Search Result
Results for "
Transcriptional inhibition
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N4182
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Akt
p38 MAPK
Autophagy
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Inflammation/Immunology
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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 .
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- HY-152223
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PCSK9
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Cardiovascular Disease
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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 .
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- HY-153347
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JY-2
1 Publications Verification
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FOXO
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Metabolic Disease
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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 .
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- HY-141703A
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Epigenetic Reader Domain
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Cancer
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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 .
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- HY-101026
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HSP
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Cancer
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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.
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- HY-N1513
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AP-1
NF-κB
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Cancer
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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 .
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- HY-50937
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ST 2825
Maximum Cited Publications
66 Publications Verification
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MyD88
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Inflammation/Immunology
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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 .
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- HY-155338
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YAP
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Cancer
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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 .
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- HY-141703
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Epigenetic Reader Domain
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Cancer
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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 .
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- HY-125839
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Glucocorticoid Receptor
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Inflammation/Immunology
Endocrinology
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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 .
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- HY-129346
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Others
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Cancer
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STF-038533 is a CREB target gene transcription inhibitor with the activity of inhibiting the expression of related genes. STF-038533 plays a regulatory role in cell signaling pathways and has potential application value in exploring the inhibition of CREB-related diseases .
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- HY-125636
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Others
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Cancer
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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 .
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- HY-126979
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Others
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Cancer
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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 .
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- HY-113843
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Others
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Cancer
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RETRA (hydrobromide) is a mutant p53-dependent activator of p73 that can inhibit cancer cells carrying mutant p53. RETRA (hydrobromide) increases the expression level of p73, induces transcriptional activation of several common to transcriptional targets p53 and p73, which leads to mutant p53- and p73-dependent inhibition of tumor growth, reduction of colony formation and induction of effector caspases .
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- HY-139664
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DNA Methyltransferase
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Cancer
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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 .
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- HY-125232
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Epigenetic Reader Domain
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Cancer
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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 .
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- HY-145572
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LY-3484356
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Estrogen Receptor/ERR
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Cancer
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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) .
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- HY-114981
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Sirtuin
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Inflammation/Immunology
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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 .
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- HY-145572A
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LY-3484356 tosylate
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Estrogen Receptor/ERR
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Cancer
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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) .
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- HY-N0292
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Cytochrome P450
PPAR
Apoptosis
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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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 .
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- HY-124593
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PTC299
2 Publications Verification
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VEGFR
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
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Cancer
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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 .
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- HY-139664A
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DNA Methyltransferase
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Cancer
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(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 .
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- HY-135046
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Others
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Neurological Disease
Inflammation/Immunology
Cancer
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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 .
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- HY-141677B
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Histone Demethylase
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Cancer
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INCB059872 tosylate is a potent, selective and orally active lysine-specific demethylase 1 inhibitor. INCB059872 binds to and inhibits LSD1, enhancing H3K4 methylation, thereby increasing the expression of tumor suppressor genes. INCB059872 inhibition also promotes H3K9 methylation, thereby reducing the transcription of tumor-promoting genes .
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- HY-117746
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Others
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Infection
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KSK120 is a potent inhibitor of drug-resistant infections with specific activity against Chlamydia trachomatis (C. trachomatis). KSK120 inhibits the developmental cycle of C. trachomatis, thereby reducing the infectivity of progeny bacteria. KSK120 targets the glucose-6-phosphate (G-6P) metabolic pathway of C. trachomatis, showing its potential application in antimicrobial inhibition. The mechanism of KSK120 may involve inhibition of the transcriptional machinery, which provides new ideas for the development of specific drugs against C. trachomatis infection .
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- HY-147187
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STAT
Apoptosis
Bcl-2 Family
Survivin
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Cancer
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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 .
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- HY-139664B
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Others
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Cancer
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(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 .
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- HY-147291
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c-Myc
PARP
Apoptosis
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Cancer
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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 .
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- HY-N0292R
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Cytochrome P450
PPAR
Apoptosis
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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Oleuropein (Standard) is the analytical standard of Oleuropein. This product is intended for research and analytical applications. 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 .
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- HY-163944
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Molecular Glues
CDK
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Cancer
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LL-K12-18 is a two-site molecular glue that enhances the protein-protein interaction of the CDK12-DDB1 complex, stabilizing the CDK12-DDB1 complex and promoting the degradation of cyclin K (EC50=0.37 nM). LL-K12-18 exhibits strong gene transcription inhibition and anti-proliferation effects in tumor cells. LL-K12-18 can be used in cancer research .
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- HY-N3810
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Tyrosinase
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Others
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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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- HY-164445
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STAT
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Cancer
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STAT3-IN-32 (compound 2p) is an orally active, potent STAT3 dual phosphorylation inhibitor with an indole-containing tetra-aromatic heterocycle scaffold. STAT3-IN-32 exhibits STAT3 luciferase inhibition activity using HEK293T cells with an IC50 of 5.3 nM and ATP production inhibition activity using BxPC-3 cells with an IC50 of 4.2 nM. STAT3-IN-32 significantly blocks p-Tyr705 and p-Ser727 and causes the abrogation of the corresponding nuclear transcription and mitochondrial oxidative phosphorylation functions of STAT3 by targeting the STAT3 SH2 domain (KD=21.3 nM). STAT3-IN-32 exhibits significant suppressive effects in a pancreatic cancer xenograft model .
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- HY-P99925
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REGN421
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Notch
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Metabolic Disease
Cancer
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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 .
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- HY-120072
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PF-74
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HIV
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Infection
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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.
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- HY-161649
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Cytochrome P450
Aryl Hydrocarbon Receptor
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Cancer
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hCYP1B1-IN-2 (compound 3n) is a potent human cytochrome P450 1B1 enzyme hCYP1B1 inhibitor. hCYP1B1-IN-2 shows the extremely potent anti-hCYP1B1 activity (IC50=0.040 nM) and blocks AhR transcription activity. hCYP1B1-IN-2 potently inhibits hCYP1B1 via a mix inhibition manner, showing a Ki value of 21.71 pM .
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- HY-12031B
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Others
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Inflammation/Immunology
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(2Z,3Z)-U0126 is a selective inhibitor of MEK1 and MEK2, demonstrating potent antiinflammatory effects by noncompetitively inhibiting AP-1 transcriptional activity with IC50 values of 72 nM for MEK1 and 58 nM for MEK2. (2Z,3Z)-U0126 also inhibits anchorage-independent growth of Ki-ras-transformed rat fibroblasts by blocking both the extracellular signal-regulated kinase and mammalian target of rapamycin pathways. Additionally, (2Z,3Z)-U0126 can undergo isomerization and cyclization, resulting in various products that show reduced affinity for MEK and diminished AP-1 inhibition compared to the parent compound.
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- HY-141582
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N-Stearoyl phytosphingosine
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Biochemical Assay Reagents
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Others
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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.
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- HY-111527
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Others
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Neurological Disease
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PPZ2 is a diacylglycerol (DAG)-activated TRPC3/TRPC6/TRPC7 channel activator with activity in promoting neuronal development and survival. PPZ2 activates recombinant TRPC3/TRPC6/TRPC7 channels in a dose-dependent manner without affecting other TRPC channels. PPZ2 elicits cation currents and calcium ion (Ca(2+)) influx in cultured central neurons. PPZ2 is able to induce BDNF-like neurite outgrowth and neuroprotection, an effect that disappears after TRPC3/TRPC6/TRPC7 knockdown or inhibition. PPZ2 also increases the activation of the calcium-dependent transcription factor cAMP response element binding protein. The effects of PPZ2 suggest that calcium signaling mediated by activation of DAG-activated TRPC channels plays an important role in its neurotrophic effects .
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HY-L015
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616 compounds
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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 616 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.
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Cat. No. |
Product Name |
Type |
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- HY-141582
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N-Stearoyl phytosphingosine
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Drug Delivery
|
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.
|
Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99925
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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 .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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