BRD4-BD1-IN-1 (Compound 9a) is a BRD4-BD1 inhibitor with an IC50 of 38.20 μM[1].
Acebilustat is a leukotriene A4 hydrolase inhibitor, used for an oral antiinflammatory drug.
Factor B-IN-5 (Example 5 target compound) is a potent complement factor B inhibitor, with an IC50 of 1.2 μM. Factor B-IN-5 can be used for the research of diseases related to inflammation and immunity[1].
(+)-Dihydrocalanolide A (DHCal A; NSC 678323) is an orally active nonnucleoside inhibitor of Reverse Transcriptase. (+)-Dihydrocalanolide A can be used to HIV infection research[1].
Naftopidil-d5 is deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia[1][2].
PrPSc-IN-1 is a fluorescent probe, binds to the misfolded protein PrPSc, inhibits its accumulation, with an IC50 of 1.6 μM. Anti-prion activity[1].
α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[1].
TLR4 agonist-1 (compound 17a) is a potent agonist of Toll-like Receptor 4 (TLR4), and induces the generation of MIP-1β in RAW 264.7 and MM6 cells[1].
Puerarin-4'-O-β-D-glucopyranoside (compound 8) is a isoflavone from Pueraria lobata root (PLR). Puerarin-4'-O-β-D-glucopyranoside has estrogenic activity and anti-proliferation of MCF-7 human breast carcinoma cells[1].
Indolapril hydrochloride (CI-907) is an orally active nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor. Indolapril hydrochloride is highly specific in suppressing the contractile or pressor responses to Angiotensin I. Indolapril hydrochloride is a potent antihypertensive agent[1].
Guancydine (Guancidine) is an antihypertensive agent[1].
Dixyrazine, a phenothiazine derivative, can prevent brain oedema induced by intracarotid injection of protamine sulphate.
Clomifene is an orally active compound used for infertility. Clomifene is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation[1].
Euphorbetin, isolated from the ethyl acetate extract of the dried whole plants of Viola yedoensis Makino, exhibits anticoagulant activities[1].
Dazopride is an antiemetic agent.
Phalloidin-FITC, a green fluorescent cytoskeleton stain, binds and labels F-actin. For most fluorescent imaging applications, cells should to be fixed and permeablilized. Excitation/emission maxima λ ~496/516 nm.
N-Formyl-DL-alanine is an alanine derivative[1].
Echinacoside is a natural polyphenolic compound, has various kinds of pharmacological activities, such as antioxidative, anti-inflammatory, neuroprotective, hepatoprotective, nitric oxide radical-scavenging and vasodilative ones.IC50 value:Target:in vitro: Echinacoside(ECH) dose dependently inhibited HEWL aggregation, and this inhibition occurred in different fiber-forming stages. ECH could also scavenge the DPPH and OH free radicals in a concentration-dependent manner. ECH could increase viability of rat pheochromocytoma PC12 cells injured by Aβ and suppress the increase in intracellular reactive oxygen species (ROS) triggered by Aβ [1]. Transient treatment with echinacoside inhibits cytochrome c release and caspase-3 activation caused by ensuing rotenone exposure via activating Trk-extracellular signal-regulated kinase (ERK) pathway in neuronal cells [2]. ECH caused a significant increase in cell proliferation, ALP activity, COL I contents, OCN levels and an enhancement of mineralization in osteoblasts at the concentration range from 0.01 to 10nmol·L(-1) (p<0.05), suggesting that ECH has a stimulatory effect on osteoblastic bone formation or has potential activity against osteoporosis [4]. in vivo: In OVX rats, the increases of body weight, serum hydroxyproline (HOP) levels, and the decreases of uterus wet weight and BMD were significantly reversed by ECH treatment [3]. Echinacoside (60 mg/kg) was given intraperitoneally to mice at 1 h prior to GalN/LPS exposure. Pretreatment with echinacoside remarkably improved the survival rate of GalN/LPS-treated mice and attenuated acute hepatotoxicity, as demonstrated by decreased ALT levels and improved histological signs. Echinacoside shows both anti-apoptotic and anti-inflammatory properties, characterized by a substantial inhibition of hepatocyte apoptosis and a significant reduction in the inflammatory markers, including myeloperoxidase, extracellular nucleosomes, high-mobility group box 1, and inflammatory cytokines in the plasma of mice, which may be important mechanisms related to its protective effect [5].
SCD1 inhibitor-4 is a potent, orally active stearoylCoA desaturase-1 (SCD1) inhibitor. SCD1 inhibitor-4 can be used for the research of diabetes[1].
Jacareubin is a xanthone compound that can be isolated from Calophyllum brasiliense. Jacareubin has antibacterial, antioxidant, gastroprotective properties, and also has certain cancer cell toxicity, which can be used in cancer research[1].
Benzyl-PEG5-THP is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Tinoridine (Y-3642) is an orally active non-steroidal anti-inflammatory agent with potent antiperoxidative ability and radical scavenger activity. Tinoridine acts function by inhibiting COX enzyme, involves in hepatotoxicity inhibition. [1][2][3].
Boldenone undecylenate(Equipoise) is a synthetic steroid which has a similar effect as the natural steroid testosterone; it is frequently used in veterinary medicine, though it is also used in humans.IC50 Value: Target: The effects of this steroid are more subtle than that of many other steroids.in vitro: in vivo: Rabbits were injected intramuscularly twice weekly for two months. BOL had no significant effect on the bwt and bwt gain. Testes and epididymis weights were decreased significantly in the BOL-treated groups. BOL caused significant reduction in serum testosterone level, seminal volume, sperm motility, and sperm count [1].
Selamectin is an anthelminthic which can be used on dogs and cats.
KIF18A-IN-4 is a moderately potent ATP and microtubule (MT) noncompetitive KIF18A inhibitor (IC50=6.16 μM). KIF18A-IN-4 has selectivity against a large panel of mitotic kinesins and kinases, and does not show any direct effects on tubulin assembly. KIF18A-IN-4 exhibits anti-tumor activity[1].
Saikogenin F, from the chloroform extract of the Chinese medicine formula Shenqi San. Anti-cancer activity[1].
18-Nor-4,15-dihydroxyabieta-8,11,13-trien-7-one is a compound isolated from the buds of Pinus banksiana Lamb[1].
Smcy HY Peptide (738-746) is a H2-Db-restricted peptide corresponding to amino acids 738-746 of Smcy protein[1].
Norfenefrine hydrochloride is an orally active, endogenously found α-adrenergic agonist and can be used for the research of female stress incontinence[1][2].
Cefpiramide sodium (SM-1652; Wy-44635) is a new Pseudomonas-active cephalosporin with a broad spectrum of antibacterial activity.IC50 value:Target: antibacterial agentCefpiramide was moderately susceptible to hydrolysis by a variety of beta-lactamases from Gram-negative bacilli. cefpiramide was more active against Acinetobacter spp. and Pseudomonas spp. Like most other cephalosporins, cefpiramide inhibited methicillin-susceptible staphylococci, non-enterococcal streptococci, Neisseria gonorrhoeae, N. meningitidis and beta-lactamase-negative Haemophilus influenzae [1]. Pharmacokinetic studies in mice showed that cefpiramide attained a peak serum concentration of 12 micrograms/ml and a serum half-life of 40 min, which are higher than attained by cefoperazone with values of 4 micrograms/ml and 18 min. These factors may have caused the combined cefpiramide-gentamicin therapy to result in significantly improved survival rates in mice as well as in higher bactericidal titers than the cefoperazone-gentamicin combination [2].Cefpiramide inhibited many Pseudomonas aeruginosa resistant to carbenicillin, piperacillin, and cefotaxime, but it was less active than ceftazidime and cefsulodin. Cefpiramide inhibited staphylococci and streptococci and had appreciable activity against Streptococcus faecalis and Listeria moncytogenes [3].