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Results for "

Transcriptional inhibition

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) AP-1 (1) Apoptosis (3) Autophagy (1) Bcl-2 Family (1) Biochemical Assay Reagents (1) c-Myc (1) Cytochrome P450 (1) Dihydroorotate Dehydrogenase (1) DNA Methyltransferase (2) DNA/RNA Synthesis (1) Epigenetic Reader Domain (3) Estrogen Receptor/ERR (2) Glucocorticoid Receptor (1) HIV (1) HSP (1) MyD88 (1) NF-κB (1) Notch (1) p38 MAPK (1) PARP (1) PPAR (1) Ser/Thr Protease (1) Sirtuin (1) STAT (1) Survivin (1) Tyrosinase (1) VEGFR (1) YAP (1)
By Research Areas:	Cancer (19) Cardiovascular Disease (2) Endocrinology (1) Infection (1) Inflammation/Immunology (6) Metabolic Disease (2) Neurological Disease (1)

By Targets:

Akt (1)

AP-1 (1)

Apoptosis (3)

Autophagy (1)

Bcl-2 Family (1)

Biochemical Assay Reagents (1)

c-Myc (1)

Cytochrome P450 (1)

Dihydroorotate Dehydrogenase (1)

DNA Methyltransferase (2)

DNA/RNA Synthesis (1)

Epigenetic Reader Domain (3)

Estrogen Receptor/ERR (2)

Glucocorticoid Receptor (1)

HIV (1)

HSP (1)

MyD88 (1)

NF-κB (1)

Notch (1)

p38 MAPK (1)

PARP (1)

PPAR (1)

Ser/Thr Protease (1)

Sirtuin (1)

STAT (1)

Survivin (1)

Tyrosinase (1)

VEGFR (1)

YAP (1)

By Research Areas:

Cancer (19)

Cardiovascular Disease (2)

Endocrinology (1)

Infection (1)

Inflammation/Immunology (6)

Metabolic Disease (2)

Neurological Disease (1)

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Inhibitory Antibodies

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N4182

Licochalcone E	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 .

HY-153347

JY-2	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 .

HY-141703A

DC-BPi-11 hydrochloride	Epigenetic Reader Domain	Cancer
DC-BPi-11 hydrochloride is an inhibitor of bromodomain PHD finger transcription factor (BPTF), with an IC₅₀ value of 698 nM. DC-BPi-11 hydrochloride shows remarkable inhibition against leukemia cell proliferation .

HY-152223

PCSK9-IN-11	Ser/Thr Protease	Cardiovascular Disease
PCSK9-IN-11 (compound 5r) is a potent and orally active PCSK9 inhibitor. PCSK9-IN-11 exhibits PCSK9 transcriptional inhibitory activity in HepG2 cells, with an IC₅₀ of 5.7 μM. PCSK9-IN-11 increases LDL receptor (LDLR) protein level. PCSK9-IN-11 can be used for atherosclerosis research .

HY-141703

DC-BPi-11	Epigenetic Reader Domain	Cancer
DC-BPi-11 is an inhibitor of bromodomain PHD finger transcription factor (BPTF), with an IC₅₀ value of 698 nM. DC-BPi-11 shows remarkable inhibition against leukemia cell proliferation .

HY-101026

CCT251236 3 Publications Verification	HSP	Cancer
CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC₅₀ of 19 nM for inhibition of HSF1-mediated HSP72 induction.

HY-N1513

Ganoderic acid H	AP-1 NF-κB	Cancer
Ganoderic acid H is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderic acid H suppresses growth and invasive behavior of breast cancer cells through the inhibition of transcription factors AP-1 and NF-kappaB signaling .

HY-125839

OP-3633	Glucocorticoid Receptor	Inflammation/Immunology Endocrinology
OP-3633 is a potent and selective steroidal glucocorticoid receptor (GR) antagonist with an IC₅₀ of 29 nM, with inhibition of GR transcriptional activity. OP-3633 exhibits low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism .

HY-50937

ST 2825 Maximum Cited Publications 64 Publications Verification	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 .

HY-155338

SWTX-143	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 .

HY-125636

Mycro1	Others	Cancer
Mycro1 is an inhibitor of c-Myc/Max dimer and DNA binding, with an IC₅₀ value of 30 μM for the inhibition of Myc/Max DNA binding activity. Mycro1 can inhibit c-myc-dependent cell proliferation, gene transcription and oncogenic transformation .

HY-126979

Mycro2	Others	Cancer
Mycro2 is an inhibitor of c-Myc/Max dimer and DNA binding, with an IC₅₀ value of 23 μM for the inhibition of Myc/Max DNA binding activity. Mycro2 can inhibit c-myc-dependent cell proliferation, gene transcription and oncogenic transformation .

HY-139664

GSK-3685032 3 Publications Verification	DNA Methyltransferase	Cancer
GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC₅₀ of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .

HY-125232

MS645	Epigenetic Reader Domain	Cancer
MS645 is a bivalent BET bromodomains (BrD) inhibitor with a K_i 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 .

HY-145572

Imlunestrant LY-3484356	Estrogen Receptor/ERR	Cancer
Imlunestrant (LY-3484356) is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC) .

HY-114981

SRTCX1002	Sirtuin	Inflammation/Immunology
SRTCX1002 is a potent activator of SIRT1 (STAC), suppresses inflammatory responses through promotion of p65 deacetylation and inhibition of NF-κB Activity. SRTCX1002 suppresses stimuli-induced NF-κB transcriptional activation and LPS-induced TNFα secretion with IC₅₀s of 0.71 and 7.58 µM, respectively .

HY-145572A

Imlunestrant tosylate LY-3484356 tosylate	Estrogen Receptor/ERR	Cancer
Imlunestrant (LY-3484356) tosylate is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant tosylate results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant tosylate can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC) .

HY-N0292

Oleuropein 1 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 .

HY-124593

PTC299 1 Publications Verification	VEGFR Dihydroorotate Dehydrogenase DNA/RNA Synthesis	Cancer
PTC299 is an orally active inhibitor of VEGFA mRNA translation that selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydroorotate dehydrogenase (DHODH). PTC299 shows good oral bioavailability and lack of off-target kinase inhibition and myelosuppression. PTC299 can be useful for the research of hematologic malignancies .

HY-139664A

(R)-GSK-3685032	DNA Methyltransferase	Cancer
(R)-GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC₅₀ of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .

HY-135046

MTOB sodium 1 Publications Verification	Others	Neurological Disease Inflammation/Immunology Cancer
MTOB sodium is a potent C-terminal binding protein (CtBP) inhibitor. MTOB sodium attenuates repetitive head injury-elicited neurologic dysfunction and neuroinflammation via inhibition of the transactivation activity of CtBP1 and CtBP2. MTOB sodium antagonizes the transcriptional regulatory activity of CtBP1 and CtBP2 by eviction from their target promoters in breast cancer cell lines .

HY-147187

MNK8	STAT Apoptosis Bcl-2 Family Survivin	Cancer
MNK8 is a potent STAT3 (signal transducer and activator of transcription 3) inhibitor. MNK8 inhibits STAT3 activation and reduced its DNA binding ability. MNK8 shows good growth inhibition against hepatocellular carcinoma (HCC) cells. MNK8 induces apoptosis in HCC cells. MNK8 reduces prosurvival proteins expression and migration/invasion of HCC cells .

HY-139664B

(S)-GSK-3685032	Others	Cancer
(S)-GSK-3685032 is the isomer of GSK-3685032 (HY-139664), and can be used as an experimental control. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC₅₀ of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .

HY-147291

VPC-70063	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 .

HY-N3810

ent-11α-Hydroxy-15-oxokaur-16-en-19-oic acid	Tyrosinase	Others
ent-11α-Hydroxy-15-oxokaur-16-en-19-oic acid is an anti-melanin synthesis tyrosinase inhibitor, which can be isolated from Pteris fern. ent-11α-Hydroxy-15-oxokaur-16-en-19-oic acid regulates the melanogenesis transcription factor microphthalmia-associated transcription factor (MITF). The 11α-OH, 15-oxo and 16-en moieties of ent-11α-Hydroxy-15-oxokaur-16-en-19-oic acid are key fragments that inhibit melanin synthesis. The 19-COOH moiety has been implicated in the inhibition of cytotoxicity associated with 11α-OH KA and related compounds .

HY-P99925

Enoticumab REGN421	Notch	Metabolic Disease Cancer
Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .

HY-120072

PF-3450074 3 Publications Verification PF-74	HIV	Infection
PF-3450074 (PF-74) is a specifical inhibitor of HIV-1 capsid protein (CA) and displays a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC₅₀=8-640 nM). PF-3450074 (PF-74) acts at an early stage of HIV-1 infection, inhibits viral replication by directly competing with the binding of CPSF6 and NUP153, and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle . CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.

HY-141582

Ceramide 3 N-Stearoyl phytosphingosine	Biochemical Assay Reagents	Others
C18 Phytoceramide (t18:0/18:0) (Cer(t18:0/18:0)) is a bioactive sphingolipid found in the stratum corneum of Saccharomyces cerevisiae, wheat grain, and mammalian epidermis. Cer(t18:0/18:0) consists of a phytosphingosine backbone amine linked to a C18 fatty acid chain. Cer(t18:0/18:0) has the function of regulating apoptosis, cell differentiation, proliferation of smooth muscle cells and inhibition of mitochondrial respiratory chain. It also suppresses the expression of allergic cytokines IL-4, TNF-α, and transcription factors c-Jun and NF-κB in histone-stimulated mouse skin tissue. Formulations containing cer(t18:0/18:0) have been used as skin protectants in cosmetics as they reduce water loss and prevent epidermal dehydration and irritation.

PI3K/Akt/mTOR Compound Library	568 compounds
The PI3K/Akt/mTOR pathway controls many cellular processes that are important for the formation and progression of cancer, including apoptosis, transcription, translation, metabolism, angiogenesis, and cell cycle progression. Every major node of this signaling network is activated in a wide range of human tumors. Mechanisms for the pathway activation include activation of receptor tyrosine kinases (RTKs) upstream of PI3K, mutation or amplification of PIK3CA encoding p110α catalytic subunit of PI3K, mutation or loss of PTEN tumor suppressor gene, and mutation or amplification of Akt1. Once the pathway is activated, signaling through Akt can stimulate a series of substrates including mTOR which is involved in protein synthesis. Thus, inhibition of this pathway is an attractive concept for cancer prevention and/or therapy. Currently some mTOR inhibitors are approved for several indications, and there are several novel PI3K/Akt/mTOR inhibitors in clinical trials. MCE owns a unique collection of 568 compounds that can be used for PI3K/Akt/mTOR pathway research. PI3K/Akt/mTOR Compound Library also acts as a useful tool for anti-cancer drug discovery.

Ceramide 3 N-Stearoyl phytosphingosine	Biochemical Assay Reagents
C18 Phytoceramide (t18:0/18:0) (Cer(t18:0/18:0)) is a bioactive sphingolipid found in the stratum corneum of Saccharomyces cerevisiae, wheat grain, and mammalian epidermis. Cer(t18:0/18:0) consists of a phytosphingosine backbone amine linked to a C18 fatty acid chain. Cer(t18:0/18:0) has the function of regulating apoptosis, cell differentiation, proliferation of smooth muscle cells and inhibition of mitochondrial respiratory chain. It also suppresses the expression of allergic cytokines IL-4, TNF-α, and transcription factors c-Jun and NF-κB in histone-stimulated mouse skin tissue. Formulations containing cer(t18:0/18:0) have been used as skin protectants in cosmetics as they reduce water loss and prevent epidermal dehydration and irritation.

Enoticumab REGN421	Notch	Metabolic Disease Cancer
Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .

Licochalcone E	Chalcones Flavonoids Classification of Application Fields Leguminosae Source classification Plants Inflammation/Immunology Disease Research Fields Glycyrrhiza uralensis Fisch.	Akt p38 MAPK Autophagy
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 .

Ganoderic acid H	Triterpenes Microorganisms Classification of Application Fields Terpenoids Source classification Polyporaceae Plants Disease Research Fields Cancer	AP-1 NF-κB
Ganoderic acid H is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderic acid H suppresses growth and invasive behavior of breast cancer cells through the inhibition of transcription factors AP-1 and NF-kappaB signaling .

Oleuropein 1 Publications Verification	Cardiovascular Disease Structural Classification Classification of Application Fields Anti-aging Source classification Plants Burseraceae Iridoids Canarium album (Lour.) Rauesch. Terpenoids Phenols Polyphenols Inflammation/Immunology Disease Research Fields Cancer	Cytochrome P450 PPAR Apoptosis
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 .

ent-11α-Hydroxy-15-oxokaur-16-en-19-oic acid	Structural Classification Terpenoids Source classification Pteridaceae Diterpenoids Plants Pteris semipinnata L. Sp.	Tyrosinase
ent-11α-Hydroxy-15-oxokaur-16-en-19-oic acid is an anti-melanin synthesis tyrosinase inhibitor, which can be isolated from Pteris fern. ent-11α-Hydroxy-15-oxokaur-16-en-19-oic acid regulates the melanogenesis transcription factor microphthalmia-associated transcription factor (MITF). The 11α-OH, 15-oxo and 16-en moieties of ent-11α-Hydroxy-15-oxokaur-16-en-19-oic acid are key fragments that inhibit melanin synthesis. The 19-COOH moiety has been implicated in the inhibition of cytotoxicity associated with 11α-OH KA and related compounds .

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