Chromatin/Epigenetics

Protein kinase C (PKC) activator

CAM2602 is an inhibitor of Aurora A-TPX2 interaction, demonstrating a binding affinity of 19 nM with Aurora A. This compound has been shown to inhibit the growth of pancreatic cancer cells. In solid tumor xenograft models, CAM2602 increases the proportion of PH3-positive cells while decreasing the ratio of P-Thr288Aurora A-positive cells, ultimately inhibiting tumor growth.

dBRD9 is a PROTAC.

SAHA inhibits class I/II HDAC; c-SAHA, a fluorescent derivative, excites at 325 nm and emits at 400 nm.

PROTAC BET Degrader-1 is a potent degrader of BET based on PROTAC.

Fibrostatin C is an inhibitor of prolyl 4-hydroxylase. It is produced by Streptomyces catenulae subsp.

LSQ-28 is an orally active HDAC3 inhibitor with an IC50 of 42 nM, demonstrating significant anticancer, antiproliferative, anti-migration, anti-invasion, and anti-wound healing activities. LSQ-28 is suitable for cancer research.

Strong PRMT5 inhibitor with 4 nM IC50, surpassing other PRMTs; halts MCL growth in lab tests.

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.

PROTAC SMARCA2 degrader-23 (Example 1) is an effective and selective degrader of PROTAC SMARCA2, with a DC50 value of less than 100 nM. It has potential for use in cancer research.

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

PRMT5-IN-12 shows remarkable inhibitory activity on PRMT5 .

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.

PF-3166 (compound PF-3166) is a cell-active inhibitor of PAD2.

dAurAB2 is a bifunctional PROTAC capable of effectively degrading Aurora-A and Aurora-B, with DC50 values of 59 nM and 39 nM, respectively. It reduces N-Myc levels in MYCN-amplified IMR32 neuroblastoma cells and is valuable for neuroblastoma research.

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.

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

PROTACBRD4 Degrader-38 is a BRD4 PROTAC degrader with DC50 values of 86 nM and 106 nM for the short and long BRD4 isoforms, respectively. It significantly induces BRD4 degradation through covalent binding at the C232 site of the E3 ligase TRIM28.

PROTAC MPS1 degrader 1 (Compound 19) acts as a potent degrader of Monopolar spindle 1 (Mps1, TTK), AURKA, and AURKB, with DC50 values of 17.7, 108.7, and 570.3 nM respectively. It is utilized in the study of acute myeloid leukemia. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase)

PROTAC BRD4 Degrader-28 (Compound 4) is a PROTAC degrader specifically targeting BRD4, and it holds potential for cancer research.

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

Go6976 is a PKC inhibitor, widely used in research to probe PKC functions in health and disease.

BT-O2C is a highly selective p300 PROTAC degrader that effectively reduces p300 levels in HAP1 cells. It exhibits significant cytotoxicity in CIC:DUX4 sarcoma (CDS) cell lines, with an IC50 of 152-221 nM, and notably decreases the expression of CDS target genes (ETV1, ETV4, ETV5). BT-O2C is applicable in cancer research.

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

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

Dot1L-IN-1 TFA: potent inhibitor, K i =2 pM, IC 50 <0.1 nM; reduces H3K79 dimethylation (IC 50 =3 nM) & HoxA9 promoter activity (IC 50 =17 nM).

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%.

PROTAC BRD4 Degrader-12 targets BRD4 in PC3 cells; conjugates with STEAP1, CLL1; DC50: 0.39/0.24 nM.

Synthetic peptide analog of bovine myelin basic protein (MBP). Non-competitive inhibitor of PKC (IC50 = 46 - 145 mM).

Echinomycin (Quinomycin A) is a quinoxaline antibiotic and a DNA-intercalating peptide that inhibits hypoxia-inducible factor-1 (HIF-1) DNA binding activity.

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.

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%.

Sphingosine (d14:1) boosts N. rileyi fungus growth, inhibits PKC, and reduces CHO cell proliferation; found in various sea creatures.

Tubulin/HDAC-IN-3 (compound 12a) serves as a potent dual inhibitor of tubulin polymerization and HDAC1/8, exhibiting IC50 values of 5.4 μM for tubulin

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.

M 1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression.

EZH2-IN-5, potent EZH2 inhibitor; IC50: 1.52 nM (wild-type), 4.07 nM (Tyr641 mutant).

CP 46665 is a bio-active chemical.

PKC β pseudosubstrate TFA is a selective cell-permeable inhibitor of PKC [1] .

MMH2 is a novel molecular glue degrader targeting BRD4 by facilitating the recruitment of CUL4 and DCAF16 ligases to BRD4's second bromodomain (BRD4 BD2) [1].

EEDi-5285: potent EED inhibitor, orally active, IC50=0.2nM, targets EED protein, anti-cancer properties.

BET BD2-IN-1 (compound 45) is a potent, selective inhibitor of BET BD2, exhibiting an IC50 value of 1.6 nM.

I-BET432, a BET inhibitor, blocks BRD4 BD1/BD2 (pIC50: 7.5/7.2), is oral, and targets cancer/inflammation.

EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).

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.

BRD4-IN-4 is a selective BRD4 inhibitor with an IC50 value of 6.83 μM for BRD4.BRD4-IN-4 selectively inhibits the proliferation of the MV4-11 cell line and

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

MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology(Kd of 4 nM for Brd4BD2)

Thalidomide-piperidine-C-Pip-C2-Pip-C2-OH (Compound C6) is a conjugate linking a ligand and an E3 ligase, which is utilized in the synthesis of PROTAC PARP1 degrader-30.

SW2_152F: Potent CBX2 ChD inhibitor, Kd 80 nM, 24-1000x selective over other CBXs in vitro.

CPI-268456 is a compound which has bioactive.

PCAF-IN-1 is a highly selective PCAF inhibitor with potential anti-tumor, anti-inflammatory, and anti-heart disease effects.

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

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

TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor (Kd: 134 nM and 5.02 μM for CBP and BRD4).

KDM4C-IN-1 is aKDM4C inhibitor withial anticancer activity.KDM4C-IN-1 inhibits the growth of HepG2 and A549 cells, and can be used for the study of leukaemia.

GSK778 selectively inhibits BD1 bromodomains (BRD2, BRD3, BRD4, BRDT) and impedes cell growth, causing arrest and apoptosis.

DTP3 is a selective MKK7/GADD45β inhibitor, which inhibits cancer-selective NF-κB survival pathway.

(2R)-Octyl-α-hydroxyglutarate ((2R)-Octyl-2-HG) is a D-isomer 2-Hydroxyglutarate modified form.

SGC-iMLLT is a potent and selective MLLT1/3-histone interactions inhibitor(IC50 = 0.26 μM),and is a first-in-class chemical probe displaying cellular target

EHMT2-IN-1: potent EHMT inhibitor, for blood disorders/cancer research; IC50s <100 nM for EHMT1/2 peptides and cellular EHMT2.

Eicosapentaenoic Acid (Standard) is the standard substance of Eicosapentaenoic Acid, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Eicosapentaenoic Acid is an ω-3 fatty acid and an inhibitor of fatty acid synthase (FASN). Eicosapentaenoic Acid promotes DNA demethylation in the reexpression of the tumor suppressor gene CCAAT/ enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates the RAS/ERK/C/EBPβ pathway in U937 leukemia cells through demethylation of the CpG island of H-RAS intron 1. Eicosapentaenoic Acid promotes the relaxation of vascular smooth muscle cells and vasodilation.

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.

GSK2879552: oral, irreversible LSD1 inhibitor with potential cancer-fighting properties.

Itacitinib adipate: oral JAK1 inhibitor, tested in phase II myelofibrosis trial.

AZ505 ditrifluoroacetate is an effective and selective SMYD2 inhibitor (IC50: 0.12 μM).

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

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

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).

GSK9311 inhibits BRPF bromodomain (pIC50: 6.0 and 4.3 for BRPF1 and BRPF2, respectively).

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

ADTL-SA1215 is a SIRT3 activator with SIRT3 deacetylase activity for the study of triple negative breast cancer.

PR5-LL-CM01 is a novel protein arginine methyltransferase 5 (PRMT5) inhibitor in colorectal and pancreatic cancers.

MC4171 is a selective KAT8 inhibitor with antiproliferative activity and can be used to study cancer.

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.

JET-209 is a potent proteolysis-targeting chimera (PROTAC) that effectively degrades CBP/p300, exhibiting half-maximal degradation concentration (DC50) values

Atinvicitinib, a selective JAK1 inhibitor, blocks cytokine signaling, modulating itch, allergy, and inflammatory responses, immune and therapeutic studies.

2'-Deoxy-2'-fluoro-beta-D-arabinocytidine HCl inhibits DNA methyltransferase with potential anti-tumor properties.

Orally active Pim-1/2 inhibitor blocks kinase phosphorylation; used in prostate cancer research.

PKC-theta inhibitor is PKC-θinhibitor, with an IC50 of 12 nM.

HDAC-IN-4 is a selective HDAC6 and HDAC10 inhibitor (pIC50s: 7.2 and 6.8 in BRET assay) with antitumoral activity.

Protein kinase inhibitor H-7 dihydrochloride(H-7 dihydrochloride) is a potent protein kinase C (PKC) inhibitor.

MS8511 hydrochloride is a selective G9a/GLP inhibitor with IC50 values of 100 nM and 140 nM respectively, exhibiting covalent and irreversible characteristics.

SIRT5 inhibitor 3 is potent and competitive by inhibiting SIRT5 deacetylation, with potential in metabolic, cancer, neurodegenerative, cardiovascular .

(±)-1,2-Diolein (1,2-Dioleoyl-rac-glycerol) (1,2-Dioleoyl-rac-glycerol) is a PKC activator. (±)-1,2-Diolein could increases myotubes Ca 2+ influx.

O6BTG-octylglucoside is a potent O6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor (IC50s: 10 nM and 32 nM in HeLa S3 cells and in vitro (cell extracts)).

Ilunocitinib is a non-selective and orally active Janus kinase (JAK) inhibitor for pruritus and atopic dermatitis caused by atopic dermatitis in dogs.

GSK-J2 is an inactive enantiomer of GSK-J1 that is lipophilic and serves as an inactive control for GSK-J21.

DA-3003-1 (NSC 663284) is a Cdc25 dual specificity phosphatase inhibitor with antitumor activity and inhibits Cdc25B2, Cdc25A, Cdc25B2, and Cdc25C.

BAY-850 is ainhibitor of adenosine triphosphatase family protein 2 that inhibits ovarian cancer growth and metastasis in in vitro and in vivo models.

SIRT-IN-3: potent SIRT1 inhibitor (IC50=17μM), 4x selective over SIRT2, 14x over SIRT3 (IC50s: 74μM & 235μM).

CHZ868 is a type II JAK inhibitor with potential antitumor activity that reverses the persistence of type I JAK inhibitors and can be used to study leukemia.

1,4-DPCA ethyl ester is a form of 1,4-DPCA modified, which has potential anticancer activity based on growth inhibition assays with the mlh1 rad18 yeast strain.

Fenbendazole-d3 is a deuterated compound of Fenbendazole. Fenbendazole has a CAS number of 43210-67-9. Fenbendazole is an antinematodal benzimidazole used in veterinary medicine.

Anti-PARP1 Antibody (8I163) is a Mouse antibody targeting PARP1. Anti-PARP1 Antibody (8I163) can be used in IHC-P.

Anti-PARP Antibody (1W26) is a Mouse antibody targeting PARP. Anti-PARP Antibody (1W26) can be used in WB,IHC-P,IP.

Anti-PARP1 Antibody (6I459) is an antibody targeting PARP1. Anti-PARP1 Antibody (6I459) can be used in ELISA, IHC.

Anti-PARP1 Antibody (7A800) is an antibody targeting PARP1. Anti-PARP1 Antibody (7A800) can be used in ELISA, WB, IHC.