element

SR 11302 is an inhibitor of activator protein-1 (AP-1).

L-692429 (MK-0751) is a potent nonpeptidyl growth hormone secretagogue (GHS) agonist and benzolactam derivative, known for reversing glucocorticoid-induced inhibition of GH secretion. L-692429 exhibits high affinity for the G protein-coupled receptor and is useful in studying acromegaly and obesity.

FzM1, a negative allosteric modulator (NAM) of the Frizzled receptor FZD4, diminishes WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=−6.2) by binding to an allosteric site on intracellular loop 3 (ICL3) of FZD4. This interaction changes the receptor's conformation and inhibits the WNT/β-catenin signaling pathway.

Crebinostat is a potent histone deacetylase (HDAC) inhibitor, targeting HDAC1, HDAC2, HDAC3, and HDAC6 with IC50s of 0.7 nM, 1.0 nM, 2.0 nM, and 9.3 nM, respectively. It increases the density of synapsin-1 punctae along dendrites in neurons in vitro, modulates chromatin-mediated neuroplasticity, and enhances memory in mice. Additionally, Crebinostat induces histone H3 and H4 acetylation and enhances the expression of Egr1, a cAMP-responsive element binding protein (CREB) target gene.

Praeruptorin B (Praeruptorin D), a compound found in the roots of Peuced, is an inhibitor of sterol regulatory element-binding proteins (SREBPs) that attenuates the metastatic ability of human renal cancer cells by targeting CTSC and CTSV expression, and can be used in the study of osteoporosis.

HIF-2a translation inhibitor is a potent HIF-2α translation inhibitor with IC50=5 μM that inhibits constitutive and hypoxia-induced HIF-2α protein expression. Among them, HIF-2α-IN-4 associates the 5'UTR iron response element with oxygen sensing.

BTZO-1 is an antioxidant response element (ARE) activator with cardioprotective activity.

HIV-1 Rev (34-50) (HIV-1 rev Protein (34-50)) is a 17-amino acid peptide with anti-HIV-1 activity, derived from the Rev-responsive element-binding domains of Rev in HIV-1.

CREBtide acetate is a synthetic substrate for PKA (Km=3.9 μM), which is based on the phosphorylation sequence in d-CREB (cAMP response element binding protein).

CDDO-EA (CDDO ethyl amide) is an activator of the Nrf2/antioxidant response element.

Luteolin 7-sulfate, derived from the marine plant Phyllospadix iwatensis Makino, suppresses TYR gene expression by intervening in a signaling pathway involving the cAMP-responsive element binding protein (CREB) and microphthalmia-associated transcription factor (MITF). This inhibition ultimately leads to a decrease in melanin synthesis.

Aminooxy-PEG3-methyl ester, a PEG-based PROTAC linker, serves as a pivotal element in the synthesis of PROTACs[1].

Nicodicosapent is a fatty acid niacin conjugate and an inhibitor of the sterol regulatory element-binding protein (SREBP), which is a key regulator of cholesterol metabolism proteins such as PCSK9, HMG-CoA reductase, ATP citrate lyase, and NPC1L1.

DL-Selenomethionine (Seleno-DL-methionine) is a selenium (Se) analogue of methionine in which sulfur is replaced with the trace element selenium. Selenomethionine (SeMet) can incorporate into proteins in place of methionine with no effects on protein structure and function, providing a mechanism for reversible Se storage in organs and tissues.

N3-PEG4-C2-NH2 (PROTAC Linker 20) is a PEG-based linker compound used in the synthesis of PROTACs, enabling efficient conjugation and acting as a bridge between the target protein and the E3 ligase, thereby facilitating targeted protein degradation[1].

TEI-9647 is a 1α,25-dihydroxy vitamin D3-26,23-lactone (1α,25-lactone) analog and is an effective VDR/vitamin D-responsive element (DRE)-mediated genomic actions antagonist.

Amino-Tri-(m-PEG4-ethoxymethyl)-methane, a PEG-based PROTAC linker, is a crucial element for synthesizing PROTACs[1].

ChREBPα/14-3-3 regulator-1 (Compound 43) is a selective molecular glue that stabilizes the interaction between carbohydrate response element-binding protein (ChREBP) and 14-3-3 proteins, with an EC50 of 3.8 μM. It effectively safeguards β cells from glucolipotoxicity, preserving cell function and making it relevant for type 2 diabetes research.

Keap1-IN-1 (Compound 27) is an inhibitor of Keap1, functioning by covalently modifying the Cys151 residue on the BTB domain of KEAP1, thereby disrupting the interaction between Keap and Nrf. It enhances the mRNA expression of the antioxidant response element (ARE) dependent gene NQO1, with an EC50 of 160 nM, and exhibits cytotoxicity in U2OS cells, with an EC50 of 527 nM.

4"-(2-(p-Chlorophenyl)acetoxyl)spiramycin (Compound 2d) is a broad-spectrum anti-coronavirus agent that targets the frameshifting element (FSE). It inhibits HCoV-OC43 and HCoV-229E with EC50 values of 0.85 μM and 1.45 μM, respectively. This compound exhibits a dual-target mechanism by acting on both viral FSE RNA and host DIS3L2.

Triisopropyl phosphate inhibits TFF1 and EGR3 gene expression and exhibits anti-estrogenic activity by suppressing Estradiol-induced proliferation of MCF-7 cells, with an EC50 of 341 μM. Additionally, Triisopropyl phosphate reduces estrogen response element (ERE)-stimulated luciferase activity in MVLN cells, with an EC50 of 900 μM.

BPP-2 is a GHSR ligand containing the element F. By labeling BPP-2 with the isotope 18F, a PET probe targeting GHSR can be produced. The binding affinity (Ki) of 18F-BPP-2 for GHSR is 274 nM.

Naphthol AS-MX phosphate (NASTRp) is a small-molecule inhibitor targeting the CREB (cyclic adenosine monophosphate response element-binding protein)-CBP (CREB-binding protein) transcription factor complex. It exhibits antitumor activity against lung cancer cells by inhibiting tumor cell proliferation (IC50=3.701 μmol/L), colony formation, and anchorage-independent growth in soft agar. This compound is valuable for studying KRAS-mutant lung cancer, particularly in cases of chemotherapy resistance and poor prognosis.

GR-28 is an inhibitor of the small C-terminal domain phosphatase 1 (SCP1). It suppresses the transcriptional activity of the repressor element 1-silencing transcription factor (REST) and inhibits the proliferation of glioblastoma cells, with IC50 values of 2.9 and 10.1 µM for cell lines A172 and T98G, respectively.