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Transcriptional activation

" in MedChemExpress (MCE) Product Catalog:

358

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6

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5

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4

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27

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2

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56

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25

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1

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20

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12270
    T-5224
    95+ Cited Publications

    		 AP-1 MMP Neurological Disease Inflammation/Immunology Cancer
    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-B0069
    Fludarabine
    100+ Cited Publications

    F-ara-A; NSC 118218

    		 Nucleoside Antimetabolite/Analog DNA/RNA Synthesis STAT Apoptosis Cancer
    Fludarabine (NSC 118218) is a DNA synthesis inhibitor and a fluorinated purine analogue with antineoplastic activity in lymphoproliferative malignancies. Fludarabine inhibits the cytokine-induced activation of STAT1 and STAT1-dependent gene transcription in normal resting or activated lymphocytes .
    Fludarabine
  • HY-14452
    Fatostatin
    50+ Cited Publications

    125B11

    		 Fatty Acid Synthase (FASN) Cancer
    Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin decreases the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties, and lowers hyperglycemia in ob/ob mice .
    Fatostatin
  • HY-141644
    PY-60
    15+ Cited Publications

    		 Annexin A YAP Inflammation/Immunology
    PY-60 is a robust and specific activator of YAP transcriptional activity that targets annexin A2 (ANXA2) with a Kd of 1.4 µM. PY-60 directly binds to ANXA2 and antagonizes its normal cellular function of repressing YAP activity .
    PY-60
  • HY-16985
    Darolutamide
    5+ Cited Publications

    ODM-201; BAY-1841788

    		 Androgen Receptor Cancer
    Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist. Darolutamide has a Ki of 11 nM for rat wild-type AR (wtAR) and IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .
    Darolutamide
  • HY-15870
    SR 11302
    20+ Cited Publications

    		 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-B0167
    Salicylic acid
    10+ Cited Publications

    2-Hydroxybenzoic acid

    		 Environmental Pollutants Endogenous Metabolite COX Autophagy Apoptosis Mitophagy Infection Neurological Disease Inflammation/Immunology Cancer
    Salicylic acid (2-Hydroxybenzoic acid) inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation. Salicylic acid has blood-brain barrier permeability .
    Salicylic acid
  • HY-135145
    Limantrafin
    5+ Cited Publications

    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-19987
    BML-284
    40+ 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-13812
    QNZ
    45+ Cited Publications

    EVP4593

    		 NF-κB TNF Receptor Neurological Disease Inflammation/Immunology
    QNZ (EVP4593) shows strong inhibitory effects on NF-κB transcriptional activation and TNF-α production with IC50s of 11 and 7 nM, respectively. QNZ (EVP4593) is a neuroprotective inhibitor of SOC channel.
    QNZ
  • HY-50937
    ST 2825
    65+ Cited Publications

    		 MyD88 Inflammation/Immunology
    ST 2825 is a specific MyD88 dimerization inhibitor. ST2825 interferes with recruitment of IRAK1 and IRAK4 by MyD88, causing inhibition of IL-1β-mediated activation of NF-κB transcriptional activity .
    ST 2825
  • HY-100508
    ITSA-1
    15+ Cited Publications

    		 HDAC Cancer
    ITSA-1 is an activator of histone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation .
    ITSA-1
  • HY-P0282A
    TAT peptide TFA

    		HIV Infection
    TAT peptide (TFA) is a cell penetrating peptide (GRKKRRQRRRPQ) derived from the trans-activating transcriptional activator (Tat) from HIV-1 .
    TAT peptide TFA
  • HY-100431
    IMR-1
    5+ Cited Publications

    		 Notch Cancer
    IMR-1 is a novel class of Notch inhibitor targeting the transcriptional activation with an IC50 of 26 μM. IMR-1 prevents the recruitment of Mastermind-like 1 (Maml1) to the Notch Ternary Complex (NTC) on chromatin, inhibits Notch target gene transcription and dramatically inhibits tumor growth .
    IMR-1
  • HY-N2370
    24-Hydroxycholesterol
    3 Publications Verification

    		 iGluR LXR Neurological Disease
    24-Hydroxycholesterol is a natural sterol, which serves as a positive allosteric modulator of N-Methyl-d-Aspartate (NMDA) receptorsR, and a potent activator of the transcription factors LXR.
    24-Hydroxycholesterol
  • HY-111498A
    RGX-104
    3 Publications Verification

    Abequolixron

    		 LXR Inflammation/Immunology Cancer
    RGX-104 is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
    RGX-104
  • HY-12316
    20(S)-Hydroxycholesterol
    3 Publications Verification

    20α-Hydroxycholesterol

    		 Smo Endogenous Metabolite Cardiovascular Disease Metabolic Disease Cancer
    20(S)-Hydroxycholesterol (20α-Hydroxycholesterol) is an allosteric activator that selectively targets the Smoothened (Smo) of the Hedgehog pathway with an EC50 of ~30 μM (Hedgehog). 20(S)-Hydroxycholesterol binds to the extracellular cysteine-rich domain (CRD) of Smo in a stereoselective manner, activating downstream Gli transcription factors (without inducing transcription of receptor genes in the Wnt pathway). 20(S)-Hydroxycholesterol enhances osteogenic differentiation of bone marrow stromal cells and synergistically activates the Raf/MEK/ERK pathway with Simvastatin (HY-17502) to promote bone regeneration. 20(S)-Hydroxycholesterol can be used to study the mechanisms of developmental biology, oncology, bone, and angiogenesis .
    20(S)-Hydroxycholesterol
  • HY-125016
    TT-10
    2 Publications Verification

    TAZ-K

    		 YAP Cardiovascular Disease Cancer
    TT-10 (TAZ-K) is an activator of YES-associated protein (YAP)-transcriptional enhancer factor domain (TEAD) activity. TT-10 can be used for the research of heart diseases accompanied by cardiomyocyte loss .
    TT-10
  • HY-14452A
    Fatostatin hydrobromide
    50+ Cited Publications

    125B11 hydrobromide

    		 Fatty Acid Synthase (FASN) Cancer
    Fatostatin hydrobromide (125B11 hydrobromide), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin hydrobromide decreases the transcription of lipogenic genes in cells. Fatostatin hydrobromide possesses antitumor properties, and lowers hyperglycemia in ob/ob mice .
    Fatostatin hydrobromide
  • HY-B0167S
    Salicylic acid-d6
    1 Publications Verification

    2-Hydroxybenzoic acid-d6

    		 Isotope-Labeled Compounds COX Autophagy Mitophagy Apoptosis Inflammation/Immunology Cancer
    Salicylic acid-d6 is a deuterium labeled Salicylic acid (HY-B0167). Salicylic acid inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation .
    Salicylic acid-d6
  • HY-12303
    OAC1
    1 Publications Verification

    		 Oct3/4 TET Protein Cancer
    OAC1 is a potent Oct4 activator. OAC1 activates Oct4 and Nanog promoters and enhances induced pluripotent stem cells (iPSC) formation. OAC1 activates OCT4 through upregulation of HOXB4 expression. OAC1 increases transcription of the Oct4-Nanog-Sox2 triad and TET1. OAC1 facilitates the reprogramming of cells by enhancing efficiency and shortening the reprogramming time .
    OAC1
  • HY-10072
    SPC 839

    		NF-κB AP-1 Inflammation/Immunology
    SPC 839 (compound 10) is an orally active inhibitor of AP-1 and NF-kB mediated transcriptional activation with IC50 of 0.008 μM .
    SPC 839
  • HY-107753
    XRP44X

    		Ras Inflammation/Immunology Cancer
    XRP44X inhibits Ras-induced transcription activation with the IC50 of 10 nM. XRP44X inhibits activation of the Ras-Erk-1/2 pathway by FGF-2 . XRP44X is an inhibitor of Ras/Erk activation of Elk3 that also affects microtubules .
    XRP44X
  • HY-111498
    RGX-104 hydrochloride
    3 Publications Verification

    Abequolixron hydrochloride

    		 LXR Inflammation/Immunology Cancer
    RGX-104 hydrochloride is a small-molecule LXR agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
    RGX-104 hydrochloride
  • HY-N2025
    Oroxin A
    4 Publications Verification

    		 PPAR Glycosidase Metabolic Disease
    Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
    Oroxin A
  • HY-112257
    S-23
    1 Publications Verification

    		 Androgen Receptor Metabolic Disease
    S-23 is an orally active selective androgen receptor modulator (SARM) with a Ki of 1.7 nM. S-23 induces androgen receptor (AR)-mediated transcriptional activation in CV-1 cells. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats .
    S-23
  • HY-100602
    HJC0152
    3 Publications Verification

    		 STAT Apoptosis Cancer
    HJC0152 is a signal transducers and activators of transcription 3 (STAT3) inhibitor.
    HJC0152
  • HY-19694
    BRD7552

    		Insulin Receptor Endocrinology
    BRD7552, a potent PDX1 transcription factor inducer, upregulates PDX1 expression in both primary human islets and ductal cells, and induces epigenetic changes in the PDX1 promoter consistent with transcriptional activation. BRD7552 increases insulin expression. PDX1 is a key transcription factor involved in pancreas development and β cell function .
    BRD7552
  • HY-402361
    TERT activator-1

    		MEK ERK AP-1 Neurological Disease Inflammation/Immunology
    TERT activator-1 is a small molecule activator of telomerase reverse transcriptase (TERT). TERT activator-1 promotes TERT transcription through the MEK/ERK/AP-1 signaling cascade. TERT activator-1 promotes adult neurogenesis and enhances neuromuscular function. TERT activator-1 reduces cellular senescence and systemic inflammation in aged mice, and can be used in the study of aging .
    TERT activator-1
  • HY-108638
    NSC 146109 hydrochloride
    2 Publications Verification

    XI-011 hydrochloride

    		 MDM-2/p53 Apoptosis PARP Cancer
    NSC 146109 hydrochloride (XI-011 hydrochloride) is a p53 activator and MDMX inhibitor. NSC 146109 hydrochloride inhibits MDMX gene transcription, downregulates MDMX mRNA and protein levels, stabilizes p53 and activates the transcriptional activity of p53. NSC 146109 hydrochloride induces cancer cell apoptosis (apoptosis) and inhibits the growth of transformed cells. NSC 146109 hydrochloride inhibits the growth of xenograft tumors. NSC 146109 hydrochloride can be used in research related to breast cancer and cervical cancer .
    NSC 146109 hydrochloride
  • HY-W019721
    Cyclosporin D

    		Nuclear Factor of activated T Cells (NFAT) Inflammation/Immunology
    Cyclosporin D, a metabolite of Cyclosporin A, is a weak immunosuppressant. Cyclosporin D is used as internal standard for quantification of Cyclosporin A . Cyclosporin A is a potent immunosuppressant agent, suppress T cell activation by inhibiting calcineurin and the calcineurin-dependent transcription factors nuclear factor of activated T cells (NFAc) .
    Cyclosporin D
  • HY-133987
    AP-1/NF-κB activation inhibitor 1
    3 Publications Verification

    		 NF-κB Inflammation/Immunology
    AP-1/NF-κB activation inhibitor 1 is a potent AP-1 and NF-κB mediated transcriptional activation inhibitor (IC50=1 μM), without blocking basal transcription driven by the β-actin promoter. AP-1/NF-κB activation inhibitor 1 has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells .
    AP-1/NF-κB activation inhibitor 1
  • HY-P0282
    TAT peptide

    		HIV Infection
    TAT peptide is a cell penetrating peptide (GRKKRRQRRRPQ) derived from the trans-activating transcriptional activator (Tat) from HIV-1 .
    TAT peptide
  • HY-112920
    TM-25659

    		YAP Metabolic Disease
    TM-25659 is a transcriptional co-activator with PDZ-binding motif (TAZ) modulator. Anti-osteoporotic and anti-obesity activities .
    TM-25659
  • HY-136251
    BRD0539

    		Bacterial Infection
    BRD0539 is a Streptococcus pyogenes Cas9 (SpCas9) inhibitor with an IC50 of 22 μM in an in vitro DNA cleavage assay .
    BRD0539
  • HY-133961
    Cholesterol β-D-glucoside

    Cholesteryl glucoside

    		 HSP Metabolic Disease
    Cholesterol β-D-glucoside (Cholesteryl glucoside) is a heat shock transcription factor 1 (HSF1) activator. Cholesterol β-D-glucoside induces HSP70 in fibroblast cells .
    Cholesterol β-D-glucoside
  • HY-105118A
    Zaldaride maleate

    CGS-9343B; KW 5617

    		 Calmodulin Neurological Disease Metabolic Disease Inflammation/Immunology
    Zaldaride maleate (CGS-9343B) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride maleate inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM . Zaldaride maleate prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na +, Ca 2+ and K + currents in PC12 cells and inhibits nAChR .
    Zaldaride maleate
  • HY-136741
    BOT-64
    2 Publications Verification

    		 IKK Inflammation/Immunology
    BOT-64 is an inhibitory κB (IκB) kinase β (IKKβ) inhibitor with an IC50 of 1 µM. BOT-64 blocks lipopolysaccharide-induced nuclear factor-κB activation and nuclear factor-κB-regulated inflammatory gene transcription .
    BOT-64
  • HY-P99316
    Sirukumab

    CNTO-136

    		 Interleukin Related Inflammation/Immunology
    Sirukumab (CNTO-136) is a humanized monoclonal anti-IL6 (Interleukin Related) IgG1κ antibody. Sirukumab binds to IL6, preventing IL6-mediated signal transduction and activation of transcriptional activators, thereby blocking the downstream biological effects of IL6. Sirukumab can be used in the study of active lupus nephritis and rheumatoid arthritis .
    Sirukumab
  • HY-N10508
    Calcitroic acid

    		Drug Metabolite VD/VDR Metabolic Disease Cancer
    Calcitroic acid is a vitamin D receptor (VDR) agonist that can activate VDR-mediated transcription. Calcitroic acid is the main metabolite of 1,25-dihydroxyvitamin D3, with the highest concentrations found in the liver and mucosa of mice, and it has metabolic stability and very low toxicity .
    Calcitroic acid
  • HY-N4182
    Licochalcone E
    4 Publications Verification

    		 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-130479
    AdipoR agonist 1

    		Adiponectin Receptor PPAR PGC-1α Sirtuin AMPK Metabolic Disease
    AdipoR agonist 1 (Compound 112254) is an agonist for adiponectin receptor (AdipoR), which activates the transcriptional regulators like peroxisome proliferator-activated receptors (PPARs), peroxisome proliferator-activated receptor gamma coactivator 1α (PGC-1α), sirtuin 1 (SIRT1), and adenylate-activated protein kinase (AMPK). AdipoR agonist 1 is utilized in preventive doping research .
    AdipoR agonist 1
  • HY-153339
    E235

    		Eukaryotic Initiation Factor (eIF) Cancer
    E235 is an expression regulator of activates transcription factor 4 (ATF4). E235 reduces cell viability by activating integrated stress response (ISR) and DNA damage response signals. E235 has anti-proliferative activity and can be used for tumor research .
    E235
  • HY-N7439
    Mogroside VI B

    		PGC-1α Metabolic Disease
    Mogroside VI B, a cucurbitane glucoside, separated from the crude extract of Siraitia grosvenorii. Mogroside VI B shows effect on activating PGC-1α transcription .
    Mogroside VI B
  • HY-124834
    Nrf2 activator-10

    		Keap1-Nrf2 Apoptosis Cancer
    Nrf2 activator-10 (Compound AI-1) is a PI3K-dependent inducer for antioxidant response element (ARE) (EC50 is 2.7 μM) and an activator for Nrf2. Nrf2 activator-10 modifies Keap1, blocks Cul3-Keap1 ubiquitin ligase complex, activates the transcription of Nrf2. Nrf2 activator-10 protects cells from H2O2-induced apoptosis.
    Nrf2 activator-10
  • HY-B0167R
    Salicylic acid (Standard)
    10+ Cited Publications

    2-Hydroxybenzoic acid (Standard)

    		 Reference Standards COX Autophagy Mitophagy Apoptosis Endogenous Metabolite Inflammation/Immunology Cancer
    Salicylic acid (Standard) is the analytical standard of Salicylic acid. This product is intended for research and analytical applications. Salicylic acid (2-Hydroxybenzoic acid) inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation .
    Salicylic acid (Standard)
  • HY-110249
    CINPA1
    1 Publications Verification

    		 Constitutive Androstane Receptor Metabolic Disease
    CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function .
    CINPA1
  • HY-16985S
    Darolutamide-d4

    ODM-201-d4; BAY-1841788-d4

    		 Isotope-Labeled Compounds Androgen Receptor Cancer
    Darolutamide-d4 (ODM-201-d4) is deuterium labeled Darolutamide (HY-16985). Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a Ki of 11 nM for rat wild-type AR (wtAR) and an IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .
    Darolutamide-d4
  • HY-14645A
    (+)-DHMEQ
    2 Publications Verification

    (1R,2R,6R)-Dehydroxymethylepoxyquinomicin; (1R,2R,6R)-DHMEQ

    		 Keap1-Nrf2 Inflammation/Immunology
    (+)-DHMEQ is an activator of antioxidant transcription factor Nrf2. (+)-DHMEQ is the enantiomer of (-)-DHMEQ. (-)-DHMEQ inhibits NF-kB than its enantiomer (+)-DHMEQ.
    (+)-DHMEQ
  • HY-127041
    Virstatin

    		Bacterial Infection
    Virstatin inhibits the pili system synthesis and prevents A. baumannii biofilm formation. Virstatin also inhibits dimerization of the transcriptional activator ToxT .
    Virstatin

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