Cefatrizine (BL-S-640) is an orally active and broad-spectrum cephalosporin antibiotic. Cefatrizine is also a eEF2K inhibitor, with anti-proliferative activity in human breast cancer cells, which could induce ER stress, leading to cell death. Cefatrizine can be used in studies of cancer and bacterial infection[1][2].
Human PD-L1 inhibitor III is a human PD-L1 inhibitor.
Belinostat is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.
D-JNKI-1 is a specific inhibitor of JNK, and strongly interferes with JNK activation.
Fmoc-PEG12-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Aliconazole is an antifungal imidazole derivative.
Febuxostat D9 is deuterium labeled Febuxostat, which is a selective xanthine oxidase inhibitor with Ki of 0.6 nM.
4',4-Dibromobiphenyl-d8 is the deuterium labeled 4',4-Dibromobiphenyl[1].
Kisspeptin-10 is a potent endogenous agonist for GPR54, used as a vasoconstrictor and an angiogenesis inhibitor.
Dicyclohexylamine (S)-2-((tert-butoxycarbonyl)amino)pent-4-enoate is a Glycine (HY-Y0966) derivative[1].
Etimumotide is an immunological agent for active immunization, as well as an antineoplastic agent[1].
Brandioside is a natural phenylpropanoid glycoside from Brandisia hancei[1].
Thiomarinol A (4-Hydroxythiomarinol C) is a potent antibiotic. Thiomarinol A is a hybrid of dithiolopyrrolone and marinolic acid. Thiomarinol A shows antimicrobial activity. Thiomarinol A inhibits MRSA IleRS in a dose-dependent with a Kiapp value of 19 nM[1].
GSK9027, as a non-steroidal glucocorticoid receptor (GR) agonist, behaves as a partial agonist on the 2×glucocorticoid response element (GRE) reporter system, and achieves intrinsic activities relative to dexamethasone[1][2].
Sarafotoxin S6b is a vasoconstrictor peptide, and a non-selective endothelin receptor agonist. Sarafotoxin S6b can induce contraction in isolated human coronary arteries , the Ki values of Coronary artery, Saphenous vein and Coronary artery are 0.27, 0.55 and 19.5 nM, respectively[1].
Biotin-PEG3-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
2’,3’,5’-Tri-O-benzoyl-2’-β-C-methyl-5-methyl uridine is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
Tazobactam sodium is an antibiotic of the beta-lactamase inhibitor class. Ceftolozane combines with Tazobactam, extends the activity of ceftolozane against many ESBL-producing Enterobacteriaceae and some Bacteroides spp..
Propylthiouracil(6-Propyl-2-thiouracil) is a thyroperoxidase and 5'-deiodinase inhibitor. Target: Thyroperoxidase (TPO)Propylthiouracil (PTU) is a thiouracil-derived drug used to treat hyperthyroidism (including Graves' disease) by decreasing the amount of thyroid hormone produced by the thyroid gland [1]. The antithyroid drug 6-propylthiouracil (PTU) was shown to have an unexpectedly prolonged inhibitory effect on iodination in the thyroid glands of rats. Eighteen hours after injection of a relatively small dose, iodination in the thyroid remained inhibited by more than 90% [2]. PTU inhibits the enzyme thyroperoxidase, which normally acts in thyroid hormone synthesis by oxidizing the anion iodide (I-) to iodine (I0), facilitating iodine's addition to tyrosine residues on the hormone precursor thyroglobulin. This is one of the essential steps in the formation of thyroxine (T4). PTU does not inhibit the action of the sodium-dependent iodide transporter located on follicular cells' basolateral membranes. Inhibition of this step requires competitive inhibitors, such as perchlorate and thiocyanate. From Wikipedia.
MEHFPGP is a nootropic neuroprotective peptide. MEHFPGP can be used in the research of brain stroke[1][2].
Broussonin C is a competitive inhibitor of Tyrosinase that can be isolated from Broussonetia kazinoki. Broussonin C inhibits monophenolase and diphenolase with IC50s of 0.43 and 0.57 μM, respectively[1].
SKF89976A hydrochloride is a selective GABA transporter (GAT-1) inhibitor with IC50s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.
(2S)-3',4',7-Trimethoxyflavan is a flavan, exhibits weak cytotoxicities against HCT116 and HepG2 with IC50 values 34.36 μg/mL and 38.51 μg/mL, respectively[1].
Afegostat was previously in phase II clinical trials for the treatment of Gaucher's disease. The experiment was discontinued.
RSV-IN-7 (example 253) is a RSV inhibitor (EC50: < 0.4 μΜ)[1].
EGFR/HER2/CDK9-IN-1 (Compound 4) is a potent inhibitor of EGFR/HER2/CDK9 with IC50s of 90.17, 131.39, and 67.04 nM, respectively. EGFR/HER2/CDK9-IN-1 exhibits remarkable antitumor activity[1].
13-O-Cinnamoylbaccatin III (Baccatin III 13-cinnamate) is a taxane that can be found in the twigs of Taxus mairei[1].
Exisulind is an inactive metabolite of the nonsteroidal, anti-inflammatory agent sulindac[1]. Exisulind inhibits aldose reductase with an IC50 of 367 nM in vitro and may contribute to the beneficial pharmacological effects of sulindac on type 2 diabetic complications[2].
Phellodendrine, a isoquinoline alkaloid, is one of important characteristic ingredients in the Phellodendri chinensis cortex. phellodendrine is against AAPH-induced oxidative stress through regulating the AKT/NF-κB pathway. Phellodendrine has good antioxidant, and anti-inflammatory effect [1].
Benzoctamine hydrochloride (Ba-30803) is a psychoactive agent with anti-anxiety effect. Benzoctamine hydrochloride blocks the central postsynaptic serotonin receptors and decreases 5-HT turnover in the brain[1][2].