Bithionol sulfoxide(Bitin-S) is a clinically approved anti-parasitic drug; has been shown to inhibit solid tumor growth in several preclinical cancer models.IC50 value:Target: anticaner agentBithionol caused dose dependent cytotoxicity against all ovarian cancer cell lines tested with IC50 values ranging from 19 μM - 60 μM. BT treatment resulted in cell cycle arrest at G1/M phase and increased ROS generation [1]. Both bithionol and bithionol sulphoxide demonstrated in vitro toxicity to Neoparamoeba spp. at all concentrations examined (0.1 to 10 mg l(-1) over 72 h), with a comparable toxicity to freshwater observed for both chemicals at concentrations > 5 mg l(-1) following a 72 h treatment [2].
LMTK3-IN-1 (compound C28) is an ATP-competitive inhibitor of lemur tyrosine kinase 3 (LMTK3) (Kd=2.5 μM)，that acts by degrading LMTK3 via the ubiquitin-proteasome pathway. LMTK3-IN-1 shows anticancer activity in a variety of cancer cell lines and in vivo BC mouse models. LMTK3-IN-1 induces apoptosis in BC cell lines at 10-20 μM[1].
Periplanetin, a 1-benzoyl-β-d-glucose, can be isolated from the secretion of the laterocervical organ of Periplaneta americana L. and Blatta orientalis L[1].
(+)-N-Formylnorglaucine is an aporphine alkaloid isolated from the leaves of Unonopsis stipitata. (+)-N-Formylnorglaucine contains a formyl group linked to the heterocyclic nitrogen[1].
3β-Hydroxy-5-cholestenoic acid-d5 is deuterium labeled 3β-Hydroxy-5-cholestenoic acid.
A-940894 is a potent histamine H4 receptor antagonist, with Ki values of 7.6 nM (rat H4) and 71 nM (human H4). A-940894 exhibits with anti-inflammatory properties[1].
Levobetaxolol is a potent and high affinity β-adrenergic antagonist with IC50 values of 33.2, 2970, 709 nM for guinea pig atrial β1, tracheal β2 and rat colonic β3 receptors, respectively. Levobetaxolol reduces IOP (intraocular pressure). Levobetaxolol exhibits a micromolar affinity for L-type Ca21-channels. Levobetaxolol decreases the effects of ischaemia/reperfusion injury in rats. Levobetaxolol has the potential for the research of glaucoma[1][2].
Sitafloxacin Hydrate is a new-generation, broad-spectrum oral fluoroquinolone antibiotic.Target: AntibacterialSitafloxacin Hydrate, a new-generation, broad-spectrum oral fluoroquinolone that is very active against many Gram-positive, Gram-negative and anaerobic clinical isolates, including strains resistant to other fluoroquinolones, was recently approved in Japan for the treatment of respiratory and urinary tract infections [1]. In terms of clinical efficacy, oral sitafloxacin was noninferior to oral levofloxacin in the treatment of community-acquired pneumonia or an infectious exacerbation of chronic respiratory tract disease, noninferior to oral tosufloxacin in the treatment of community-acquired pneumonia, and noninferior to oral levofloxacin in the treatment of complicated urinary tract infections, according to the results of randomized, double-blind, multicentre, noninferiority trials. Noncomparative studies demonstrated the efficacy of oral sitafloxacin in otorhinolaryngological infections, urethritis in men, C. trachomatis-associated cervicitis in women and odontogenic infections [2].
Wortmannin is a multi-target inhibitor of PI3K and MLCK with IC50s of 3 nM and 200 nM, respectively. Wortmannin is also a potent inhibitor of DNA-PK (IC50, 16 nM) and ATM (IC50, 150 nM). Wortmannin is also a potent inhibitor of Polo-like kinase (Plk).
Alloisolithocholic acid (AILCA) activates large-conductance calcium-activated potassium (BK) channels with an EC50 value of 44.21 μM in Xenopus oocytes[1].
TRP-601 is a caspase inhibitor.
LAS101057 is a potent, selective, and orally efficacious A2B receptor antagonist.
PXS-4728A is a selective, orally active inhibitor of semicarbazide-sensitive amine oxidase (SSAO). PXS-4728A ameliorates chronic obstructive pulmonary disease in mice[1].
JG-98 is an allosteric heat shock protein 70 (Hsp70) inhibitor with anti-cancer activities, which disrupts Hsp70 interaction with a co-chaperone Bag3 and affects signaling pathways important for cancer development[1][2][3].
PAD4-IN-2 (compound 5i) is a PAD4 inhibitor (IC50=1.94 μM). PAD4-IN-2 inhibits tumor growth in mice by specifically inhibiting the PAD4-H3cit-NETs pathway in neutrophils[1].
GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
AKR1C1-IN-1 is a potent and selective inhibitor of human 20α-hydroxysteroid dehydrogenase (AKR1C1), with a Ki value of 4 nM for AKR1C1[1].
1,2-Dilauroyl-sn-glycero-3-phosphocholine (DLPC) is an LRH-1 agonist ligand.1,2-Dilauroyl-sn-glycero-3-phosphocholine is a phospholipid for biological study[1][2].
OHM1 is a potent HIF1α mimic that binds to CH1 domain of p300/CBP with Kd of 500 nM, reduces the level of HIF1α transcriptional activity under hypoxia to that observed under normoxia at 20 uM in A549 cells; reduces the median tumor volume in murine tumor xenografts, and does not cause measurable changes in animal body weight or other signs of toxicity in tumor-bearing animals.
HCV-IN-7 is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 has anti-viral activity[1].
Glabrene, an isoflavene derived from licorice root, shows estrogen-like activity. Glabrene is a tyrosinase inhibitor with an IC50 of 3.5 μM[1][2].
Chelidonic acid is a component of Chelidonium majus L., used as a mild analgesic, an antimicrobial, an acentral nervous system sedative. Chelidonic acid also shows anti-inflammatory activity. Chelidonic acid has potential to inhibit IL-6 production by blocking NF-κB and caspase-1[1]. Chelidonic acid is a glutamate decarboxylase inhibitor, with a Ki of 1.2 μM[2].
Ethoxylated hydrogenated castor oil (PEG-40 hydrogenated castor oil) is a combination of synthetic polyethylene glycol (PEG) with natural castor oil. Ethoxylated hydrogenated castor oil can be used to emulsify and solubilize oil-in-water (o/w) emulsions. Ethoxylated hydrogenated castor oil can be used as a cosolvent in vivo[1].
Micronomicin (Gentamicin C2b) is an aminoglycoside antibiotic, with antibacterial and bactericidal activities[1].
MDL 72527 dihydrochloride is a potent polyamine oxidase (PAO) inhibitor. MDL 72527 dihydrochloride shows a lysosomotropic effect. MDL 72527 dihydrochloride shows neuroprotective effects[1][2].
(S)-3-Amino-4-hydroxybutanoic acid is a serine derivative[1].
H-Ser-Phe-OH is a biologically active peptide.
Lenapenem (BO-2727 free acid), a carbapenem antibiotic, has potent antibacterial activity against Gram-positive and Gram-negative bacteria including P. aeruginosa[1].
Smilagenin acetate is a Sapogenin derivative extracted from patent US20030004147A1. Smilagenin acetate increases the expression of acetylcholine m2 receptors and can be used for the research of dementia[1].
Tripelennamine Hcl, a H1-receptor antagonist, is a psychoactive drug and member of the pyridine andethylenediamine classes that is used as an antipruritic and first-generation antihistamine.IC50 Value:Target: Histamine H1 receptorTripelennamine can be used in the treatment of asthma, hay fever, rhinitus and urticaria.in vitro: Arterial and mixed venous blood-gas and pH measurements were made at rest before and after saline or drug administration and during incremental exercise leading to maximal exertion at 14 m/s on 3.5% uphill grade for 120 s. Galloping at this workload elicited maximal heart rate and induced exercise-induced pulmonary hemorrhage in all horses in both treatments, thereby indicating that capillary stress failure-related pulmonary injury had occurred [1].in vivo: The data obtained (median and range in brackets) in camels and horses, respectively, were as follows: the terminal elimination half-lives were 2.39 (1.91-6.54) and 2.08 (1.31-5.65) h, total body clearances were 0.97 (0.82-1.42) and 0.84 (0.64-1.17)L/h/kg. The volumes of distribution at steady state were 2.87 (1.59-6.67) and 1.69 (1.18-3.50) L/kg, the volumes of the central compartment of the two compartment pharmacokinetic model were 1.75 (0.68-2.27) and 1.06 (0.91-2.20) L/kg [2]. After intramuscular administration of 50 or 100 mg tripelennamine, mean plasma concentrations at 30 minutes were 105 and 194 ng/ml, respectively, and mean plasma t1/2 values were 2.9 and 4.4 hours, respectively [3].