1. Search Result
Search Result
Results for "

transcriptional+activity

" in MedChemExpress (MCE) Product Catalog:

215

Inhibitors & Agonists

2

Fluorescent Dyes

2

Biochemical Assay Reagents

2

Peptides

40

Natural
Products

6

Isotope-Labeled Compounds

2

Click Chemistry

1

GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12071
    LDN193189
    80+ Cited Publications

    DM-3189

    Organoid TGF-β Receptor Cancer
    LDN193189 (DM-3189) is a potent selective BMP type I receptor (BMP I) inhibitor. LDN193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva .
    LDN193189
  • 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-15484
    Pifithrin-α hydrobromide
    95+ 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-13982
    JSH-23
    Maximum Cited Publications
    141 Publications Verification

    NF-κB Metabolic Disease Inflammation/Immunology Cancer
    JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation .
    JSH-23
  • HY-N0292
    Oleuropein
    Maximum Cited Publications
    9 Publications Verification

    Cytochrome P450 PPAR Apoptosis Cardiovascular Disease Inflammation/Immunology Cancer
    Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity . Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase .
    Oleuropein
  • HY-12071B
    LDN193189 dihydrochloride
    80+ Cited Publications

    DM-3189 dihydrochloride

    Organoid TGF-β Receptor Cancer
    LDN193189 (DM-3189) dihydrochloride is a potent selective BMP type I receptor (BMP I) inhibitor. LDN193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva .
    LDN193189 dihydrochloride
  • 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-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-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-10172
    IMD-0354
    20+ 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-12071A
    LDN193189 Tetrahydrochloride
    80+ Cited Publications

    DM-3189 Tetrahydrochloride

    Organoid TGF-β Receptor Cancer
    LDN193189 (DM-3189) Tetrahydrochloride is a potent selective BMP type I receptor (BMP I) inhibitor. LDN193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva .
    LDN193189 Tetrahydrochloride
  • HY-129603
    SI-109
    2 Publications Verification

    STAT Ligands for Target Protein for PROTAC Cancer
    SI-109 is a potent STAT3 SH2 domain inhibitor (Ki=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36 .
    SI-109
  • HY-N0041
    Ginsenoside Rb3
    1 Publications Verification

    Gypenoside IV

    NF-κB COX NO Synthase Inflammation/Immunology Cancer
    Ginsenoside Rb3 is extracted from steamed Panax ginseng C. A. Meyer. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
    Ginsenoside Rb3
  • HY-107850

    NSC 1612; NSC 47462

    Drug Metabolite UGT Cardiovascular Disease Metabolic Disease
    Pregnanediol (NSC 1612) is a Progesterone (HY-N0437) metabolite. Pregnanediol does not affect the transcriptional activity of UGT1A1 enhancer-promoter complex of WT and variant type. pregnanediol inhibits glucuronidation activity of G71R-UGT1A1. Pregnanediol is a cause of breast milk jaundice in carriers of G71R .
    Pregnanediol
  • HY-155338

    YAP Cancer
    SWTX-143 is an orally active 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
  • HY-15510
    Tenovin-6
    5 Publications Verification

    MDM-2/p53 Dihydroorotate Dehydrogenase Sirtuin Autophagy Cancer
    Tenovin-6, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 also inhibits dihydroorotate dehydrogenase (DHODH) .
    Tenovin-6
  • HY-134761
    EN4
    2 Publications Verification

    c-Myc Cancer
    EN4 is a covalent ligand that targets cysteine 171 (C171) of MYC. EN4 is selective for c-MYC over N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis .
    EN4
  • HY-153347
    JY-2
    2 Publications Verification

    FOXO 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-N6069
    Raspberry ketone glucoside
    1 Publications Verification

    Interleukin Related JAK STAT Inflammation/Immunology
    Raspberry ketone glucoside is a melanogenesis inhibitor. Raspberry ketone glucoside inhibits melanogenesis by activating the IL6/JAK1/STAT3 pathway, inhibiting the transcriptional activity of MITFa, and its downstream expression levels of the TYR and TYRP1a genes. Raspberry ketone glucoside shows remarkable whitening activity on both B16F10 cells in vitro and zebrafish model in vivo .
    Raspberry ketone glucoside
  • HY-19625

    Reactive Oxygen Species (ROS) Paraptosis Cancer
    MCB-613 is a potent Steroid receptor coactivator SRC small molecule ‘stimulator’ (SMS), super-stimulates SRCs’ transcriptional activity. MCB-613 increases SRCs’ interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS). MCB-613 is a SMS that target oncogenes can be exploited as anti-cancer agents by over-stimulating the SRC oncogenic program .
    MCB-613
  • HY-N0906
    Ginsenoside Rk3
    1 Publications Verification

    NF-κB Cardiovascular Disease Inflammation/Immunology
    Ginsenoside Rk3 is present in the roots Panax ginseng herbs. Ginsenoside Rk3 significantly inhibits TNF-α-induced NF-κB transcriptional activity, with an IC50 of 14.24±1.30 μM in HepG2 cells.
    Ginsenoside Rk3
  • HY-109070

    EPI-002

    Androgen Receptor Cancer
    Ralaniten (EPI-002) is a potent and orally active antagonist of the androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC50 of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC) .
    Ralaniten
  • HY-12784A
    Cycloguanil hydrochloride
    3 Publications Verification

    Chlorguanide triazine hydrochloride

    Antifolate Parasite DNA/RNA Synthesis STAT Infection Cancer
    Cycloguanil (Chlorguanide triazine) hydrochloride is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil hydrochloride blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil hydrochloride also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity .
    Cycloguanil hydrochloride
  • HY-B1152
    Piperacetazine
    1 Publications Verification

    Dopamine Receptor CD276/B7-H3 FOXO Neurological Disease Cancer
    Piperacetazine is an orally active dopamine receptor antagonist and phenothiazine antipsychotic. Piperacetazine can directly bind to the PAX3::FOXO1 fusion protein and inhibit its transcriptional activity. Piperacetazine also exhibits antitumor activity with an IC50 of 7.627 μM against PANC-1 cells. Piperacetazine can be used for the research of diseases such as schizophrenia and pancreatic cancer and other tumors .
    Piperacetazine
  • 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-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-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-150102
    EPI-7170
    1 Publications Verification

    Androgen Receptor Cancer
    EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 has antitumor effects against enzalutamide resistant castration-resistant prostate cancer (CRPC) .
    EPI-7170
  • HY-125232
    MS645
    1 Publications Verification

    Epigenetic Reader Domain Cancer
    MS645 is a bivalent BET bromodomains (BrD) inhibitor with a Ki of 18.4 nM for BRD4-BD1/BD2. MS645 spatially constrains bivalent inhibition of BRD4 BrDs resulting in a sustained repression of BRD4 transcriptional activity in solid-tumor cells .
    MS645
  • HY-N3026
    Soyasaponin Ab
    1 Publications Verification

    PPAR Apoptosis Reactive Oxygen Species (ROS) Neurological Disease Metabolic Disease Inflammation/Immunology
    Soyasaponin Ab is an orally active soyasaponin. Soyasaponin Ab inhibits PPARγ transcriptional activity. Soyasaponin Ab induces apoptosis in high concentrations. Soyasaponin Ab exerts anti-obesity, anti-oxidation, anti-inflammation, anti-aging effects. Soyasaponin Ab prevents Scopolamine (HY-N0296)-induced memory impairment .
    Soyasaponin Ab
  • HY-116785

    DNA/RNA Synthesis Cancer
    BRD32048 is a direct binder of ETV1 with a KD of 17.1 μM. BRD32048 modulates both ETV1-mediated transcriptional activity and invasion of ETV1-driven cancer cells. BRD32048 inhibits ETV1 acetylation and promotes its degradation. BRD32048 acts as a top candidate ETV1 perturbagen .
    BRD32048
  • HY-12071C
    LDN193189 hydrochloride
    70+ Cited Publications

    DM-3189 hydrochloride

    Organoid TGF-β Receptor Cancer
    LDN193189 (DM-3189) hydrochloride is a potent selective BMP type I receptor (BMP I) inhibitor. LDN193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva .
    LDN193189 hydrochloride
  • HY-110028

    Cannabinoid Receptor Fatty Acid Synthase (FASN) Androgen Receptor Endocrinology Cancer
    Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees . Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. Leelamine hydrochloride suppresses transcriptional activity of androgen receptor, which is known to regulate fatty acid synthesis [2,3].
    Leelamine hydrochloride
  • HY-15510B
    Tenovin-6 Hydrochloride
    5 Publications Verification

    MDM-2/p53 Dihydroorotate Dehydrogenase Sirtuin Autophagy Cancer
    Tenovin-6 Hydrochloride, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 Hydrochloride inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 Hydrochloride also inhibits dihydroorotate dehydrogenase (DHODH) .
    Tenovin-6 Hydrochloride
  • HY-16023A
    Acolbifene
    2 Publications Verification

    EM-652; SCH 57068

    Estrogen Receptor/ERR Cancer
    Acolbifene (EM-652), the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist. Acolbifene (EM-652) inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM). Acolbifene (EM-652) possesses potent and pure anticarcinogenic properties .
    Acolbifene
  • HY-145709

    Androgen Receptor Cancer
    Ar-V7-IN-1 is a potent inhibitor of Ar-V7. Ar-V7-IN-1 inhibits the transcriptional activity of androgen receptor (AR) and the secretion of prostate-specific antigen (PSA) with an eGFP IC50 of 1232 nM and the PSA IC50 of 1391 μM. Ar-V7-IN-1 has the potential for the research of various indications, in particular cancers such as prostate cancer .
    Ar-V7-IN-1
  • HY-147291

    c-Myc PARP Apoptosis Cancer
    VPC-70063 is a potent Myc-Max inhibitor with an IC50 value of 8.9 μM for Myc-Max transcriptional activity inhibition. VPC-70063 reduces UBE2C promotor activity and AR-V7 levels, and induces PARP cleavage. VPC-70063 induces apoptosis and blocks Myc-Max interactions with DNA. VPC-70063 can be used for researching anticancer .
    VPC-70063
  • 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-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-141487
    CLP-3094
    2 Publications Verification

    Androgen Receptor Metabolic Disease Inflammation/Immunology
    CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM) . CLP-3094 is a selective, potent GPR142 antagonist .
    CLP-3094
  • HY-142682

    Phosphatase Neurological Disease Cancer
    SCP1-IN-1 is a Small CTD Phosphatase 1 (SCP1) inhibitor with a human IC50 of 10 μM. SCP1-IN-1 inactivates SCP1, promotes REST transcription factor degradation, and reduces REST transcriptional activity. SCP1-IN-1 can be used for the research of glioblastoma multiforme .
    SCP1-IN-1
  • HY-159957

    Histone Acetyltransferase Estrogen Receptor/ERR
    BAY-184 is a selective and orally active KAT6A and KAT6B inhibitor. BAY-184 inhibits KAT6A/KAT6B activity with an IC50 of 71 nM and 83 nM. respectively BAY-184 inhibits ERα transcriptional activity. BAY-184 inhibits proliferation of diverse breast cancer subtypes, and inhibits tumor growth .
    BAY-184
  • HY-163173

    YAP Cancer
    TEAD-IN-8 is a novel TEAD inhibitor, which potently and specifically inhibits TEAD-YAP transcriptional activities. TM2, alone or in combination with MEK inhibitors, exhibits potent antiproliferative effects in YAP-dependent cancer cells .
    TEAD-IN-8
  • HY-145848

    Estrogen Receptor/ERR Neurological Disease
    ERRγ agonist-1 is a potent ERRγ agonist. ERRγ agonist-1 increases transcriptional activities of ERRγ. ERRγ agonist-1 has the potential for the research of neuropsychological disorders .
    ERRγ agonist-1
  • HY-160038

    LXR Cancer
    GAC0003A4 is an LXR inverse agonist that inhibits LXR transcriptional activity. GAC0003A4 also efficiently degrades LXRβ protein. GAC0003A4 has the potential to be used in advanced pancreatic cancer and other refractory malignancies .
    GAC0003A4
  • HY-122716

    PPAR Others
    PTGR2-IN-1 is a potent PTGR2 inhibitor with an IC50 of ~0.7 μM. PTGR2-IN-1 increases 15-keto-PGE2-dependent PPARγ transcriptional activity in PTGR2-transfected HEK293T cells .
    PTGR2-IN-1
  • HY-116247

    PPAR Metabolic Disease Inflammation/Immunology
    ST247 a potent PPARβ/δ inverse agonist. ST247 has a higher affinity to PPARβ/δ. ST247 modulates expression of the activation marker CCL2 in the opposite direction. ST247 efficiently induces the interaction with corepressors. ST247 inhibits the agonist-induced transcriptional activity of PPARβ/δ .
    ST247
  • HY-120018

    Androgen Receptor Cancer
    VPC-13566, a BF3-specific small molecule, is an androgen receptor (AR) inhibitor. VPC-13566 is effective in inhibiting AR transcriptional activity in vitro as well as the growth of AR-dependent PCa cell lines. VPC-13566 can be used as a chemical probe to help identify unknown AR partners.VPC-13566 can be used for the research of cancer.
    VPC-13566
  • HY-110315

    Apoptosis MDM-2/p53 Epigenetic Reader Domain Cardiovascular Disease
    Ischemin sodium is a CBP bromodomain inhibitor that inhibits p53 interaction with CBP and transcriptional activity in cells. Ischemin sodium salt inhibits p53-induced p21 activation with an IC50 value of 5 µM. Ischemin sodium salt also prevents apoptosis in ischemic cardiomyocytes. Ischemin sodium salt can be used in the study of cardiovascular diseases (such as myocardial ischemia) .
    Ischemin sodium
  • HY-123009

    HIF/HIF Prolyl-Hydroxylase Histone Acetyltransferase Cancer
    KCN1 is a p300/HIF-1α interaction inhibitor. KCN1 inhibits HIF transcriptional activity by binding to the CH1 domain of p300 and preventing the p300/HIF-1α assembly. KCN1 exerts antitumor activities through cell cycle arrest .
    KCN1

Inquiry Online

Your information is safe with us. * Required Fields.

Salutation

 

Country or Region *

Applicant Name *

 

Organization Name *

Department *

     

Email Address *

 

Product Name *

Cat. No.

 

Requested quantity *

Phone Number *

     

Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: