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chromatin binding

" in MedChemExpress (MCE) Product Catalog:

33

Inhibitors & Agonists

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3

Recombinant Proteins

2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N0005
    Curcumin
    120+ Cited Publications

    Diferuloylmethane; Natural Yellow 3; Turmeric yellow

    Histone Acetyltransferase Epigenetic Reader Domain Keap1-Nrf2 Autophagy Mitophagy Influenza Virus Ferroptosis Apoptosis Infection Metabolic Disease Inflammation/Immunology Cancer
    Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
    Curcumin
  • HY-136521

    Epigenetic Reader Domain Cancer
    AZ13824374 is a potent and selective ATAD2 bromodomain inhibitor (pIC50 of 6.9 in HCT116 cells). AZ13824374 disrupts chromatin interactions and gene transcription by binding to the acetyl-lysine binding site of the ATAD2 bromodomain. AZ13824374 has anticancer activity against breast cancer .
    AZ13824374
  • HY-N0005R
    Curcumin (Standard)
    1 Publications Verification

    Diferuloylmethane (Standard); Natural Yellow 3 (Standard); Turmeric yellow (Standard)

    Reference Standards Histone Acetyltransferase Epigenetic Reader Domain Keap1-Nrf2 Autophagy Mitophagy Influenza Virus Ferroptosis Infection Neurological Disease Inflammation/Immunology Cancer
    Curcumin (Standard) is the analytical standard of Curcumin (HY-N0005). This product is intended for research and analytical applications. Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
    Curcumin (Standard)
  • HY-168534

    SF3B1 Apoptosis Cancer
    WX-02-23 is a small-molecule probe that stereoselectively and site-specifically binds to C258 of FOXA1 and C1111 of SF3B1. WX-02-23 remodels FOXA1's chromatin binding and pioneer activity in a DNA-dependent manner, disrupts spliceosome assembly, and enhances the thermal stability of SF3B1. WX-02-23 inhibits tumor cell proliferation and induces apoptosis. WX-02-23 can be used for research on cancers such as prostate cancer .
    WX-02-23
  • HY-13032B
    Molibresib besylate
    20+ Cited Publications

    GSK 525762C; I-BET 762 besylate

    Epigenetic Reader Domain ERK Cancer
    Molibresib besylate (GSK 525762C; I-BET 762 besylate) is an orally active pan-BET inhibitor that targets and binds to BRD2, BRD3, BRD4 and BRDT. By competitively occupying acetylated lysine binding sites, Molibresib besylate disrupts the interaction between BET proteins and chromatin, thereby effectively inhibiting MYC expression and target gene transcription. Molibresib besylate exhibits broad antiproliferative activity, which not only inhibits cancer cell growth and induces growth arrest, but also downregulates mitosis-related genes and upregulates the level of p-ERK1/2. When combined with MEK inhibitors, Molibresib besylate shows a significant synergistic effect, reduces tumor burden in mouse models of leukemia, modulates the immune microenvironment and prolongs survival. Molibresib besylate is widely applicable to research related to acute myeloid leukemia, multiple myeloma, triple-negative breast cancer, small-cell lung cancer and various advanced refractory solid tumors .
    Molibresib besylate
  • HY-112589

    Bacterial Infection Cancer
    BRITE-338733 is an inhibitor of E. coli RecA ATPase activity (IC50: 4.7 μM). BRITE-338733 also inhibits the ATP hydrolysis activity of RSC chromatin remodeling enzyme by binding to its ATP-binding pocket and DNA (IC50: 0.316 μM). BRITE-338733 exhibits cytotoxicity against MCF-7 and MDA-MB-231 breast cancer cells. BRITE-338733 can be used in studies on antibacterial adjuvants and anticancer research .
    BRITE-338733
  • HY-124012

    DNA/RNA Synthesis Apoptosis Cancer
    PCNA-I1 is a selective small molecule inhibitor targeting proliferating cell nuclear antigen (PCNA) with anticancer activity. PCNA-I1 can stabilize the PCNA trimer structure (Kd=0.14-0.41μM), reduce its binding to chromatin, induce tumor cell cycle arrest, inhibit DNA replication and repair, and enhance the anti-tumor effect of DNA damaging agents. PCNA-I1 can be used in the study of targeted therapy for prostate cancer, lung cancer and other tumors .
    PCNA-I1
  • HY-19553

    Epigenetic Reader Domain Inflammation/Immunology
    LP99, an epigenetic probe, is a potent and selective inhibitor of the BRD7 and BRD9 bromodomains with a Kd of 99 nM against BRD9. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells .
    LP99
  • HY-126428
    ZL0580
    1 Publications Verification

    HIV Epigenetic Reader Domain Infection Inflammation/Immunology
    ZL0580, a structurally close analog of ZL0590, induces epigenetic suppression of HIV via selectively binding to BD1 domain of BRD4. ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter .
    ZL0580
  • HY-116501

    Androgen Receptor Cancer
    VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD), with IC50 of 0.34 μM for full-length human AR. VPC-14449 reduces the ability of full-length AR as well as AR variants to interact with chromatin. VPC-14449 can be used for the research of prostate cancer .
    VPC-14449
  • HY-161409

    Androgen Receptor Apoptosis Cancer
    SC912 is an AR-V7 inhibitor (IC50 = 0.36 μM). SC912 possesses safety, potency and selectivity. SC912 binds directly to AR-FL and AR-V7 proteins, inhibites nuclear localization and chromatin binding capabilities. SC912 exerts anticancer activity through inhibition of proliferation, induction of cell cycle arrest and apoptosis .
    SC912
  • HY-117669

    Androgen Receptor Cancer
    VPC-14228 is an inhibitor that selectively targets androgen receptor DNA binding domain (AR-DBD). VPC-14228 inhibits the interaction between AR and DNA, thereby blocking AR-mediated transcriptional activation. VPC-14228 does not rely on nuclear localization inhibition, but rather inhibits the activity of full-length AR and splice variant AR-V7 by interfering with AR binding to chromatin. And VPC-14228 has high selectivity for other nuclear receptors such as ER and PR. VPC-14228 can be used in the study of prostate cancer [2].
    VPC-14228
  • HY-157251

    Histone Methyltransferase Cancer
    UNC8153 TFA is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 TFA reduces the cellular levels of both NSD2 protein (DC50 in cell U2OS is 0.35 μM) and the H3K36me2 chromatin mark. UNC8153 TFA contains a simple warhead that confers proteasome-dependent degradation of NSD2 .
    UNC8153 TFA
  • HY-116940
    Sm4
    1 Publications Verification

    Oct3/4 Notch STAT Cancer
    Sm4 is a selective and orally active SOX18 inhibitor. Sm4 inhibits SOX18-DNA binding (IC50 = 97.5 μM); Sm4 disrupts the SOX18-RBPJ protein-protein interaction (IC50 = 42.3 μM). Sm4 blocks SOX18 DNA binding, disrupts multiple SOX18 protein-protein interactions with RBPJ, DDX1, DDX17, ILF3, SOX7 and STAT1, modulates SOX18 chromatin binding dynamics. Sm4 exerts anti‑angiogenic and anti‑lymphangiogenic effects, reduces tumor vascular density, triggers vascular defects in zebrafish, prolongs survival in mouse metastatic cancer models. Sm4 can be used for the research of breast cancer .
    Sm4
  • HY-N0005S

    Diferuloylmethane-d6; Natural Yellow 3-d6; Turmeric yellow-d6

    Isotope-Labeled Compounds Keap1-Nrf2 Ferroptosis Autophagy Histone Acetyltransferase Epigenetic Reader Domain Mitophagy Influenza Virus Infection Metabolic Disease Inflammation/Immunology Cancer
    Curcumin-d6 (Diferuloylmethane-d6 ) is deuterium labeled Curcumin (HY-N0005). Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
    Curcumin-d6
  • HY-148739

    PROTACs Epigenetic Reader Domain Apoptosis Cancer
    dBRD 9-A is a selective BRD9 PROTAC degrader. dBRD 9-A induces near complete BRD9 degradation dependent on E3 ubiquitin ligase CRBN and BRD9 bromodomain engagement, and drives loss of BRD9 chromatin binding genome-wide. dBRD 9-A downregulates oncogenic SS18-SSX-driven transcriptional programs, super enhancer-associated gene expression, and SS18-SSX1 super enhancer binding, and depletes GBAF complex members GLTSCR1/1L from SS18-SSX complexes. dBRD 9-A induces cell cycle arrest and increases apoptosis in synovial sarcoma cells. dBRD 9-A can be used for the research of synovial sarcoma .
    dBRD 9-A
  • HY-123621

    Epigenetic Reader Domain Cancer
    GNE-375 is a potent and highly selective BRD9 inhibitor with an IC50 of 5 nM. GNE-375 shows >100-fold selective for BRD9 over BRD4, TAF1, and CECR2. GNE-375 decreases BRD9 binding to chromatin .
    GNE-375
  • HY-116818

    HDAC Neurological Disease
    Crebinostat is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.7 nM, 1.0 nM, 2.0 nM and 9.3 nM for HDAC1, HDAC2, HDAC3 and HDAC6, respectively. Crebinostat potently induces acetylation of both histone H3 and histone H4 as well as enhances the expression of the cAMP response element-binding protein (CREB) target gene Egr1. Crebinostat increases the density of synapsin-1 punctae along dendrites in cultured neurons. Crebinostat can modulate chromatin-mediated neuroplasticity and exhibits enhanced memory in mice .
    Crebinostat
  • HY-157251A

    Histone Methyltransferase Cancer
    UNC8153 is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 reduces the cellular levels of both NSD2 protein (DC50 in cell U2OS is 0.35 μM) and the H3K36me2 chromatin mark. UNC8153 contains a simple warhead that confers proteasome-dependent degradation of NSD2 .
    UNC8153
  • HY-164373

    Androgen Receptor Apoptosis Cancer
    SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1 .
    SC428
  • HY-160267

    HIV DNA/RNA Synthesis Infection Neurological Disease Cancer
    iPAF1C is a inhibitor of the polymerase-associated factor 1 complex (PAF1C) with specific targeting to the PAF1 binding groove of CTR9 (a key subunit of PAF1C). iPAF1C disrupts PAF1C assembly by interfering with the PAF1-CTR9 interaction. iPAF1C selectively impairs BRD4-mediated recruitment of PAF1 to chromatin at hypoxia-responsive genes and inhibits RNA polymerase II (RNAPII) pause release. iPAF1C increases the population of HIV-1 NL4.3 Nef-IRES-GFP infected primary human CD4 +T cells in a dose-dependent manner. PAF1C can be used for the study of infection and diseases associated with abnormal hypoxic adaptation (e.g., cancers, neurological disorders) .
    iPAF1C
  • HY-161483

    Epigenetic Reader Domain Histone Acetyltransferase Neurological Disease Cancer
    CBP/p300 ligand 3 is a target protein ligand of CBPD-268 (HY-161369). CBP and p300 are two proteins with histone acetyltransferase (HAT) activity, and CBP and p300 play key roles in regulating biological processes such as gene expression, cell proliferation, differentiation and DNA repair. Through its acetyltransferase activity, CBP/p300 can acetylate histones and other proteins, thereby regulating chromatin structure and gene expression. CBP/p300 ligand 3 regulates the function of CBP/p300 by binding to a specific domain of the CBP/p300 protein (the bromine domain or HAT domain), inhibiting its enzyme activity or altering its interactions with other proteins (transcription factors). CBP/p300 ligand 3 can be used in cancer, neurodegenerative diseases and other disease models associated with abnormal CBP/p300 function .
    CBP/p300 ligand 3
  • HY-161391

    CRM1 Cancer
    CW0134 (Compound 12) is a modulator for exportin1 (XPO1) ,which disrupts the chromatin binding, inhibits NFAT transcription factors and activation of T cells .
    CW0134
  • HY-120907

    SF3B1 Cancer
    Sudemycin E is an analog of FR901464 (HY-16212). Sudemycin E can induce reversible changes in alternative splicing and abnormalities in chromatin modifications by binding to SF3B1, a component of the U2 small nuclear ribonucleoprotein (snRNP), thereby leading to the death of cancer cells. Sudemycin E has anti-tumor activity and can be used in tumor research .
    Sudemycin E
  • HY-N0005S1

    Diferuloylmethane-d3; Natural Yellow 3-d3; Turmeric yellow-d3

    Isotope-Labeled Compounds Autophagy Histone Acetyltransferase Keap1-Nrf2 Influenza Virus Mitophagy Epigenetic Reader Domain Ferroptosis Infection Metabolic Disease Inflammation/Immunology Cancer
    Curcumin-d3 (Diferuloylmethane-d3 ) is deuterium labeled Curcumin (HY-N0005). Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
    Curcumin-d3
  • HY-161392

    CRM1 Cancer
    CW2158 (Compound 13) is a modulator for exportin1 (XPO1) ,which disrupts the chromatin binding, inhibits NFAT transcription factors and activation of T cells .
    CW2158
  • HY-141551

    Estrogen Receptor/ERR Cancer
    GNE-274 is a structural analog of the ER degrader GDC-0927 and is a non-degrader. GNE-274 does not induce conversion of ER in breast cancer cell lines and functions as a partial ER agonist (partial ER agonist). GNE-274 increases the chromatin accessibility of ER-DNA binding sites, whereas GDC-0927 does not. GNE-274 is an effective ER ligand binding domain (LBD) inhibitor. GNE-274 can be used in cancer research.
    GNE-274
  • HY-151153

    HDAC Microtubule/Tubulin Caspase Apoptosis Cancer
    HDAC1-IN-5 is a potent HDAC1 inhibitor with IC50 values of 15 nM and 20 nM for HDAC1 and HDAC6, respectively. HDAC1-IN-5 can enhance the acetylation of histone H3 and α-tubulin, as well as promote the activation of caspase 3 in cancer cells, thereby inducing apoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitory activity against tumor growth in xenograft mice .
    HDAC1-IN-5
  • HY-183622

    MDM-2/p53 Cancer
    UCI-1014 is a mutant p53 (p53 R175H) corrector/reactivator. UCI-1014 restores the wild-type-like DNA-binding activity of p53 R175H, promotes the redistribution of the mutant protein to chromatin, and induces the expression of p53-dependent target genes. UCI-1014 inhibits the proliferation of p53 R175H-mutant cancer cells through an SLC7A11-independent mechanism. UCI-1014 can be used for research related to p53-mutant cancers .
    UCI-1014
  • HY-181421

    SF3B1 Cancer
    WX-02-43 is a weak covalent inhibitor of SF3B1, and is the (1S,3R) enantiomer of WX-02-23 (HY-168534). WX-02-43 cannot effectively covalently modify the C258 site in the DNA-binding domain of FOXA1, and its inhibitory activity against SF3B1 is also weaker than that of WX-02-23. WX-02-43 serves as a negative control probe that fails to remodel the chromatin binding pattern and transcriptional activity of FOXA1. WX-02-43 can be used in studies on cancers such as prostate cancer to verify the specific effects of WX-02-23 on FOXA1 and SF3B1 targets .
    WX-02-43
  • HY-182037

    DNA/RNA Synthesis Pyruvate Kinase Cancer
    Multi-target kinase-IN-9 is a multi-target enzyme inhibitor with antiproliferative and antiangiogenic activities, and exhibits remarkable selectivity against hepatocellular carcinoma cells. By broadly binding to the active sites or ATP-binding regions of multiple key enzymes including DNA polymerase β, Pyruvate Kinase M2 (PKM2), Multi-target kinase-IN-9 comprehensively disrupts DNA repair and replication, glycolysis, chromatin dynamics and transcriptional programs, and blocks the self-renewal of cancer stem cells. Multi-target kinase-IN-9 induces genomic instability, lysosomal dysfunction and autophagic flux impairment, thereby triggering tumor cell death, effectively inhibiting tumor proliferation, invasion, metastasis and angiogenesis, and significantly reducing tumor volume in xenograft models. Multi-target kinase-IN-9 is applicable to hepatocellular carcinoma-related research .
    Multi-target kinase-IN-9
  • HY-P11137

    HSV Cancer
    LANA is a KSHV latency-associated nuclear antigen. The core function of LANA is to act as an "anchor" for the viral genome, attaching it to the chromatin of the host cell. LANA ensures that the episomal DNA of KSHV replicates together with the host chromosome and is evenly distributed among the daughter cells, thereby maintaining the latent infection of the virus in the cell population. LANA can regulate the transcription of viral and host cell genes, and regulate certain host cell genes to promote cell survival. LANA can be used to study the viral DNA tethering structure .
    LANA
  • HY-107446

    Ligands for Target Protein for PROTAC Epigenetic Reader Domain Others
    BI-7273 acid, BI-7273 (HY-100351) derivative, is a BRD9 PROTAC ligand. BI-7273 acid can be conjugated with E3 ligase Ligand Thalidomide (HY-14658) and linker to synthesize BRD9 PROTAC degrader dBRD 9-A (HY-148739) .
    BI-7273 acid

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