Antifungal agent 87(10) acts as a highly potent PDT antimycotic photosensitizer (PDT-IC50 = 1 nM for T. rubrum)[1].
Levofloxacin ((-)-Ofloxacin) sodium is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin sodium inhibits the DNA gyrase and topoisomerase IV. Levofloxacin sodium can be used for chronic periodontitis, airway inflammation and BK Viremia research. Levofloxacin sodium shows anti-orthopoxvirus activity[1][2][3][4][5].
M4K2234 is a potent, selective ALK1 (ACVRL1) and ALK2 (ACVR1) protein kinase inhibitor with IC50 of 7 and 14 nM, respectively.M4K2234 inhibits only ALK1/2 and one additional off target (TNIK) by kinome-wide screening against 375 protein kinases at 1 uM.M4K2234 demonstrated in cell based target engagement assays with an IC50 of 83nM for ALK1 and 13 nM for ALK2.M4K2234 exhibits only very weak potency against ALK4/5.M4K2234 affects phosphorylation of SMAD1/5/8 that corresponds to BMP branch of signalling which is mediated, besides others, also by ALK1/2 kinases.M4K2234 has only a very weak effect on SMAD2/3 phosphorylation that corresponds to TGF beta branch of signalling which is mediated mostly via ALK4/5/7.
UCM05 (G28UCM) is a potent inhibitor of fatty acid synthase (FASN) shows activity against HER2+ breast cancer xenografts and is active in anti-HER2 drug-resistant cell lines[1]. UCM05 is a Filamentous temperature-sensitive protein Z (FtsZ) inhibitor and inhibits the growth of the Gram-positive bacterium B. subtilis with MIC values of 100 μM but lack activity on the Gram-negative bacterium E. coli[2].
Apigenin 7-O-malonylglucoside is found in chrysanthemum flowers[1].
Phytic acid dodecasodium salt hydrate is a phosphorus storage compound of seeds and cereal grains. Phytic acid has the strong ability to chelate multivalent metal ions, especially zinc, calcium, and iron.
3-Hydroxy-4-methoxyacetophenone(Acetoisovanillone; Isoacetovanillone) is an active compound isolated from P. spinosa. Isoacetovanillone possesses anti-inflammatory activity and prevented injuries due to administration of acetic acid in the colon[1].
Antitubercular agent-30 is an antibacterial agent against Mycobacterium tuberculosis (MIC=50 μg/mL). Antitubercular agent-30 has little cytotoxic effect on murine macrophage cells (LD85=~100 μg/mL)[1].
Leptin (116-130) is a bioactive leptin fragment. Leptin (116-130) promotes AMPA receptor trafficking to synapses and facilitate activity-dependent hippocampal synaptic plasticity. Leptin (116-130) prevents hippocampal synaptic disruption and neuronal cell death in models of amyloid toxicity. Leptin (116-130) has the potential for the research of Alzheimer's disease (AD)[1].
MRTX849 is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. MRTX849 covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction[1][2].
MY-673 is a colchicine binding site inhibitor (CBSI), that inhibits tubulin polymerization. MY-673 inhibits the ERK signaling pathway, which in turn affects SMAD4 protein expression levels in the TGF-β/SMAD pathway. MY-673 inhibited cell proliferation, migration and induced apoptosis in vivo and in vitro[1].
Chrodrimanin B, a metabolite of a fungal, is a potent, non-open-channel-blocking antagonist on B. mori GABAR RDL with an IC50 of 1.13 nM. Chrodrimanin B attenuates the peak current amplitude of the GABA response of RDL with an IC50 of 1.66 nM. Chrodrimanin B, a meroterpenoid, shows insecticidal activity[1].
Bombolitin I is an antimicrobial peptide derived from bumblebee venom. Bombolitin I can lysate erythrocyte and liposome[1].
Gypenoside LI, a gypenoside monomer, possesses anti-tumor activity. Gypenoside LI induces cell apoptosis, cell cycle and migration[1][2].
Pemetrexed disodium is a novel antifolate that inhibits the folatedependent enzymes thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase with Kis of 1.3, 7.2, and 65 nM, respectively.
Xelaglifam is a potent GPR40 agonist. Antihyperglycaemic activity[1].
exo BCN-O-PNB is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].
N-Dodecyl-β-D-maltoside (Lauryl Maltoside) is a derivatives of pyrene (Py), and it is a alkyl maltopyranoside detergent, especially in transporters and respiratory complexes. N-Dodecyl-β-D-maltoside has also been employed in applications such as in the purification and stabilization of RNA polymerase and detection of protein-lipid interactions[1].
Dipotassium glycyrrhizinate is a natural compound, inhibits atopic dermatitis-related gene expression with anti-anti-inflammatory activity[1].
Z-Tyr-OtBu is a tyrosine derivative[1].
Enterolactone is a bioactive phenolic metabolite known as a mammalian lignan derived from dietary lignans. Enterolactone has estrogenic properties and anti-breast cancer activity[1]. Enterolactone is a radiosensitizer for human breast cancer cell lines through impaired DNA repair and increased apoptosis[2].
Lexithromycin is an erythromycin A derivative, with antibacterial activity.
Methyl D-leucinate is a leucine derivative[1].
Rp-cAMPS triethylammonium salt is an analog of cAMP which acts as a potent, competitive and cell-permeable antagonist of cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 6.05 µM and 9.75 µM, respectively). Rp-cAMPS triethylammonium salt is resistant to hydrolysis by phosphodiesterases[1][2][3][4][5].
Rutin hydrate is a flavonol glycoside, able to cross the blood-brain barrier, and acts by inhibiting JNK and ERK1/2 activation and activating mTOR signalling.
Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.
Histone H1-derived Peptide is a phosphopeptide and the peptide substrates containes a sequence in accordance with the optimal recognition motif for CDKs[1].
3,3-Dibutylthiacarbocyanine iodide is a fluorescent dye with an excitation of 559 nm and an emission 604 nm[1].
2-Amino-2-cyclopentylacetic acid is a Glycine (HY-Y0966) derivative[1].
Gardenoside is a natural compound found in Gardenia fruits, with hepatoprotective properties. Gardenoside suppresses the pain of chronic constriction injury by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis[1][2].