Chromatin/Epigenetics

<p>Delcasertib (KAI-9803) is a potent and selective inhibitor of δ-protein kinase C (δPKC).</p>

<p>Phenelzine sulfate is a non-selective and irreversible inhibitor of monoamine oxidase (MAOI), and with antidepressant and anxiolytic.</p>

<p>FIDAS-5 is an orally active methionine adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. Cost-effective and quality-assured.</p>

<p>NI-42, a BRPFs inhibitor: IC50(BRPF1/2/3)=7.9/48/260 nM, Kd(BRPF1/2/3)=40/210/940 nM; selective for class IV BRDs.</p>

<p>Pulrodemstat benzenesulfonate (CC-90011 benzenesulfonate) is a potent and orally inhibitor of lysine specific demethylase-1 (LSD1) with anticancer effect.</p>

<p>Miglitol (BAY1099) is an alpha-Glucosidase Inhibitor with antihyperglycemic activity.</p>

<p>BMS-986158: BET inhibitor, IC50 of 6.6 nM in SCLC, 5 nM in TNBC cells.</p>

<p>SJ10542: potent JAK2/3-targeting PG-PROTAC; DC50s: JAK2 - 14 nM, JAK3 - 11 nM, JAK2-fusion ALL - 24 nM; CRBN recruiter.</p>

<p>Fluorescein NAD+ is a non-radioactive PARP assay substrate, enabling direct enzyme measurement by fluorescence. Comes as 81μg in 250μl water.</p>

<p>PROTAC HDAC6 degrader4 (Compound 17c) is a PROTAC that targets and degrades HDAC6, with a DC50 of 14 nM. It exhibits inhibitory activity against HDAC1, HDAC2, HDAC3, and HDAC6, with IC50 values of 2.2, 2.37, 0.61, and 0.295 μM, respectively. [Pink: ligand for target protein HDAC6 ligand-3; Black: linker; Blue: ligand for cereblon E3 ligase]</p>

<p>AUR1545 is a selective KAT2A/KAT2B degradator exhibiting inhibitory activity against cancer models including AML, SCLC, and NEPC, and suppressing tumour growth in the NCI-H1048 xenograft model.</p>

<p>ZL0590 is an effective and selective inhibitor of BD1-BRD4 (IC50 = 90 nM) with anti-inflammatory activities.</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>CARM1/IKZF3 ligand 1 functions as an inhibitor of CARM1 and serves as a target protein ligand for the synthesis of PROTAC CARM1/IKZF3 degrader-1.</p>

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

<p>KDM1A-IN-29 is a histone demethylase inhibitor.</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>A unique collection of xnum DNA Damage &amp;amp; Repair related compounds for high throughput screening (HTS) and high content screening (HCS);</p>

<p>SAMS peptide is a specific substrate for the AMP-activated protein kinase (AMPK).</p>

<p>NP213 is a rapidly acting synthetic antimicrobial peptide (AMP).</p>

<p>Menin–KMT2A-IN-1 (Compound 20) is an inhibitor of menin–KMT2A, binding to menin with an IC50 of 8 nM, and disrupting the interaction between menin and lysine methyltransferase 2A (KMT2A). It inhibits hERG channels with an IC50 of 65 μM and suppresses MV4-11 cells with an IC50 of 74 nM. Furthermore, Menin–KMT2A-IN-1 exhibits favorable pharmacokinetic properties in CD-1 mice, with an oral bioavailability of 74%.</p>

<p>TCIP3 is a bivalent molecular glue (molecular glue) that can simultaneously bind to both p300/CBP and BCL6. It redirects p300 and CBP to activate programmed cell death genes, which are typically repressed by the oncogenic driver BCL6. TCIP3 is useful for studying diffuse large B-cell lymphoma (DLBCL) and is not toxic to untransformed tonsil lymphocytes or fibroblasts.</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>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>A unique collection of 2720 kinase inhibitors/regulators for high throughput screening and high content screening for drug discovery in kinase related diseases;</p>

<p>PROTAC BRD4 Degrader-5 is a PROTAC that degrades BRD4 in HER2 positive and negative breast cancer cell lines.</p>

<p>Pumecitinib is a Janus kinase (JAK) inhibitor. Pumecitinib exhibits anti-inflammatory activity.</p>

<p>Protein Kinase C (19-31), a PKC inhibitor derived from PKCa, has a serine at position 25 and tests PKC activity.</p>

<p>Hyp-dBET1 is a PROTAC degrader targeting BRD4, with an IC50 value of 3.4 μM in MDA-MB-231 cells. Under hypoxic conditions, Hyp-dBET1 becomes active, recruiting E3 ubiquitin ligase, and facilitates the degradation of BRD4 via the ubiquitin-proteasome system. Hyp-dBET1 is applicable in anti-cancer research.</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>HDAC6-IN-53 (Compound W28) is an inhibitor targeting histone deacetylase 6 (HDAC6) with an IC50 of 19.65 nM. It reduces the idiopathic pulmonary fibrosis (IPF) phenotype by inhibiting TGF-β1-induced collagen expression and demonstrates therapeutic efficacy in a bleomycin-induced mouse model of pulmonary fibrosis. HDAC6-IN-53 is applicable for research in idiopathic pulmonary fibrosis and related pulmonary fibrotic diseases.</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>Uzansertib (INCB053914) is a potent pan-PIM kinase inhibitor with low IC50s: 0.24, 30, 0.12 nM for PIM1, 2, 3; hinders hematologic tumor growth.</p>

<p>GSK8573 is an inactive control compound for GSK2801. GSK8573 has binding activity to BRD9 (Kd of 1.04 μM).</p>

<p>PROTAC BRD4 Degrader-19 (compound 176) is a proteolysis-targeting chimera (PROTAC) designed to specifically degrade the BRD4 protein, offering potential utility</p>

<p>BRD7-IN-1, a BI7273 derivative, transforms into PROTAC VZ185 (targets BRD7/9 with 4.5/1.8 nM DC50s) via a VHL linker.</p>

<p>GSK040: Potent BET BD2 inhibitor, pIC50 8.3, 5000x selectivity over BD1, for oncology &amp; immunology research.</p>

<p>SMD-3040 TFA is a selective SMARCA2 degrader comprising SMARCA2/4 ligands, a linker, and VHL ligands, utilized in PROTAC drug synthesis.</p>

<p>MNK/PIM-IN-1 is a novel dual inhibitor targeting both MNK and PIM pathways, characterized by its favorable pharmacokinetic profile.</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>MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology(Kd of 4 nM for Brd4BD2)</p>

<p>HIF-1 alpha (556-574) is a 19-mer fragment vital for gene expression in low oxygen; it binds VHL with critical proline 564 for stability.</p>

<p>CDD-1102 HCl is a novel BRDT-BD4 / BRD2-BD1302 selective inhibitor that shows non-hormonal contraceptive potential in ex vivo experiments.</p>

<p>MNN-02-155 is a bivalent molecular glue that can simultaneously interact with both p300/CBP and BCL6. It effectively induces the activation of BCL6-targeted reporter genes and promotes cell death. This compound is used in the research of diffuse large B-cell lymphoma (DLBCL).</p>

<p>CBP/p300-IN-8 strongly inhibits CBP/P300 bromodomains; CBP IC50=0.01-0.1μM, BRD4 IC50=1-1000μM.</p>

<p>HDAC11-IN-1 (Compound 14-NC6OH) is a macrocyclic inhibitor that selectively targets HDAC11 with a Ki of 40 nM. It demonstrates effective cell permeability and suppresses the expression of YAP1 and SOX2.</p>

<p>Axl-IN-16, a dual Axl/HIF inhibitor, promotes Flammulina velutipes fruiting body formation and suppresses hypoxia-inducible factor activity along with receptor</p>

<p>MS9024 is a degrader of DNA methyltransferase 1 (DNMT1), facilitating its degradation in HCT116 cells via the ubiquitin-proteasome pathway, with a DC50 of 35 nM (DC50 values are 254 nM in MDA-MB-468 and 101 nM in H1299). Additionally, MS9024 inhibits DNMT1 with an IC50 of 0.43 μM.</p>

<p>SNIPER(BRD)-1 has LCL-161, (+)-JQ1 linked; degrades BRD4, cIAP1/2, XIAP; IC50s: 6.8, 17, 49nM.</p>

<p>PRO-HD3 is a cell-specific, PROTAC-based degrader targeting HDAC6 [1].</p>

<p>XF067-68 is a PROTAC for targeted degradation of WD40 repeat domain protein 5 ( WDR5 )[1] .</p>

<p>KB02-JQ1: potent BRD4-degrading PROTAC, stable, specific; doesn't affect BRD2/3, modifies DCAF16 for action.</p>

<p>Namoline, a γ-pyrone, inhibits LSD1 with a 51 μM IC50, blocking cell growth and showing potential in prostate cancer studies.</p>

<p>Lyngbyatoxin A is an indole alkaloid from blue-green alga Lyngbya majuscula Gomont; responsible for dermatitis known as &amp;quot;swimmers' itch&amp;quot; in Hawaii.</p>

<p>PROTAC BET Degrader-3 is a potent degrader OF BET based on PROTAC.</p>

<p>MS33 degrades WDR5 protein, Kd 870 nM (VCB), 120 nM (WDR5); uses VHL ligase, aids acute myeloid leukemia study.</p>

<p>Okicenone is an antibiotic, interferring with HuR RNA binding, HuR trafficking, T-cell activation and cytokine expression.</p>

<p>PROTAC SMARCA2/4-degrader-28 (PROTAC 1) functions as a partial degrader of SMARCA2 and SMARCA4 through the PROTAC-based mechanism.</p>

<p>BAY-184,KAT6A/B inhibitor (IC50=71/83 nM). Suppresses ERα activity. Impedes breast cancer proliferation.</p>

<p>Vanicoside A is a protein kinase C( PKC ) inhibitor from Polygonum pensylvanicum [1] .</p>

<p>3β,6α,12β-Dammar-E-20(22)-ene-3,6,12,25-tetraol is a compound that functions as a SIRT1 activator, effectively enhancing SIRT1 activity.</p>

<p>Compound 8b, a dual-ligand PROTAC, targets VHL &amp; BRD4, degrades BRD4 in PC3 cells; conjugates with STEAP1/CLL1, DC50: 1.3/18 nM.</p>

<p>R 8605 is a third-generation retinoid.</p>

<p>GSK3735967: DNMT1 inhibitor, IC50 40 nM, dicyanopyridine core, binds hemimethylated CpG, interacts with H4K20me3.</p>

<p>ZMF-23, a PAK1/HDAC6 dual inhibitor, suppresses PAK1 and HDAC6-mediated aerobic glycolysis and cellular migration while inducing TNF-α-regulated necroptosis and</p>

<p>DS-103 is an HDAC inhibitor that targets HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 with IC50 values of 0.029, 0.123, 0.022, 0.367, and 9.26 μM, respectively. It also inhibits the malignant malaria parasite [Plasmodium falciparum 3D7] with an IC50 of 5.08 μM. In A2780 and Cal27 cells, DS-103 exhibits cytotoxicity with IC50 values of 1.48 μM and 1.47 μM, respectively, and reverses cisplatin resistance in these cells with IC50 values of 4.62 μM and 2.23 μM. DS-103 acts synergistically with cisplatin, enhancing apoptosis induced by cisplatin.</p>

<p>HIV-1 protease-IN-10 (Compound 2), exhibiting HIV-1 latency reversing activity (IC50: 0.22 μM), selectively binds to the PKCδ C1b domain (IC50: 0.69 μM) and</p>

<p>Blocks HIF-1α/β dimerization, not HIF-2α; suppresses VEGF, CAIX in cancer cells; antiangiogenic in HUVECs (IC50 = 1.3 μM).</p>

<p>PROTAC BRD4 Degrader-13 targets VHL and BRD4, degrading BRD4 with DC50 of 0.025/6.0 nM in PC3 cells when linked to STEAP1/CLL1 antibodies.</p>

<p>Antidiabetic agent 7 (Compound 5m) functions as a potent hyperglycemia inhibitor. It effectively stimulates GLUT4 translocation in skeletal muscle cells by activating the AMPK-dependent pathway. Additionally, this compound is capable of reducing blood glucose levels and exhibits favorable pharmacokinetic properties. Antidiabetic agent 7 is suitable for research related to antihyperglycemic treatments.</p>

<p>Dihydrochlamydocin, an inhibitor of histone deacetylases (HDAC), exhibits potent cytostatic activity against mastocytoma cells.</p>

<p>UNC2399, a biotinylated version of UNC1999, functions as a selective degrader of EZH2 and exhibits strong in vitro efficacy against EZH2, demonstrated by its IC</p>

<p>AB3067 is a PROTAC degrader targeting BET protein, efficiently recruiting two distinct E3 ligases, Cereblon and VHL, with strong affinity (demonstrated by IC50 values of 559 nM for VHL and 190 nM for CRBN in vivo HEK293). It degrades BRD2, BRD3, BRD4, and CRBN with DC50 values of 2.1~2.3, 1.6, 15, and 75 nM, respectively. Additionally, AB3067 inhibits the proliferation of RKO cells, with an EC50 of 111 nM. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase VHL and CRBN)</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 unique collection of 252 JAK/STAT signaling targeted compounds for high throughput and high content screening;</p>

<p>CW-3308 is an orally active PROTAC that targets BRD9. It is composed of the PROTAC target protein ligand Naphthyridin-Me-dimethoxybenzene-COOH, the linker 3-Azaspiro[5.5]undecane-9-methanol, and the E3 ubiquitin ligase ligand Thalidomide-methylpyrrolidine. The coupling of the E3 ubiquitin ligase ligand with the linker results in the conjugate Thalidomide-pyrrolidine-C-azaspiro.</p>

<p>SW2_110A acetate is a selective, cell-permeable chromobox inhibitor of homologue CBX8 (Kd = 800 nM) bound to CBX8 N-terminal color gamut (ChD).</p>

<p>JQ-1 (carboxylic acid)-NH-C2-NH-AMPRO-222 incorporates a BRD4 ligand and a PROTAC linker, and is used in the synthesis of PROTAC BRD4 Degrader-29.</p>

<p>AZD1152 is a pro-drug of Barasertib (AZD1152)-hQPA. Which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.</p>

<p>WDR5ligand 2 is a ligand for WDR5 and can be utilized in the synthesis of PROTAC WDR5degrader 1.</p>

<p>PROTAC BRD4 Degrader-9 degrades BRD4 in PC3 cells; binds VHL and BRD4; DC50: STEAP1-0.86 nM, CLL1-7.6 nM.</p>

<p>BRD4 degrader-6 is a dimeric BDR4PROTAC class degrader with a DC50 of less than 0.1 μM. It effectively induces the ubiquitination and degradation of BDR4, exhibiting anticancer properties.</p>

<p>MS049 inhibits PRMT4 (IC50=34nM) &amp; PRMT6 (IC50=43nM), less so for PRMT1, PRMT3, PRMT8, not others.</p>

<p>ZXH-3-26 is a PROTAC composed of a Cereblon ligand, an E3 ubiquitin ligase, and a BRD4 ligand that can be used to study cancer.</p>

<p>PRMT5-IN-12 shows remarkable inhibitory activity on PRMT5 .</p>

<p>PI3Kα/HDAC6-IN-1 (compound 21j) is a dual inhibitor of PI3Kα and HDAC6, exhibiting IC50 values of 2.9 nM and 26 nM, respectively.</p>

<p>Sirtuin modulator 5 activates SIRT1 (&lt;50 μM DC50), may extend cell lifespan, and could aid in researching various age/stress-related diseases.</p>

<p>MAK683 hydrochloride is an inhibitor of embryonic ectoderm development (EED), with IC50 values of 59, 26nM measured in EED Alphascreen, ELISA.Cost-effective and quality-assured.</p>

<p>GSK9311 hydrochloride is a less active GSK6853 analog, serving as a negative control, inhibiting BRPF1/2 (pIC50: 6.0/4.3).</p>

<p>Thalidomide-NH-CBP/p300 ligand 2 (P-007) is a PROTAC-based compound designed to degrade CBP and p300, acting as a functional antagonist (WO2020173440).</p>

<p>SR-0813 is a potent and selective inhibitor of the YEATS domain in ENL/AF9.</p>

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

<p>PROTACBRD4 degrader-30 is an ISOX-DUAL-based PROTAC degrader, targeting BRD4 with an IC50 value of 65 nM. It is used in research studies related to c-Myc oncoproteins and the pathophysiology of cancer cells.</p>

<p>Anemonin, a furanone dimer from Buttercups, may help manage melanocytes and osteoarthritis.</p>

<p>GNE-987 is a potent chimeric BET degrader, binding BRD4 BD1/BD2 at IC50: 4.7/4.4 nM &amp; has a DC50: 0.03 nM in EOL-1 AML cells.</p>

<p>MRS2698: potent P2Y2 agonist, EC50 8 nM, &gt;300x selectivity over P2Y4/P2Y6.</p>

<p>PROTAC SMARCA2/4-degrader-25 is a PROTAC that targets SMARCA2/4. It consists of the E3 ligase ligand (2S,4R)-4-Hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide, a PROTAC Linker (S)-2-Amino-3,3-dimethylbutanoic acid, and the target protein ligand SMARCA2/4-ligand-3. The conjugate of the E3 ubiquitin ligase ligand and Linker is (S,R,S)-AHPC.</p>

<p>PF-04577806: potent &amp; selective PKC inhibitor, ATP competitive, blocks PKCα/βI/βII/γ/θ (IC50: 2.4-45.9 nM), may reverse diabetic retinal leakage.</p>

<p>JB300 is a PROTAC-based compound that serves as a highly selective degrader of Aurora A, with a DC50 of 30 nM. It is utilized in cancer research. JB300 comprises the PROTAC target protein ligand MK-5108 [pink part], E3 ligase ligand Thalidomide-O-COOH [blue part], and PROTAC Linker Boc-NH-PEG2-C2-NH2 [black part]. The conjugate of the E3 ubiquitin ligase ligand and linker is Thalidomide-O-COOH-NH2-C2-PEG2-NH-Boc.</p>

<p>EXQ-2d is an inhibitor of tankyrase, effectively targeting TNKS1 and TNKS2 with IC50 values of 48.8 nM and 13.8 nM (pIC50=7.31 and 7.86), respectively. Additionally, EXQ-2d suppresses the WNT/β-catenin signaling pathway with an IC50 of 515 nM. It demonstrates antiproliferative activity in cancer cells COLO 320DM and RKO, with GI50 values of 4.9 μM and 77 μM, respectively.</p>