Ceftaroline fosamil is a cephalosporin with activity against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA).
9-Methoxycanthin-6-one, a canthin-6-one alkaloid, is present in intact plant parts and in callus tissues of different explants. 9-Methoxycanthin-6-one shows anti-tumor activity[1][2].
Oil Red O is a fat-soluble diazol dye, with a maximum absorption at 518 nm. Oil Red O stains neutral lipids and cholesteryl esters but not biological membranes. Oil Red O can be used for detecting and quantifying hepatic steatosis in mouse liver biopsies. Oil Red O staining efficiently helps to visualize the radical changes that occur in tissues as metabolic disease occurs and progresses[1].
Propiverine hydrochloride is a bladder spasmolytic with calcium antagonistic and anticholinergic properties. Propiverine hydrochloride can be used for the research of overactive blaqdder and urinary incontinence[1][2].
2-Aminobenzamide is a neutral and stable compound used as fluorescent tag, numerously in Glycan analysis. 2-aminobenzamide acts as the starting material for several important reactions like Bargellini reaction as an competent ambident nucleophile. Specifically 2-aminobenzamide and its derivatives are used in the blood coagulation cascade[1][2].
GNF179 is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.IC50 value: 4.8 nM [1]Target: Anti-parasitic agent GNF179 exhibits a low clearance (CL=22 ml/min/kg, ~25% of hepatic blood flow in mice), a large volume of distribution (steady-state volume of distribution, Vss=11.8 l/kg), a moderate residence time (MRT=9 hours) and suitable terminal half-life (t1/2=8.9 hours). GNF179 reduced Plasmodium berghei parasitemia levels by 99.7% with a single 100 mg/kg oral dose, and prolonged mouse survival by an average of 19 days. GNF179 was able to protect against an infectious P. berghei sporozoite challenge with a single oral dose at 15 mg/kg while NITD609 was not.
Quinine sulfate (2:1) (Qualaquin) is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine sulfate (2:1) is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM[1][2].
DL-Syringaresinol diacetate is a glucoside. DL-Syringaresinol inhibits cAMP phosphodiesterase and alleviation of stress[1].
BCN-exo-PEG2-NH2 is an ADC Linker containing 2 PEG units. BCN-exo-PEG2-NH2 contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, BCN reacts with molecules containing azide groups to form stable triazoles in the absence of catalysts.
Cnidilin (Knidilin) is isolated from the root of Angelica dahurica[1].
Toonaciliatin M (compound 6) is a pmaradiene-type diterpenoid that can be isolated from Toona ciliate. Toonaciliatin M show antifungal activity against Trichophyton rubrum with an MIC value of 12.5 µg/mL[1].
TCO-PEG3-NHS ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
NR-160 (NR160) is a novel potent, selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 30 nM, shows SI (75-1847 )over all HDAC class I isoforms.NR-160 induced α-tubulin acetylation (ac-α-tubulin) in treated acute myeloid leukemic (AML) cell line HL60, but not histone H3 (ac-H3) (a marker for the inhibition of class I HDACs).NR-160 enhances the cytotoxicity induction of bortezomib, epirubicin and daunorubicin on a panel of seven leukemia cell lines
2',3'-O-Isopropylideneadenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
Aganirsen is a 25 mer DNA antisense oligonucleotide, which silences expression of insulin receptor substrate-1 (IRS-1).
1,2-Di-O-acetyl-3,5-di-O-benzoyl-D-xylofuranose 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].
Azido Myristic Acid is a click chemistry reagent containing an azide group. Azido Myristic Acid can be used to identify and characterize post-translationally myristylated proteins with using a simple and robust two-step labeling and detection technique[1].
Ganoderic acid I is a triterpenoid found in ganoderma lucidum[1].
P-gb-IN-1 (compound Ⅲ-8), a 2,5-disubstituted furan derivative, is a highly effective, broadspectrum P-glycoprotein (P-gp) inhibitor. P-gb-IN-1 displayed the reversal activity by inhibiting P-gp efflux. P-gb-IN-1 has a potent affinity to P-gp by forming H-bond interactions with residues Asn 721 and Met 986. P-gb-IN-1 possesses broad-spectrum reversal activity and low toxicity in MCF-7/ADR cells[1].
(S)-Lercanidipine D3 (hydrochloride) is a deuterium labeled Lercanidipine D3 hydrochloride. (S)-Lercanidipine hydrochloride is an antihypertensive agent[1].
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin has shown various biological activities, including inhibition of TNF-α, NF-κB, HIV-1.
Malabaricone B, a naturally occurring plant phenolic, is an orally active α-glucosidase inhibitor with an IC50 of 63.7 µM. Malabaricone B has anticancer, antimicrobial, anti-oxidation and antidiabetic activities[1][2][3].
Everolimus (RAD001) is a potent mTOR inhibitor that binds to FKBP-12 to generate an immunosuppressive complex.
JA2131 is a small molecular inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG) (IC50=0.4 μM). JA2131 regulate DNA damage responses, causes replication fork stalling and cancer cell death[1][2].
BOC-O-Benzyl-L-threonine is a threonine derivative[1].
Acrivastine (BW825C) is a short acting histamine 1 receptor antagonist for the treatment of allergic rhinitis.
Compound 48/80 (Poly-p-methoxyphenethylmethylamine) is widely used in animal and tissue models as a "selective" mast cell activator. Compound 48/80 acts at the mast cell membrane to stimulate trimeric G-proteins and induces degranulation via phospholipase C and D pathways[1][2].
Balovaptan is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors, and is used for the research of autism.
Chloroprocaine hydrochloride (2-Chloroprocaine hydrochloride) is a potent inhibitor of Na,K-ATPase activity with an IC50 of 13 mM. Chloroprocaine hydrochloride blocks peripheral nerve[1].
Odetiglucan, a novel beta glucan, is a potent immunostimulant. Odetiglucan activates innate immune effector cells and triggers a coordinated anti-cancer immune response[1].