N-Acetyldopamine dimer-3 (compound 11) is a natural product that can be found in Aspongopus chinensis[1].
IU1-248, a derivative of IU1, is a potent and selective USP14 inhibitor with an IC50 of 0.83 μM.
(+)-Cloprostenol is a prostaglandin F2α (PGF2α) analogue, and shows selective agonistic activity at the prostaglandin receptor.
CCT 007093 is an effective PPM1D inhibitor that selectively reduces viability of human tumour cell lines.IC50 value: Target: PPM1DAs expected of a specific inhibitor, the toxicity of CCT007093 to PPM1D overexpressing cell lines after inhibitor treatment is P38 dependent [1]. Knockdown of WIP1 or treatment with the WIP1 inhibitor CCT007093 results in increased phosphorylation of known WIP1 targets, reduced HDM2 expression, and reduced growth specifically in WIP1 wild-type and high-expressing medulloblastoma cells [2]. CCT007093 treatment appeared to promote apoptosis in breast cancer cells and skin transformed keratinocytes that ectopically expressed Wip1, demonstrating that the effect of CCT007093 differs based on the level of Wip1 expression [3].
GLP-1R agonist 4 is a potent agonist of GLP-1R. Glucagon-like peptide-1 (GLP-1) is an intestinal hypoglycemic hormone secreted by L-cells in the lower gastrointestinal tract. GLP-1R agonist 4 has the potential for the research of diabetes (extracted from patent WO2019239319A1, compound 96)[1].
Tetrahydrobiopterin is a cofactor of the aromatic amino acid hydroxylases enzymes and also acts as an essential cofactor for all nitric oxide synthase (NOS) isoforms.
Bcl-2-IN-4 is a potent, orally active and selective Bcl-2 inhibitor with an IC50 of 1.5 nM. Bcl-2-IN-4 displays >200-fold selectivity over Bcl-xL (IC50 of 411 nM). Bcl-2-IN-4 inhibits RS4; 11 cell proliferation with an IC50 of 2.7 nM (WO2021180040A1; compound 2)[1].
HCV-IN-33 (Compound (S)-3i) is an HCV entry inhibitor[1].
Metronidazole hydrochloride (SC 326421) is an orally active nitroimidazole antibiotic, can be used to research anaerobic infections. Metronidazole hydrochloride can cross blood brain barrier and results inflammation and skeletal muscle contraction under long-term application[1][2][3][4].
RH01386 is a small molecule that protect pancreatic β cells against endoplasmic reticulum stress-induced cell death; increases the survival of human primary β cells and rodent β cell lines subjected to ER stressors including palmitate; also restores ER stress-impaired glucose-stimulated insulin secretion responses.
NSC745887 (compound 25) is an anti-cancer agent. NSC745887 exhibits dose-dependent inhibition of proliferation in all 60 cancer cell lines[1].
Triphala, an Ayurvedic polyherbal formulation comprising of equiproportional fruit parts of Terminalia chebula, Terminalia bellerica, and Phyllanthus emblica[1]. Triphala inhibits NF-κB activation. Triphala exerts antifungal action[2]. Anti-adipogenic, anti-inflammatory, and anti-neoplastic activities.
Antitubercular agent-26 (Compound 32) is an orally active anti-tubercular agent with an extracellular IC50 of 0.50 μM and an intracellular IC50 of 0.51 μM against M. tuberculosis H37Rv. Antitubercular agent-26 shows good metabolic stability, low risk of cardiotoxicity and no genotoxicity[1].
Invopressin (Compound 42) is a vasopressin V1A receptor partial agonist (EC50: 1.0 nM). Invopressin can be used for research of cirrhosis, including bacterial peritonitis, HRS2 and refractory ascites[1].
Larixyl acetate is a potent and selective TRPC6 inhibitor with IC50 values of 0.58 μM and 6.83 μM against hTRPC6-YFP and hTRPC3-YFP, respectively. Larixyl acetate prevents HPV and is effective in protecting against traumatic brain injury-induced systemic endothelial dysfunction[1][2].
(+)-trans-Isolimonene is a natural monoterpene isolated from essential oil[1].
BrBzGCp2 is a Glyoxalase 1 (GLO1) inhibitor, with a GC50 of 4.23 μM in HL-60 cells. BrBzGCp2 possesses antitumor and neuroprotective activity[1][2].
SC-58125 is a potent and selective inhibitor of cyclooxygenase 2 (COX-2), with an IC50 of 0.04 μM. SC-58125 exhibits antitumor activity in vitro and in vivo, and it also can inhibit edema at the inflammatory site and is analgesic[1][2][3].
Akuammidine, isolated from the seeds of Picralima nitida, shows a preference for μ-opioid binding sites with Ki values of 0.6, 2.4 and 8.6 μM at μ-, σ- and κ-opioid binding sites, respectively. Akuammidine possesses anti-inflammatory and anti-asthmatic properties[1][2].
Ethyl 2-((tert-butoxycarbonyl)((1-(hydroxymethyl)cyclopropyl)methyl)amino)acetate is a Glycine (HY-Y0966) derivative[1].
N-(Amino-PEG1)-N-bis(PEG2-propargyl) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
ITX3 is a specific and nontoxic inhibitor of the TrioN (N-terminal GEF domain of the multidomain Trio protein) with IC50 of 76 uM; inhibits TrioN-stimulated RhoG exchange in vitro.IC50 value: 76 uM [1]Target: TrioN inhibitorIn transfected mammalian cells, ITX3 blocked TrioN-mediated dorsal membrane ruffling and Rac1 activation while having no effect on GEF337-, Tiam1-, or Vav2-mediated RhoA or Rac1 activation. ITX3 specifically inhibited endogenous TrioN activity, as evidenced by its ability to inhibit neurite outgrowth in nerve growth factor (NGF)–stimulated PC12 cells or C2C12 differentiation into myotubes [1]. ITX3 repressed the Rac1 activity and dose dependently up-regulated the E-cadherin protein level in the Tara-KD cells [2].
Isoguvacine hydrochloride is a GABA receptor agonist.
DBCO-PEG9-DBCO is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
SM 16 is a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively.
PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor[1][2].
Apoptosis inducer 3 (Compound 3) is an apoptosis inducer that selectively triggers apoptosis and late-apoptosis. Apoptosis inducer 3 shows cytotoxicity against cancer cells[1].
Sulfaethoxypyridazine is a sulfonamide antibacterial agent. Sulfaethoxypyridazine is a sulfonamide that is used in veterinary medicine as feedstuffs[1].
Sildenafil Mesylate is an orally active and selective phosphodiesterase type 5 (PDE5) inhibitor. Sildenafil Mesylate can be used in studies of erectile dysfunction and cancer[1].