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DiBaC4(5) is a fluorescent voltage-sensitive dye that can be used to monitor the transmembranepotentials when Papain-dissociated retinal cells from adult zebrafish were exposed to GABAergic ligands. DiBaC4(5) is a potential-sensitive fluorescence dye .
GO-203 TFA is a potentMUC1-C oncoprotein inhibitor. GO-203 TFA is an all D-amino acid peptide that consists of a poly-R transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. GO-203 TFA downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 TFA induces the production of ROS and loss of mitochondrial transmembranepotential. GO-203 TFA inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice .
(R)-Olacaftor ((R)-VX-440) is a Cystic fibrosis transmembrane conductance regulator (CFTR) modulator. (R)-Olacaftor has good potential for the study of cystic fibrosis (CF) .
CFTR corrector 6 is a potent potentiator of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). CFTR corrector 6 has the potential for cystic fibrosis (CF) and other CFTR associated disorders research .
CFTR corrector 4 (Compound 13), an active (R,R)-form enantiomer, is a highly potent and orally active cystic fibrosis transmembrane conductance regulator (CFTR) corrector. CFTR corrector 4 can increase CFTR levels at the cell surface and have the potential for treatment of cystic fibrosis .
Agaric acid (Agaricinic Acid) is obtained from various plants of the fungous tribe, i.e. Polyporus officinalis and Polyporus igniarius. Agaric acid induces mitochondrial permeability transition through its interaction with the adenine nucleotide translocase. Agaric acid promotes efflux of accumulated Ca 2+, collapse of transmembranepotential, and mitochondrial swelling. Agaric acid is used to regulate lipid metabolism .
(5E)-7-Oxozeaenol is an active fungal extract that is cytotoxic. (5E)-7-Oxozeaenol exhibits antibacterial, mitochondrial transmembranepotential, and NF-κB effects .
G092 is a potent inhibitor of MsbA. MsbA is an ABC transporter. Transmembrane ATP-binding cassette (ABC) transporters are crucial cellular machines that move molecules small and large across membranes. G092 has the potential for the research of antimicrobial agents .
GSK812397 is a CXCR4 antagonist with potential for the treatment of HIV infection. To evaluate the clinical potential of GSK812397, kilogram-scale agent candidates are needed. Here, an improved, scalable synthetic route for the CXCR4 antagonist GSK812397 is described. This new route has been scaled up in a 50-liter stationary facility to obtain 1.2 kg of agent substance in 20% overall yield and >99% chemical and enantiomeric purity in five steps. CXC chemokine receptor 4 (CXCR4) is a 7-transmembrane protein that functions in part as a host co-receptor for multiple strains of HIV-1. It is thought that targeting CXCR4 will help inhibit the replication of several late cytopathic viruses; therefore, CXCR4 antagonists are one of the most promising new classes of experimental anti-HIV agents. GSK812397 is a potent CXCR4 antagonist and is therefore a candidate for investigation for the treatment of HIV infection.
Exendin-P5 is a selective agonist that targets the GLP-1R. Exendin-P5 promotes rapid activation of G proteins by transient interactions with the transmembrane domain of GLP-1R, enhancing its potency in G protein-mediated signaling and accelerating cAMP production. This mechanism suggests the potential application of Exendin-P5 in the study of metabolic diseases .
RET-IN-9 is a potent inhibitor of RET. RET kinase is a single-pass transmembrane receptor tyrosine kinase that plays an important role in the development of the kidney and enteric nervous system, and the maintenance of homeostasis in the nervous, endocrine, hematopoietic, and male reproductive systems. RET-IN-9 has the potential for the research of RET-related disease including non-small cell lung cancer and medullary thyroid cancer (extracted from patent WO2021115457A1, compound 29) .
N-a-Tosyl-L-lysinyl-chloromethylketone hydrochloride (TLCK hydrochloride) is an irreversible inhibitor for serine protease, which inhibits trypsin and trypsin-like protease by alkylating histidine residues in their active site. N-a-Tosyl-L-lysinyl-chloromethylketone hydrochloride inhibits caspase-3, caspase-6 and caspase-7, with IC50s of 12.0, 54.5 and 19.3 μM, respectively. N-a-Tosyl-L-lysinyl-chloromethylketone hydrochloride induces apoptosis in cell HL-60, and inhibits the decrease in mitochondrial transmembranepotential during apoptosis .
Antibacterial agent 244 is an orally active compound with broad-spectrum antibacterial activity, primarily targeting Gram-positive bacteria, with a MIC value of 1–4 μg/mL and low hemolytic toxicity (HC50 of 111.6 μg/mL). Antibacterial agent 244 disrupts bacterial transmembranepotential, increases membrane permeability, leading to leakage of cellular contents such as DNA and proteins, ultimately causing bacterial death. Antibacterial agent 244 can be used in research related to Gram-positive bacterial infections .
Antibiofilm agent-13 (compound 14b) is a potent antibacterial agent that displays a broad-spectrum antimicrobial activity. Antibiofilm agent-13 could disintegrate the integrity of bacterial cell membranes by destroying transmembranepotential and enhancing membrane permeability, and causing the generation of intracellular ROS and the leakage of DNA and proteins, ultimately leading to bacterial death. Antibiofilm agent-13 inhibits both Gram-positive bacteria (MIC of 0.5-1 μg/mL) and Gram-negative bacteria (MIC of 1-32 μg/mL) .
(S)-VU0637120 is a Y4R antagonist that effectively reduces the binding response of its endogenous ligand, pancreatic polypeptide (PP), on Y4R, with an IC50 value of 2.7 μM. (S)-VU0637120 binds to the allosteric site of Y4R, which is located in the core region of the Y4R transmembrane structure, near the binding pocket of pancreatic polypeptide (PP), with a KB value of 300-400 nM. (S)-VU0637120 holds potential for research in the field of metabolic diseases .
UCCF-029 Free base is a potent activator of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel. UCCF-029 Free base exhibits enhanced activity through benzannulation of the flavone A-ring at the 7,8-position. UCCF-029 Free base serves as a structural guide for the development of more effective flavonoid analogues. UCCF-029 Free base demonstrates improved potency compared to apigenin in activating wild-type CFTR. UCCF-029 Free base also exhibits potential for activating the mutant CFTR (G551D-CFTR) though not as robustly as apigenin.
DiBaC4(5) is a fluorescent voltage-sensitive dye that can be used to monitor the transmembranepotentials when Papain-dissociated retinal cells from adult zebrafish were exposed to GABAergic ligands. DiBaC4(5) is a potential-sensitive fluorescence dye .
GO-203 TFA is a potentMUC1-C oncoprotein inhibitor. GO-203 TFA is an all D-amino acid peptide that consists of a poly-R transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. GO-203 TFA downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 TFA induces the production of ROS and loss of mitochondrial transmembranepotential. GO-203 TFA inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice .
Exendin-P5 is a selective agonist that targets the GLP-1R. Exendin-P5 promotes rapid activation of G proteins by transient interactions with the transmembrane domain of GLP-1R, enhancing its potency in G protein-mediated signaling and accelerating cAMP production. This mechanism suggests the potential application of Exendin-P5 in the study of metabolic diseases .
Agaric acid (Agaricinic Acid) is obtained from various plants of the fungous tribe, i.e. Polyporus officinalis and Polyporus igniarius. Agaric acid induces mitochondrial permeability transition through its interaction with the adenine nucleotide translocase. Agaric acid promotes efflux of accumulated Ca 2+, collapse of transmembranepotential, and mitochondrial swelling. Agaric acid is used to regulate lipid metabolism .
(5E)-7-Oxozeaenol is an active fungal extract that is cytotoxic. (5E)-7-Oxozeaenol exhibits antibacterial, mitochondrial transmembranepotential, and NF-κB effects .
TRPA1; Transient receptor potential cation channel subfamily A member 1; Ankyrin-like with transmembrane domains protein 1; Transformation-sensitive protein p120; Wasabi receptor
The TRPA1 protein is a receptor-activated nonselective cation channel that is critical for pain detection and may affect cold sensation, oxygen sensing, cough reflex, itch, and inner ear function. It responds to inflammatory mediators and irritants such as allyl thiocyanate (AITC), cinnamic aldehyde, diallyl disulfide (DADS), and acrolein. TRPA1 Protein, Human (HEK293, His, MBP, FLAG) is the recombinant human-derived TRPA1 protein, expressed by HEK293 , with N-10*His, N-MBP, C-Flag labeled tag. The total length of TRPA1 Protein, Human (HEK293, His, MBP, FLAG) is 1118 a.a. .
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