inhibits TYK2 [1].</p>

<p>Tyk2-IN-14, a small molecule inhibitor of TYK2, is significant in treating inflammatory diseases and conditions linked to hypersecretion of IFNa and interferons [1].</p>

<p>PARP-1-IN-1: Selective, oral PARP-1 inhibitor with 0.96 nM IC50; well-tolerated and effective in single-dose MDA-MB-436 model.</p>

<p>B026: Oral p300/CBP HAT inhibitor, IC50: p300 1.8 nM, CBP 9.5 nM; targets AR+ prostate cancer cells.</p>

<p>Pim-1 kinase inhibitor 6 (Compound 4d) is a robust inhibitor of Pim-1 kinase, demonstrating an IC 50 of 0.46 μM. It significantly exhibits cytotoxic effects on cancer cells [1].</p>

<p>DS44470011 is an inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PHD) with oral bioavailability. It enhances the release of erythropoietin (EPO) from cells and is utilized in research related to renal anemia.</p>

<p>IBL-302 (AMU302), an orally available dual-signaling inhibitor targeting PIM and PI3K/AKT/mTOR, is effective against breast cancer and neuroblastoma. It has shown in vivo efficacy in a nude mouse xenograft model by combating trastuzumab resistance. Additionally, IBL-302 augments the effectiveness of widely used cytotoxic chemotherapy drugs such as cisplatin, doxorubicin, and etoposide [1] [2] [3].</p>

<p>SE-7552, a derivative of 2-(difluoromethyl)-1,3,4-oxadiazole (DFMO), serves as an orally active, highly selective non-hydroxamate HDAC6 inhibitor, boasting an IC50 of 33 nM. It exhibits over 850-fold selectivity against all other known HDAC isozymes. Demonstrating efficacy in vivo, SE-7552 effectively inhibits the growth of multiple myeloma. Additionally, it functions as an anti-obesity agent in diet-induced obese mice [1] [2].</p>

<p>Menin-MLL inhibitor 26: Active reference, inhibits cell growth, used in leukemia research.</p>

<p>EED ligand 1: potent PRC2 inhibitor targeting EED subunit.</p>

<p>MDH1/2-IN-1 is an MDH1/2 inhibitor with IC50 values of 1.07 nM and 1.06 nM, respectively. It suppresses mitochondrial respiration and the HIF-1α pathway. MDH1/2-IN-1 exhibits significant antitumor potential and offers new avenues for developing drugs targeting cancer metabolism.</p>

<p>JAK1/TYK2-IN-4 serves as a dual inhibitor targeting both JAK and TYK2, displaying IC50 values of 39 nM and 21 nM, respectively. It is also orally bioavailable [1].</p>

<p>WDR5-IN-5: Selective oral inhibitor for WDR5's WIN site with high affinity (Ki&lt;0.02 nM) and anti-cancer properties. Good pharmacokinetics.</p>

<p>Aurora inhibitor 1 is a potent Aurora inhibitor (IC50: ≤ 4 nM and ≤13 nM for Aurora A and Aurora B kinase).</p>

<p>BET-IN-8 (Compound 27) is a potent inhibitor of BET (Ki: 0.83 μM, Kd: 0.571 μM), which ameliorates LPS-induced sepsis in vivo.BET-IN-8 has shown potential in</p>

<p>GSK8814 is a selective and ATAD2/2B bromodomain chemical probe and inhibitor (binding constant pKd=8.1 and a pKi=8.9 in BROMOscan).</p>

<p>Basroparib is an inhibitor of ribose polymerase (PARP) and has shown antitumour effects.</p>

<p>BRD-7880 is a potent and highly specific inhibitor of aurora kinases B and C.</p>

<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>