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transcriptional activity

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192

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-142942

    Glucocorticoid Receptor MMP Inflammation/Immunology
    Glucocorticoid receptor-IN-2 (Compound WX019) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-2 exhibits very good transcriptional repressive activity with an IC50 of 0.171 nM against hMMP1, and comparable transcriptional activation activity with an EC50 of 0.94 nM against MMTV .
    Glucocorticoid receptor-IN-2
  • HY-146184

    Bcl-2 Family Cancer
    CCT373567 is a potent degrader of transcriptional repressor BCL6, with an IC50 of 2.9 nM. CCT373567 exhibits antiproliferative activity .
    CCT373567
  • HY-142941

    Glucocorticoid Receptor MMP Inflammation/Immunology
    Glucocorticoid receptor-IN-1 (Compound WX002) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-1 exhibits very good transcriptional repressive activity with an IC50 of 2.11 nM against hMMP1, and transcriptional activation activity with an EC50 of 5.59 nM against MMTV .
    Glucocorticoid receptor-IN-1
  • HY-118414

    Prostaglandin Receptor Neurological Disease Cancer
    20-Ethyl prostaglandin E2 (compound 62) is a PG analog that stimulates Nurr1-dependent transcriptional activity .
    20-Ethyl prostaglandin E2
  • HY-N12011

    PGC-1α Others
    11-Oxoisomogroside V (compound 3) is a cucurbitacin isolated from the crude extract of Luo Han Guo. 11-Oxoisomogroside V activates the transcriptional activity of PGC-1α. In the luciferase experiment, the results showed that 10 μM and 20 μM 11-Oxoisomogroside V could increase the luciferase activity to 133.79% and 143.81% .
    11-Oxoisomogroside V
  • HY-143587

    CDK Cancer
    CDK7-IN-2 is a potent inhibitor of CDK7. CDK7 is implicated in both temporal control of the cell cycle and transcriptional activity. CDK7 is implicated in the transcriptional initiation process by phosphorylation of Rbpl subunit of RNA Polymerase II (RNAPII). CDK7 has the potential for the research of cancer disease, in particular aggressive and hard- to-treat cancers (extracted from patent WO2019099298A1, compound 1) .
    CDK7-IN-2
  • HY-142682

    Others Neurological Disease Cancer
    SCP1-IN-1 (compound SH T-62) is a potent and selective covalent inhibitor against SCP1. SCP1-IN-1 promotes REST degradation and reduces transcriptional activity. A high level of REST protein drives the tumor growth in some glioblastoma cells. SCP1-IN-1 has the potential for the research of glioblastoma whose growth is driven by REST transcription activity .
    SCP1-IN-1
  • HY-142683

    Others Neurological Disease Cancer
    SCP1-IN-2 (Compound SH T-65) is a potent and selective covalent inhibitor against SCP1. SCP1-IN-2 promotes REST degradation and reduces transcriptional activity. A high level of REST protein drives the tumor growth in some glioblastoma cells. SCP1-IN-2 has the potential for the research of glioblastoma whose growth is driven by REST transcription activity .
    SCP1-IN-2
  • HY-N2509

    Iristectrigenin B

    LXR Cardiovascular Disease
    Iristectorigenin B (Iristectrigenin B) is a liver X receptor (LXR) modulator. Iristectrigenin B stimulates the transcriptional activity of both LXR-α and LXR-β .
    Iristectorigenin B
  • HY-100277
    Mifobate
    1 Publications Verification

    SR-202

    PPAR Metabolic Disease
    Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects .
    Mifobate
  • HY-145431

    Epigenetic Reader Domain Parasite Infection
    (S)-GSK1379725A (compound AU1) is a selective bromodomain and PHD finger containing transcription factor (BPTF) bromodomain inhibitor with a Kd of 2.8 μM. (S)-GSK1379725A shows to be selective for BPTF over BRD4 bromodomain. (S)-GSK1379725A shows antimalarial activity .
    (S)-GSK1379725A
  • HY-111411
    IZCZ-3
    2 Publications Verification

    c-Myc Autophagy Cancer
    IZCZ-3 is a potent c-MYC transcription inhibitor with antitumor activity .
    IZCZ-3
  • HY-15870
    SR 11302
    5 Publications Verification

    AP-1 Inflammation/Immunology Cancer
    SR 11302 is an activator protein-1 (AP-1) transcription factor inhibitor. SR 11302 is a retinoid that specifically inhibits AP-1 activity without activating the transcription of retinoic acid response element (RARE) .
    SR 11302
  • HY-108441

    β-catenin Cancer
    CCT 031374 hydrobromid is a potent inhibitor of β-catenin/transcription factor (TCF) complex signaling. CCT031374 inhibits TCF-dependent transcription of genes of Wnt signaling pathway. CCT 031374 has antitumor activity .
    CCT031374 hydrobromide
  • HY-N10457

    Bacterial Infection Cancer
    Norstictic acid is a potent and selective allossteric transcriptional regulator. Norstictic acid shows anticancer activity. Norstictic acid shows antioxidant activity and antimicrobial activity .
    Norstictic acid
  • HY-116940

    Others Cancer
    Sm4 is a SOX18 inhibitor. Sm4 shows SOX18-DNA binding inhibitory activity. Sm4 selectively affects SOX18 transcriptional output in vitro. Sm4 blocks SoxF transcriptional activity in vivo. Sm4 can be used for cancer metastasis and vascular cancers research .
    Sm4
  • HY-103223

    NSC 710305

    Cytochrome P450 Cancer
    Phortress is a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1 .
    Phortress
  • HY-12270
    T-5224
    45+ Cited Publications

    AP-1 MMP Others
    T-5224 is a transcription factor c-Fos/activator protein (AP)-1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription .
    T-5224
  • HY-153347

    Others Metabolic Disease
    JY-2 is a moderately selective and orally active Forkhead transcription factor forkhead box O1 (FoxO1) inhibitor that inhibits FoxO1 transcriptional activity with an IC50 of 22 μM. JY-2 shows moderate inhibition against FoxO3a and FoxO4. JY-2 shows anti-diabetic activity .
    JY-2
  • HY-112920

    Others Metabolic Disease
    TM-25659 is a transcriptional co-activator with PDZ-binding motif (TAZ) modulator. Anti-osteoporotic and anti-obesity activities .
    TM-25659
  • HY-14422
    SR1078
    10+ Cited Publications

    ROR Cancer
    SR1078 is a selective agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ). SR1078 directly binds to the ligand binding domain of RORα and RORγ and increases the transcriptional activity of these receptors, leading to stimulation of RORα/γ target gene transcription .
    SR1078
  • HY-101464
    ML329
    5 Publications Verification

    Others Others
    ML329 is a micropthalmia-associated transcription factor (MITF) inhibitor, which inhibits TRPM-1 promoter activity with an IC50 of 1.2 μM.
    ML329
  • HY-135732

    Androgen Receptor Cancer
    SK33, a trifluoromethylated enobosarm analog, is a potent, and tissue selective anti-androgen. SK33reduces androgen receptor (AR) transcriptional activity .
    SK33
  • HY-156673

    c-Myc Cancer
    m-Se3 is a potent and selective c-MYC transcription inhibitor that can inhibit tumor growth and has anti-cancer activity .
    m-Se3
  • HY-B0167
    Salicylic acid
    5+ Cited Publications

    2-Hydroxybenzoic acid

    COX Autophagy Mitophagy Apoptosis Endogenous Metabolite Inflammation/Immunology Cancer
    Salicylic acid (2-Hydroxybenzoic acid) inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation .
    Salicylic acid
  • HY-142100

    NF-κB Inflammation/Immunology
    Licoagrochalcone C, a flavonoid, reveals efficacious inhibitory activity on NF-κB transcription. Licoagrochalcone C shows significant inhibitory activity on LPS (HY-D1056)-induced NO production .
    Licoagrochalcone C
  • HY-15865

    Others Cancer
    FR901463 is a potent anti-cancer agent and can be used for cancer research. FR901463 enhances the transcriptional activity of the promoter of SV40 DNA virus .
    FR901463
  • HY-15681
    Senexin A
    5+ Cited Publications

    CDK Cancer
    Senexin A is an inhibitor of CDK8/19 (IC50: 280 nM, CDK8) and an inhibitor downstream of p21 transcription. It only inhibits p21-induced transcription but does not inhibit other biological effects of p21. Senexin A inhibits CMV-GFP induction as well as the p21 stimulatory activity of the consensus NF-κB-dependent promoters .
    Senexin A
  • HY-15681A

    CDK Cancer
    Senexin A hydrochloride is an inhibitor of CDK8/19 (IC50: 280 nM, CDK8) and an inhibitor downstream of p21 transcription. It only inhibits p21-induced transcription but does not inhibit other biological effects of p21. Senexin A hydrochloride inhibits CMV-GFP induction as well as the p21 stimulatory activity of the consensus NF-κB-dependent promoters .
    Senexin A hydrochloride
  • HY-19987
    BML-284
    20+ Cited Publications

    Wnt Cancer
    BML-284 is a potent and cell-permeable Wnt signaling activator. BML-284 induces TCF-dependent transcriptional activity with an EC50 of 700 nM .
    BML-284
  • HY-N4182

    Akt p38 MAPK Autophagy Inflammation/Immunology
    Licochalcone E, a flavonoid compound isolated from Glycyrrhiza uralensis, inhibits NF-κB and AP-1 transcriptional activity through the inhibition of AKT and MAPK activation .
    Licochalcone E
  • HY-19987A

    Wnt Cancer
    BML-284 hydrochloride is a potent and cell-permeable Wnt signaling activator. BML-284 induces TCF-dependent transcriptional activity with an EC50 of 700 nM .
    BML-284 hydrochloride
  • HY-114646

    Endogenous Metabolite Cancer
    TMC-205 is a natural fungal metabolite with antiproliferative activity against cancer cell lines. TMC-205 is a transcriptional up-regulator of SV40 promoter .
    TMC-205
  • HY-161127

    c-Myc Cancer
    NT-B2R is a potent MYC inhibitor. NT-B2R inhibited MYC transcriptional activity and cell proliferation .
    NT-B2R
  • HY-115672
    KS15
    1 Publications Verification

    Cryptochrome Cancer
    KS15 is an inhibitor of the interactions between cryptochromes (CRYs: CRY1 and CRY2) and the CLOCK:BMAL1 heterodimer. KS15 impairs the feedback actions of CRYs on E-box-dependent transcription (EC50=4.9 μM) by CLOCK:BMAL1 heterodimer, an indispensable transcriptional regulator of the mammalian circadian clock. Anti-proliferative activity .
    KS15
  • HY-12484
    BMH-21
    5 Publications Verification

    DNA/RNA Synthesis Cancer
    BMH-21 is a first-in-class DNA intercalator which inhibits RNA polymerase I (Pol I) transcription. BMH-21 possesses anticancer activity .
    BMH-21
  • HY-114740
    β-Naphthoflavone
    1 Publications Verification

    5,6-Benzoflavone; beta-NF

    Aryl Hydrocarbon Receptor Apoptosis Neurological Disease Cancer
    β-Naphthoflavone is a non-carcinogenic AhR agonist as a positive control for the induction of AhR transcriptional activity . β-Naphthoflavone inhibits hydrogen peroxide-induced apoptosis .
    β-Naphthoflavone
  • HY-126037
    (±)-ML 209
    1 Publications Verification

    ROR Inflammation/Immunology
    (±)-ML 209 (compound 4n), a diphenylpropanamide, is a retinoic acid-related orphan receptor RORγ antagonist with an IC50 of 1.1 μM. (±)-ML 209 inhibits RORγt transcriptional activity with an IC50 of 300 nM in HEK293t cells. (±)-ML 209 inhibits the transcriptional activity of RORγt, but not RORα in cells. (±)-ML 209 selectively inhibits murine Th17 cell differentiation without affecting the differentiation of naïve CD4 + T cells into other lineages, including Th1 and regulatory T cells .
    (±)-ML 209
  • HY-132205

    Estrogen Receptor/ERR Metabolic Disease
    DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.80 μM. DS45500853 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM) .
    DS45500853
  • HY-15484
    Pifithrin-α hydrobromide
    50+ Cited Publications

    Pifithrin hydrobromide; PFTα hydrobromide

    MDM-2/p53 Aryl Hydrocarbon Receptor Ferroptosis Apoptosis Cancer
    Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis. Pifithrin-α hydrobromide is also an aryl hydrocarbon receptor (AhR) agonist.
    Pifithrin-α hydrobromide
  • HY-100760
    Toxoflavin
    3 Publications Verification

    Xanthothricin; Toxoflavine; PKF-118-310

    Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex, also acts as an inhibitor of KDM4A, with antitumor activity . Antibiotic properties.
    Toxoflavin
  • HY-122234

    Others Cancer
    VPC-18005 inhibits ERG-induced transcription and interacts directly with the ERG-ETS domain, and disrupts the ERG binding to DNA. VPC-18005 is a potent inhibitor of luciferase activity .
    VPC-18005
  • HY-117726

    Estrogen Receptor/ERR NF-κB Inflammation/Immunology
    WAY-169916 is a pathway-selective ligand of ER (estrogen receptor) that acts by inhibiting NF-kB transcriptional activity. WAY-169916 has potent anti-inflammatory effect .
    WAY-169916
  • HY-16401

    PM00104

    Apoptosis Cancer
    Zalypsis (PM00104) has anti-tumor activity. Zalypsis binds to DNA and shows cytotoxicity. Zalypsis inhibits cell cycle and transcription, and leads to double stranded DNA breaks .
    Zalypsis
  • HY-N0907

    NF-κB Apoptosis Inflammation/Immunology Cancer
    Ginsenoside Rg6 inhibits TNF-α-induced NF-κB transcriptional activity with an IC50 of 29.34 μM in HepG2 cells. Ginsenoside Rg6 also exhibits apoptosis-inducing effect.
    Ginsenoside Rg6
  • HY-B0167S

    2-Hydroxybenzoic acid-d6

    COX Autophagy Mitophagy Apoptosis Inflammation/Immunology Cancer
    Salicylic acid-d6 is a deuterium labeled Salicylic acid. Salicylic acid inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation[1].
    Salicylic acid-d6
  • HY-N0268

    NO Synthase Inflammation/Immunology
    Irisflorentin, a naturally occurring isoflavone, is an abundant active constituent in Belamcanda chinensis. Irisflorentin markedly reduces the transcriptional and translational levels of inducible nitric oxide synthase (iNOS) as well as the production of NO. Anti-inflammatory activity .
    Irisflorentin
  • HY-135145
    Limantrafin
    5 Publications Verification

    CB-103

    Notch Cancer
    Limantrafin (CB-103) is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. Limantrafin has anti-tumor activity .
    Limantrafin
  • HY-10172
    IMD-0354
    10+ Cited Publications

    IKK2 Inhibitor V

    IKK Cancer
    IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity . IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM .
    IMD-0354
  • HY-155338

    YAP Cancer
    SWTX-143 is a novel covalent YAP/TAZ-TEAD inhibitor that binds to the palmitoylation pocket of all four TEAD isoforms. SWTX-143 causes irreversible and specific inhibition of the transcriptional activity of YAP/TAZ-TEAD and shows antitumor activity .
    SWTX-143

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