Cromatina/Epigenética

<p>PF-03622905: potent ATP-competitive PKC inhibitor, IC50: 5.6-74.1 nM for PKCα/βI/βII/γ/θ, high specificity for PKC.</p>

<p>7-Hydroxyneolamellarin A, from Dendrilla nigra, inhibits HIF-1α and VEGF in cancer research.</p>

<p>JPS035: potent benzamide-based VHL E3 ligase PROTAC, degrades HDAC1/2, increases gene expression and apoptosis in HCT116 cells.</p>

<p>K-252b, an indolocarbazole derived from the actinomycete Nocardiopsis, functions as a protein kinase C (PKC) inhibitor.</p>

<p>Biguanide can reduce oxidative stress in rats with hyperglycemia.</p>

<p>BRD3067, a Tubacin derivative, inhibits HDAC6 (IC50 15 nM) and acts as a negative control for Tubacin A, showing anticancer and anti-inflammatory effects.</p>

<p>Pulrodemstat HCl is an LSD1 inhibitor and a KDM1A inhibitor with anticancer anti, proliferative activity.</p>

<p>MSC2504877 inhibits tankyrase, boosts CDK4/6 inhibitors, blocks Cyclin D2/E2 upregulation, and strengthens phospho-Rb suppression.</p>

<p>Pan-BET/BD2-IN-1 (compound 6b) is a selective BET protein inhibitor with BRDT-1Ki of 1.05 μM and BRD4-1Ki of 0.68 μM. It effectively inhibits the growth of MM.1S cancer cells with an IC50 value of 2.6 μM.</p>

<p>POI ligand 1 serves as a template for the non-selective HDAC inhibitor Vorinostat. It functions as a target protein ligand (PROTAC target protein ligand) in the creation of PROTAC HDAC degraders with anti-tumor properties. Additionally, POI ligand 1 is utilized in the synthesis of FF2049.</p>

<p>SJ1008030, a JAK2 PROTAC, degrades JAK2; EC50: 5.4 nM, IC50: 32.09 nM in MHH-CALL-4 cells for leukemia research.</p>

<p>BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.</p>

<p>Malantide, a synthetic dodecapeptide, boosts and measures PKA activity by undergoing PKA-induced phosphorylation.</p>

<p>6-O-Isobutyrylbritannilactone, a sesquiterpene natural melanogenesis inhibitor, can be extracted from Inula britannica flowers.</p>

<p>SAMβA TFA, a selective antagonist of Mfn1-βIIPKC association conjugated to the cell permeable peptide TAT47-57, is a rationally designed inhibitor that improves</p>

<p>PRMT3-IN-4 (intermediate 15) is an inhibitor of Protein arginine methyltransferase 3 (PRMT3) and serves as the active control for SGC707. It can be utilized in the synthesis of PROTACs targeting PRMT3 and is applicable in research related to leukemia.</p>

<p>M-808, a strong covalent Menin-MLL inhibitor, binds tightly with a 2.6 nM IC50.</p>

<p>JAK/HDAC-IN-4 (compound 11 i) is a dual inhibitor targeting both JAK2 and HDAC6, with IC50 values of 0.49 nM and 12 nM respectively. It inhibits cell proliferation and the production of nitric oxide. In a mouse model induced by Imiquimod, JAK/HDAC-IN-4 ameliorates psoriasiform skin lesions with low toxicity.</p>

<p>HDAC-IN-26 is a highly selective class I HDAC inhibitor with an EC 50 value of 4.7 nM.</p>

<p>EEDi-5273: Potent oral EED inhibitor, IC50 ~0.2 nM; induces complete, lasting tumor regression.</p>

<p>C8 Dihydroceramide is a control for C8 Ceramide, a bioactive, cell-permeable, chemotherapeutic agent that boosts T cell responses and slightly activates PKC.</p>

<p>SJ46421, a PROTAC protein degrader derived from (+)-JQ-1, targets KLHDC2. It efficiently forms a stable ternary complex with KLHDC2, exhibiting an IC50 of 7.8 nM. Furthermore, SJ46421 promotes the polyubiquitination of the BD2 domain of BRD2, BRD3, or BRD4.</p>

<p>SMD-3236 is a PRAOTAC degrader targeting SMARCA2, designed using SMARCA ligand and VHL-1 ligand, and exhibits prolonged anti-tumor activity in vivo. SMARCA2 acts as a synthetic lethal target in cancer cells lacking SMARCA4, with SMD-3236 showing 2000-fold selectivity for SMARCA2 over SMARCA4, having a DC50 of less than 1 nM and a Dmax of over 95%. In the human cancer xenograft models deficient in SMARCA4, notably the H838 model, SMD-3236 effectively induces loss of SMARCA2 in tumor tissue while sparing the SMARCA4 protein, thereby inhibiting tumor growth. The compound consists of a target protein ligand (red part) SMI-1074, a PROTAC linker (black part) (trans-4-Ethynylcyclohexyl)methyl methanesulfonate, and an E3 ligase ligand (blue part) SMARCA2 ligand-14, forming the E3LigaseLigand-linker Conjugate 159.</p>

<p>Ep300/CREBBP-IN-8, IC50: 0.014/0.018 μM, potent Ep300/CREBBP inhibitor, oral, for cancer research.</p>

<p>Ac-MBP 1-11, a primary encephalitogenic epitope in myelin basic protein (MBP), is a dominant short peptide sequence[1].</p>

<p>Dihydrochlamydocinanalog-1 (compound 2) is a Chlamydocin analog that inhibits the deacetylation of histone H4 peptides, with an IC50 of 30 nM.</p>

<p>PROTAC SMARCA2/4-degrader-26 is a PROTAC targeting the SMARCA2/4 proteins. It is composed of the ligand for PROTAC targeting proteins, 2-(4-(3-Amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)acetic acid, an E3 ligase component (2S,4R)-4-Hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide, and a PROTAC linker (S)-2-Amino-3,3-dimethylbutanoic acid. The coupled complex of the E3 ubiquitin ligase ligand + Linker is referred to as (S,R,S)-AHPC.</p>

<p>HDAC1-IN-9 (13c) is an HDAC1 inhibitor. It inhibits the HDAC1 enzyme with an IC50 value of 1.07 µM. This compound exhibits the strongest antiproliferative activity against HT-29 (human colon adenocarcinoma cells), with an IC50 of 1.78 μM. In HCT-116 (human colon cancer cells), HDAC1-IN-9 significantly induces apoptosis. Additionally, HDAC1-IN-9 possesses antiangiogenic properties, reducing the expression levels of VEGFR-2 and phosphorylated VEGFR-2 (pVEGFR-2) by approximately 80%.</p>

<p>E3 ligase ligand-linker '(S,R,S)-AHPC-C5-COOH' for PROTACs, VH032 inhibits VHL/HIF-1α with 185 nM Kd, may aid anemia and ischemic disease research.</p>

<p>EPZ028862 is a</p>

<p>Pim-1 kinase inhibitor 11 (10f) is an inhibitor of PIM-1 with an IC50 value of 0.18 μM. It exhibits anticancer activity by inducing apoptosis and causing cell cycle arrest.</p>

<p>UNC6864, an ethylisopropyllysine-containing ligand, exhibits binding affinity to wild-type CBX5, demonstrating a dissociation constant (K D) of 3.3 μM.</p>

<p>EZH2-IN-4, an oral EZH2 inhibitor, targets WT and mutant forms with IC50s of 0.923 nM and 2.65 nM, showing strong anti-cancer effects.</p>

<p>JAK-2/3-IN-1 inhibits JAK-2/3 isoforms with sub-250 nM Ki; from US patent US8163732B2.</p>

<p>Potent SIRT1/2/3-IN-1 inhibits SIRT1/2/3 with IC50: 0.54, 0.25, 0.72 μM; used in cancer research.</p>

<p>NF-κB/HIF-1α-IN-1 (compound 9c) effectively inhibits the NF-κB activation pathway and demonstrates selective antifibrotic activity. This compound exhibits no significant cytotoxicity in NCI tumor cell lines. In rat models, NF-κB/HIF-1α-IN-1 successfully ameliorates liver fibrosis, suppresses the expression levels of NF-κB and HIF-1α, and induces Nrf2.</p>

<p>MZP-55 is a selective BRD3/4 degrader based on PROTAC technology(Brd4BD2 with Kd of 8 nM)</p>

<p>QA-68 is a potent BRD9 degrader, inhibits cell growth, and has anti-leukemic properties.</p>

<p>JQ1-TCO, a BET inhibitor derivative, enables click chemistry for molecular probing in vivo and in vitro.</p>

<p>1,4-DPCA is an inhibitor of prolyl-hydroxylase with an IC50 of 2.4 µM for collagen hydroxylation in human foreskin fibroblasts and 60 μM for factor inhibiting</p>

<p>Kiss2 peptide acetate is the acetate form of Kiss2 peptide, serving as a positive regulator of reproduction. It binds to its homologous receptor Kiss2R (GPR54) in COS-7 cells, activating the PKA and PKC signaling pathways through Gas and Gaq proteins. This activation enhances the activity of both cAMP response element-dependent luciferase (CRE-luc) and serum response element-dependent luciferase (SRE-luc).</p>

<p>OKI-006 is an oral HDAC inhibitor with potential for cancer research, derived from largazole.</p>

<p>TB22 is a non-nucleoside inhibitor of DOT1LR231Q with anticancer activity. It inhibits the malignant phenotype of lung cancer cells harboring the R231Q mutation via the MAPK/ERK signaling pathway, making it useful for lung cancer research.</p>

<p>WDR5-MYC-IN-1 (compound 4o) is an effective inhibitor of the WDR5-MYC interaction, demonstrating a Ki value of 1.0 µM and exhibiting antiproliferative activity.</p>

<p>Malantide TFA: synthetic dodecapeptide, PKA-specific with Km 15 μM, &gt;90% PKI blockage, also PKC substrate, Km 16 μM.</p>

<p>MRK-990 is an inhibitor of PRMT that targets both PRMT5 and PRMT9, with IC50 values of 30 nM and 10 nM, respectively.</p>

<p>(+)-JQ-1-aldehyde is the aldehyde derivative of (+)-JQ1, commonly used as a precursor for the synthesis of PROTACs targeting the BET bromine domain[1].</p>

<p>TAS-119 (TAS-2104) is an orally available, selective and potent inhibitor of Aurora A with an IC50 of 1.0 nM.TAS-119 also inhibits Aurora B with an IC50 of 95</p>

<p>KDM4ligand-1 is a ligand targeting the protein (histone lysine demethylase KDM4) in PROTACs. It can be utilized for the synthesis of PROTACs.</p>

<p>UNC10013 is an allosteric modulator of SETDB1, exhibiting negative allosteric regulation through covalent bond formation with Cys385 on the 3TD domain. It has a kinact/KI value of 1.0 × 10^6 M^-1*s^-1. UNC10013 effectively disrupts SETDB1-mediated Akt methylation, holding potential for application in cancer and neurodegenerative disease research.</p>

<p>dBET23 is a BRD4 degrader.</p>

<p>CPI-268456 is a compound which has bioactive.</p>

<p>UNC10142 (Compound 44) is a small-molecule antagonist of CHD1, with a binding IC50 value of 1.7 μM. It induces a dose-dependent reduction in the viability of PTEN-deficient prostate cancer cells.</p>

<p>PRMT1-IN-1 is a PRMT1 inhibitor.</p>

<p>SYY-B085-1 is a histone acetyltransferase (HAT) inhibitor.</p>

<p>SRG-II-19F is a BRDT BD1 degrader, useful for studying ClpC2's impact on ClpC1P1P2 protease.</p>

<p>ACBI2: potent, oral VHL PROTAC, EC50=7nM; degrades SMARCA2, DC50=1nM in RKO cells; for lung cancer research.</p>

<p>Compound I-291, also known as PROTAC SMARCA2/4-degrader-30, targets the catalytic subunits of the SWI/SNF complex, specifically SMARCA2 and SMARCA4. It effectively degrades SMARCA2 in A549 and MV411 cells, as well as SMARCA4 in MV411 cells, with a degradation concentration (DC50) of less than 100 nM.</p>

<p>EP300/CBP ligand 2 (compound S19) serves as a specific ligand for the bromodomain of CREB binding protein (CBP) and E1A-associated protein (EP300). It plays a critical role in PROTAC technology by acting as a target protein ligand. By linking to an E3 ubiquitin ligase ligand via the PROTAC Linker, it facilitates the synthesis of PROTAC molecules capable of targeted protein degradation. For instance, when EP300/CBP ligand 2 is connected to the conjugate (E3 ubiquitin enzyme ligand + Linker) Thalidomide-NH-C10-Boc, it results in the formation of the PROTAC molecule dCE-2.</p>

<p>TNKS-2-IN-2 is a TNKS2 selective inhibitor (IC50: 22 nM) with potential anti-tumour activity for the study of colon cancer lung cancer and breast cancer.</p>

<p>HSP90/LSD1-IN-1 (compound 6) is a dual inhibitor of HSP90 and LSD1. This compound effectively inhibits the proliferation of prostate cancer cell lines PC-3 and DU145, with GI50 values of 0.24 μM and 0.30 μM, respectively.</p>

<p>PARP1-IN-6, a dual-function inhibitor, targets both tubulin and PARP-1, demonstrating inhibitory concentration (IC50) values of 0.94 μM for tubulin and 0.48 μM</p>

<p>HAT-SIL-TG-1&amp;AT: a hypoxia-activated JAK inhibitor that curbs HEL cell growth &amp; STAT3/5 phosphorylation in tumors.</p>

<p>HIF-PHD-IN-4 (Compound 13) is an orally active PHD2 inhibitor with an IC50 of 100 nM. At a dose of 2 mg/kg, it effectively enhances G-CSF-induced mobilization of hematopoietic stem cells in mice. HIF-PHD-IN-4 is suitable for research in the oncology field.</p>

<p>AZD-9574 is a selective inhibitor of PARP1 at the sites of SSBs.</p>

<p>Protein Kinase C (19-36) is a pseudosubstrate peptide inhibitor of protein kinase C (PKC), with an IC50 of 0.18 μM.</p>

<p>PIM-IN-1 is a pan-PIM kinase inhibitor (KG-1, EC 50 = 61 nM; pS6, EC 50 = 71 nM).</p>

<p>KAT6-IN-2 is a potent inhibitor of KAT6, showing promise for use in cancer research.</p>

<p>JAK1/TYK2-IN-1 is a dual inhibitor of TYK2 and JAK1 ( IC 50 = 29 and 41 nM respectively).</p>

<p>CD532 hydrochloride, potent Aurora A inhibitor (IC50=45 nM), hampers MYCN protein, changes AURKA's shape, aids cancer research.</p>

<p>FTX-6058 hydrochloride is a potent EED inhibitor, induces HbF, and aids sickle cell and β-thalassemia research.</p>

<p>LLY-284, a less active PRMT5 inhibitor diastereomer of LLY-283, serves as its negative control.</p>

<p>A cyclopropanoid LSD1 inhibitor targeting schizophrenia and neurodegenerative disorders.</p>

<p>SMARCA2 degrader-17 is a degrader of SMARCA2, exhibiting synergistic antiproliferative effects with Adagrasib in cancer cells and capable of inhibiting tumor growth.</p>

<p>PRMT1 inhibitor, IC50=1.8μM; 5x more selective than PRMT6; &gt;250x over PRMT3, CARM1.</p>

<p>α-Hydroxyglutaric Acid is a natural product for research related to life sciences. The catalog number is T36624 and the CAS number is 2889-31-8.</p>

<p>Tyrosine Protein Kinase JAK 2 (Phospho-Tyr8, 9) is a peptide derived from mouse JAK2, specifically composed of amino acids 475 to 491.</p>

<p>dAURK-4, a derivative of Alisertib, functions as a potent and selective degrader of AURKA (Aurora A), exhibiting anticancer properties [1].</p>

<p>SJ1008030 (compound 8) formic is a selective JAK2 degrader within the PROTAC class, demonstrating efficacy in inhibiting MHH-CALL-4 leukemia cell growth with an</p>

<p>PROTAC TYK2 Agent1 selectively degrades TYK2, with a 14 nM DC50, for autoimmune research.</p>

<p>CPI-1328 is an EZH2 inhibitor with a K i value of 63 fM.</p>

<p>PF-3166 (compound PF-3166) is a cell-active inhibitor of PAD2.</p>

<p>S-Ruxolitinib can be used in related research in the field of life sciences. Its product number is T3066 and CAS number is 1160597-27-2.</p>

<p>Foenumoside B, a triterpene saponin extracted from Lysimachia foenum-graecum, stimulates AMPK signaling, suppresses PPARγ-induced adipogenesis, and promotes</p>

<p>BBDDL2204 (compound 13) is a potent and selective covalent inhibitor of EZH2, demonstrating an IC50 of 2.5 nM against EZH2Y641F.</p>

<p>dBAZ2B is a BAZ2B PROTAC degrader with a DC50 value of 19 nM. (Pink: BAZ2A/B ligand; Black: linker; Blue: CRBN Ligand)</p>

<p>PRMT5-IN-4 (compound AAA-1) is a PRMT5 inhibitor.</p>

<p>SIRT1 activated by CAY10591, mimics caloric restriction, extends lifespan, inhibits apoptosis, suppresses TNF-α, and promotes fat mobilization.</p>

<p>PROTACBRD4 Degrader-32 (Compound 22) is a potent BRD4 PROTAC degrader with a DC50 of 0.20 nM. It employs a unique carbon-carbon linker to connect the BRD4 binding domain with the CRBN binding domain, forming a ternary complex that induces BRD4 ubiquitination and facilitates proteasomal degradation. PROTACBRD4 Degrader-32 holds promise for research into BRD4-related cancers, such as hematological malignancies.</p>

<p>NPC-15437 dihydrochloride is a PKC inhibitor blocking enzyme activity and phorbol ester binding, selective over other kinases, in cellular signaling research.</p>

<p>TO-1187 is a selective HDAC6 PROTAC degrader with a DC50 of 5.81 nM. It enhances the ubiquitination and subsequent degradation of HDAC6, making it useful for research in hematological malignancies and solid tumors.</p>

<p>Larsucosterol ammonium salt is a derivative of 25HC3S. It is a DNMT inhibitor, a LXR antagonist, an endogenous epigenetic modulator of lipid metabolism.</p>

<p>A compound inhibits EZH2, overexpressed in cancers, affecting Treg activity and innate immunity.</p>

<p>Ifidancitinib (ATI-50002) is a JAK kinase 1/3 inhibitor used to study autoimmune diseases.</p>

<p>T-448 is a lysine-specific demethylase 1 inhibitor (IC50: 22 nM) that improves learning function in mice.T-448 can be used to study memory deficits.</p>

<p>AS-85 is an ASH1L inhibitor with anti-leukemic activity that inhibits leukemic cell growth and increases cLogP.</p>

<p>I-BET567: potent, oral pan-BET inhibitor; pIC50s: 6.9 (BRD4 BD1), 7.2 (BD2); effective in mouse cancer and inflammation models.</p>

<p>EZM0414 TFA (SETD2-IN-1 TFA) is a SETD2 inhibitor with anticancer and antiproliferative effects for the study of leukemia and immune dysfunction.</p>

<p>(R)-HH2853, a mutant EZH2 inhibitor, IC50 &lt;100 nM for EZH2-Y641F, targets cancer/autoimmune diseases.</p>

<p>PARP Protein, Mouse, Recombinant (His) is expressed in Baculovirus insect cells with His tag.</p>

<p>N-Descyclopropanecarbaldehyde Olaparib is a CRBN ligand for dual EGFR/PARP PROTAC, suitable for F-18 radiolabeling and tumor imaging via PET.</p>

<p>PROTAC EZH2 Degrader-1 suppresses EZH2 methyltransferase activity with IC50 2.7 nM, serving as a potent tool in cancer research and EZH2 inhibition studies.</p>

<p>PARP Protein, Human, Recombinant (His) is expressed in Baculovirus insect cells with His tag.</p>

<p>MI-3454: potent, oral menin-MLL1 inhibitor, IC50 of 0.51 nM, halts leukemia cells, aids remission in mice.</p>

<p>INO-1001: potent PARP inhibitor with antitumor properties, enhances radiosensitivity &amp; radiation-induced cell death.</p>

<p>Itacitinib adipate: oral JAK1 inhibitor, tested in phase II myelofibrosis trial.</p>

<p>Boc-Lys(Ac)-AMC (Boc-L-Lys(Ac)-AMC) is a synthetic substrate coupled to an HDAC-specific fluorophore (Ex/Em = 355 nm/460 nm).</p>

<p>PROTAC PARP1 degrader suppresses MDA-MB-231 cells at 10 μM, IC50: 6.12 μM in 24h.</p>