(Cys(Acm)6,12)-Orexin A (human, mouse, rat) is a biologically active peptide.
COX-2-IN-19 (Compound 24) is a potent COX-2 inhibitor with an IC50 of 1.76 μM. COX-2-IN-19 shows in vivo anti-inflammatory activity[1].
Fmoc-Trp(Me)-OH is synthesized by N-(9-Fluorenylmethoxycarbonyloxy)succinimide (Fmoc-ONSu) and 1-Methyl-Ltrypthophan and can be used for protein or peptide synthesis[1].
Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC50 of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC50 of 11 nM[1].
Pyridostatin is a G-quadruplexe stabilizer, with a Kd of 490 nM.
AZ505 is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM.
Phenacaine (Holocaine) is a local anesthetic. Phenacaine inhibits the specific calmodulin-dependent stimulation of erythrocyte Ca2+-ATPase and cyclic nucleotide phosphodiesterases from brain and heart[1][2].
NW 1028 is a potent VCP/p97 inhibitor. NW 1028 targets the ND1L domain of p97 and inhibits the degradation of a p97-dependent reporter. NW 1028 has good binding affinity with Kd values of 100 and 285 nM for ND1L and full length p97, respectively. NW 1028 has the function of regulating the mitotic spindle of cells[1].
Bis-PEG11-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
OTX008 is a selective inhibitor of galectin-1.
DMP 777 is a potent, selective, and orally active human leukocyte elastase (HLE) inhibitor.
Sulfamonomethoxine is a long acting sulfonamide antibacterial agent, used in blood kinetic studies,and blocks the synthesis of folic acid by inhibiting synthetase of dihydropteroate.
1,4,5,6-Tetrahydroxy-7,8-diprenylxanthone is a xanthone that can be isolated from Garcinia xanthochymus. 1,4,5,6-Tetrahydroxy-7,8-diprenylxanthone shows moderate cytotoxicities against MDA-MB-435S and A549 cell lines with IC50s of 1.3 and 3.86 渭g/ml, respectively[1].
Cyclovirobuxine D (CVB-D) is the main active component of the traditional Chinese medicine Buxus microphylla. Cyclovirobuxine D induces autophagy and attenuates the phosphorylation of Akt and mTOR[1]. Cyclovirobuxine D inhibits cell proliferation of gastric cancer cells through suppression of cell cycle progression and inducement of mitochondria-mediated apoptosis[2]. Cyclovirobuxine D is beneficial for heart failure induced by myocardial infarction[3].
Lidocaine-d6 (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a drug to treat ventricular arrhythmia and an effective tumor-inhibitor[2].
2’-Azido-2’-deoxy-5’-O-(4,4’-dimethoxytrityl)-5-methyluridine 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].
Undecanoic acid-d21 is the deuterium labeled Undecanoic acid. Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum[1].
Apremilast D5 (CC-10004 D5) is a deuterium labeled Apremilast. Apremilast is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM[1].
NecroX-5 is a derivative of the NecroX, reduces intracellular calcium concentration, and possesses anti-inflammatory and anti-cancer activity.
Vincanol ((-)-Isoeburnamine) is a blocker of voltage-gated Na+ channels. Vincanol blocks Na+ currents with an IC50 value of 40 μM. Vincanol has neuroprotective effect[1].
DDO3711, a PP5-recruiting phosphatase recruitment chimeras (PHORCs), is formed by connecting a small molecular apoptosis signal-regulated kinase 1 (ASK1) inhibitor to a PP5 activator through a chemical linker. DDO3711 specifically inhibits ASK1 (IC50 =164.1 nM) not ASK2 (IC50>20 μM). DDO3711 significantly dephosphorylates p-ASK1T838 by recruiting PP5 and shows the ASK1-dependent antiproliferative activity. DDO3711 has anti-cancer activity and has the potential for abnormally phosphorylated oncoproteins research[1].
Metipranolol is a nonselective and orally active β-adrenergic receptor antagonist. Metipranolol can be used for hypertension and glaucoma research[1][2].
Kanshone B (Compound 5) is isolated from the natural Nardostachys chinensis. Kanshone B shows inhibitoryactivity against LPS-induced NO production (IC50=11.5 μM)[1].
Cinoctramide is an intermediate of pharmaceutical synthesis.
Territrem B is an irreversible inhibitor of Acetylcholinesterase (AChE) inhibitor. Territrem B is also a fungal meroterpenoid that can be isolated from Aspergillus terreus[1][2].
HY-19163 is an orally active fibrinogen receptor antagonist, with antiplatelet activities.
Hydroxyzine is a histamine H1-receptor antagonist.Target: Histamine H1-ReceptorHydroxyzine inhibits carbachol (10 μM)-induced serotonin release by 34% at 10 μM, by 25% 1 μM and by 17% 0.1 μM in pretreated bladder slices for 60 min [1]. Hydroxyzine (0.1 mM) treatment inhibits the progression and severity of EAE by 50% and the extent of mast cell degranulation by 70% in Lewis rats with allergic encephalomyelitis (EAE) [2]. Hydroxyzine (500 ?M) significantly increases transport of etoposide to the serosal site in the jejunal everted sacs. Hydroxyzine significantly reduces the efflux and approximately 2.4 ?g/mL of etoposide in the jejunum and ileum. Hydroxyzine (0.2 μg/mL) significantly enhances the efflux of RH123 to the lumen [3].Hydroxyzine (500 μM) significantly decreases the steady-state etoposide concentration 2-fold, where the steady-state concentration reached about 0.055 μM/mL in Sprague-Dawley rats [3]. Hydroxyzine (12.5 mg/kg, 25 mg/kg and 50 mg/kg i.p.) shows little direct analgesic activity but markedly potentiates only the effect of morphine on the vocalization after-discharge which represents the affective component of pain in rats. Hydroxyzine (50 mg/kg i.p.) potentiates morphine on the tail-flick test, while Hydroxyzine (12.5 mg/kg i.p.) decreases morphine antinociception in rats [4].
Epigenetic factor-IN-1 (40569Z) is a epigenetic factor inhibitor. Epigenetic factor-IN-1 has strong binding effect on SIRT7. Epigenetic factor-IN-1 can be used for liver cancer research[1].
anti-TNBC agent-2 an anti-Triple negative breast cancer (TNBC) purine derivative. anti-TNBC agent-2 induces MDA-MB-231 cells apoptosis, and inhibits its migration and angiogenesis. anti-TNBC agent-2 inhibits tumor growth and metastasis and reduces the expression of Ki67 and CD31 protein in TNBC xenograft models. anti-TNBC agent-2 can be used for Triple negative breast cancer (TNBC) research[1].
Melinamide, an amide derivative of an unsaturated long-chain fatty acid, is an inhibitor of cholesterol absorption with an IC50 of 20.9 μM.