Bursehernin (Methylpluviatolide) is an antitumor agent. Bursehernin induces Apoptosis and cell cycle arrest at G2/M phase. Bursehernin shows anti-proliferative activity[1][2].
Ligustrazine (hydrochloride) is a natural product.IC50 value:Target:In vitro: Ligustrazine hydrochloride displayed a protection effect on injured ECV304 cells, NOS and NO formation were significantly increased compared with the model group [1].In vivo:
Pifithrin-β is a potent p53 inhibitor with an IC50 of 23 μM.
TVD-0003510 is a carboxamide derivative, and involves in synthesis of (2-((6-(2-aminopyrimidine-5-carboxamido)-8-methoxy-3,4-dihydro-2H-pyrimido[1,2-c]quinazolin-9-yl)oxy)ethyl)piperazine-l-carboxylate (C51), as a part of tert-butyl2-(4-hydroxyphenyl)acetate[1].
4-Chloro-3,5-dimethylphenoxyacetic acid (compound 602 UC) is a product of masked amide bond hydrolysis of auxin analog 602 (compound 602).602 can effectively stimulate hypocotyl growth in wild-type seedlings[1].
Pramipexole 2Hcl is a partial/full D2S, D2L, D3, D4 receptor agonist with a Ki of 3.9, 2.2, 0.5 and 5.1 nM for D2S, D2L, D3, D4 receptor, respectively. IC50 Value: 3.9 nM(D2S); 2.2 nM(D2L); 0.5 nM(D3); 5.1 nM(D4)Target: Dopamine ReceptorPramipexole dihydrochloride is a dopamine receptor agonist with selectivity for the D3 receptor (Ki values are 3.9, 3.3, 0.5 and 3.9 nM for D2L, D2S, D3 and D4 receptors respectively). Pramipexole dihydrochloride exhibits negligable affinity for D1 and D5 receptors. Pramipexole has been found to have neuroprotective effects independent of its dopamine receptor agonism. It reduces mitochondrial reactive oxygen species (ROS) production and inhibits the activation of apoptotic pathways. Pramipexole displays activity in the treatment of Parkinson's disease (PD) and restless legs syndrome (RLS).
N-Acetyl-S-(N-methylcarbamoyl)-L-cysteine-d3 is the deuterium labeled N-Acetyl-S-(N-methylcarbamoyl)-L-cysteine[1].
Emodin-1-O-β-gentiobioside is an anthraquinone[1][2].
(-)-Oxypeucedanin hydrate ((-)-Prangol) is a derivative of furocoumarin isolated from Ducrosia anethifolia[1].
Medroxalol (RMI81968) is an orally active adrenergic receptor antagonist, blocks α- and β-adrenergic receptors. Medroxalol shows antihypertensive and vasodilating effects[1].
H-L-Tyr(2-azidoethyl)-OH hydrochloride is a unnatural Tyrosine derivative. H-L-Tyr(2-azidoethyl)-OH hydrochloride is a click chemistry reagent containing an azide group[1][2].
CLR1501, a fluorescently labeled CLR1404 analog, is a cancer cell-selective fluorescence compound[1][2].
Picrocrocin, an apocarotenoid found in the flowers of Cochliobolus sativus. Picrocrocin shows anticancer effect. Picrocrocin exhibits growth inhibitory effects against SKMEL-2 human malignant melanoma cells[1].
1,4-Epidioxybisabola-2,10-dien-9-one is a 1,4-epidioxy-bisabola-2,12-diene derivate, which can be isolated from Curcuma longa L. 1,4-Epidioxybisabola-2,10-dien-9-one exhibits antiviral activity against influenza virus A/PR/8/34 (H1N1) in the MDCK cell line with an IC50 of 16.79 ± 4.03 μg/mL[1].
NVP-CGM097 is a potent and selective MDM2 inhibitor with IC50 of 1.7±0.1 nM for hMDM2.
1-BOC-4-(2-Hydroxyethyl)piperazine-d4 is the deuterium labeled 1-BOC-4-(2-Hydroxyethyl)piperazine[1].
Isatuximab is a monoclonal antibody targeting the transmembrane receptor and ectoenzyme CD38, a protein highly expressed on hematological malignant cells, including those in multiple myeloma (MM). Isatuximab has antitumor activity via multiple biological mechanisms, including antibody-dependent cellular-mediated cytotoxicity, complement-dependent cytotoxicity, antibody-dependent cellular phagocytosis, and direct induction of apoptosis without crosslinking. Isatuximab also directly inhibits CD38 ectoenzyme activity, which is implicated in many cellular functions[1][2].
Ethyl Caffeate is a natural phenolic compound isolated from Bidens pilosa. Ethyl caffeate suppresses NF-κB activation and its downstream inflammatory mediators, inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and prostaglandin E2 (PGE2) in vitro or in mouse skin[1].
ATV006 is a potent, orally active antiviral agent and ester prodrugs of GS-441524. ATV006 inhibits the replication of SARS-CoV-2 and its variants. ATV006 can be used for SARS-CoV-2 research[1].
HR1 is a mastoid protease. HR1 can increase the permeability of human erythrocyte membrane. HR1 can induce cytoplasmic membrane permeation in bacteria and mast cells [1].
3’-O-(t-Butyldiphenylsilyl) thymidine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Rosuvastatin Calcium is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM. IC50 Value: 11 nM [1]Target: HMG-CoA reductasein vitro: Rosuvastatin is relatively hydrophilic and is highly selective for hepatic cells; its uptake is mediated by the liver-specific organic anion transporter OATP-C. Rosuvastatin is a high-affinity substrate for OATP-C with apparent association constant of 8.5 μM [2]. Rosuvastatin inhibits cholesterol biosynthesis in rat liver isolated hepatocytes with IC50 of 1.12 nM. Rosuvastatin causes approximately 10 times greater increase of mRNA of LDL receptors than pravastatin [1]. Rosuvastatin (100 μM) decreases the extent of U937 adhesion to TNF-α-stimulated HUVEC. Rosuvastatin inhibits the expressions of ICAM-1, MCP-1, IL-8, IL-6, and COX-2 mRNA and protein levels through inhibition of c-Jun N-terminal kinase and nuclear factor-kB in endothelial cells [3].in vivo: Rosuvastatin (3 mg/kg) daily administration for 14 days decreases plasma cholesterol levels by 26% in male beagle dogs with normal cholesterol levels. In cynomolgus monkeys, Rosuvastatin decreases plasma cholesterol levels by 22% [1]. Rosuvastatin (20 mg/kg/day) administration for 2 weeks, significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin [4]. Rosuvastatin shows antiatherothromhotic effects in vivo. Rosuvastatin (1.25 mg/kg) significantly inhibits thrombin-induced transmigration of monocvtes across mesenteric venules via inhibition of the endothelial cell surface expression of P-selectin, and increases the basal rate of nitric oxide in aortic segments by 2-fold times [5].
Tetramycin B (4-Hydroxytetramycin A) is a polyene macrolide antibiotic, an antifungal active compound isolated from Streptomyces hygrospinosus var. Beijingensis. The antifungal activity of Tetramycin B is higher than that of Tetramycin A, and the C-4 hydroxyl of Tetramycin B plays an important role in its biological activity[1].
PSB069 bearing a p-chlorophenylamino residue is a potent, well-tolerated and nonselective NTPDases1, 2, 3 inhibitor(Ki=16~18 μM)[1].
N-(2-Nitrophenylsulfenyl)glycine (dicyclohexylammonium) salt is a Glycine (HY-Y0966) derivative[1].
Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. PKI-587 is equally effective in both complexes of mTOR, mTORC1 and mTORC2.
Ronidazole is an antiprotozoal agent.Target: AntiparasiticRonidazole is an antiprotozoal agent used in veterinary medicine. It may also have use for the treatment of Tritrichomonas foetus infection in cats. Ronidazole kills T foetus at concentrations > 0.1 μg/mL in vitro. Ronidazole (30 or 50 mg/kg) cures T foetus infection for follow-up durations of 21 to 30 weeks after treatment in 10/10 cats [1].
Estradiol 3-sulfamate (BLE 00084; E2MATE; ES-J 995) is a potent, long-acting, and orally active steroid sulfatase inhibitor; inhibits estrone sulfatase with an IC50 of 251 nM and a Ki of 133 nM.
Yimitasvir (Emitasvir) is an orally active hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor. Yimitasvir can be used for research of chronic HCV infection[1].
4-Methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazole-5-carboxylic acid is a metabolite of GW 501516 (HY-10838) [1].