Kievitone, an isoflavanone, could be isolated from hypocotyls of Phaseolus vulgaris L. infected with Rhizoctonia solani Kühn. Kievitone has antifungal activity and antitumor activity[1][2].
Tofacitinib is a JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
3,5-Dimethoxyphenol is a toxin metabolite, found in human consuming yew leaves[1].
Epirizole (Mepirizole) is an orally active NSAID (nonsteroidal anti-inflammatory drug). Epirizole shows anti-inflammatory activity, and can be used in chronic rheumatoid arthritis research[1].
GNE-781 is a highly potent and selective CBP inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nΜ, respectively.
Fulimetibant is a bradykinin receptor antagonist[1].
Delphinidin 3,5-diglucoside is an anthocyanin, and can be isolated from Punica granatum[1].
Pamidronate disodium pentahydrate is a nitrogen-containing bisphosphonate, used to prevent osteoporosis.
Aloin (mixture of A&B) is anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) has diverse biological activities such as anti-inflammatory, immunity, antidiabetic, antioxidant, antibacterial, antifungal, and antitumor activities. Aloin (mixture of A&B) also an effective inhibitor of stimulated granulocyte matrix metalloproteinases (MMPs)[1][2].
GNE-272 is a potent and selective in vivo probe for the bromodomains of CBP/EP300 with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively.
Pyrocatechol monoglucoside is a phenolic glycoside that can be isolated from Itoa orientalis[1].
Trimebutine-d5 is the deuterium labeled Trimebutine. Trimebutine is a drug with antimuscarinic and weak mu opioid agonist effects[1][2].
TM5441 is a plasminogen activator inhibitor-1 (PAI-1); inhibits several tumor cell lines with IC50 values between 9.7 and 60.3 μM.
Tolmetin sodium is an orally active and potent COX inhibitor with IC50s of 0.35 µM and 0.82 µM human COX-1 and COX-2, respectively. Tolmetin sodium is a non-steroidal anti-inflammatory drug (NSAID)[1][2].
μ-Conotoxin GIIIB is a 22-residue polypeptide that can be isolated from the venom of piscivorous cone snail Conus geographus. μ-Conotoxin GIIIB is a NaV1.4 channel inhibitor. μ-Conotoxin GIIIB blocks muscle cell's contraction[1][2][3].
1,2-Dihydrotanshinone (1,2-Dihydrotanshinquinone) is an abietane diterpene. 1,2-Dihydrotanshinone inhibits the formation of the pathogenic complex formed between (CUG)n-RNA and the splicing-factor muscleblind-like 1 (MBNL1). 1,2-Dihydrotanshinone can be used for the research of myotonic dystrophy type 1[1][2].
(-)-Pinocembrin exhibits anti-mycobacterium activity against mycobacteriuum tuberculosis H37Ra with an IC50 value of 1.11 mg/mL in dormant phase and 1.21 mg/mL in active phase, respectively. (-)-Pinocembrin has potent antiproliferative activity with IC50 values of 1.88-11.00 mg/mL against THP-1, A549, Panc-1, HeLa and MCF7 cell lines[1].
BOC-D-GLU-OH is a glutamic acid derivative[1].
DL 071IT is a potent non-selective beta-adrenergic receptor blocker. DL 071IT exhibits intrinsic sympathomimetic activity and weak membrane stabilizing activity. DL 071IT reduces exercise heart rate and systolic blood pressure, and even significantly lowers resting heart rate[1].
Midodrine D6 hydrochloride is deuterium labeled Midodrine, which is a vasopressor/antihypotensive agent.
PFKFB3-IN-2 is a 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) inhibitor. PFKFB3-IN-2 has potential applications in cancer, neurodegenerative diseases, autoimmune diseases, inflammatory diseases, multiple sclerosis, metabolic diseases, angiogenesis inhibition and other diseases[1].
Hoechst stains are part of a family of blue fluorescent dyes used to stain DNA.IC50 Value:Target: These Bis-benzimides were originally developed by Hoechst AG, which numbered all their compounds so that the dye Hoechst 33342 is the 33342nd compound made by the company. There are three related Hoechst stains: Hoechst 33258, Hoechst 33342, and Hoechst 34580. The dyes Hoechst 33258 and Hoechst 33342 are the ones most commonly used and they have similarexcitation/emission spectra. Both dyes are excited by ultraviolet light at around 350 nm, and both emit blue/cyan fluorescent light around anemission maximum at 461 nm. Unbound dye has its maximum fluorescence emission in the 510-540 nm range. Hoechst dyes are soluble in water and in organic solvents such as dimethyl formamide or dimethyl sulfoxide. Concentrations can be achieved of up to 10 mg/mL. Aqueous solutions are stable at 2-6 °C for at least six months when protected from light. For long-term storage the solutions are instead frozen at ≤-20 °C.The dyes bind to the minor groove of double-stranded DNA with a preference for sequences rich in adenine andthymine. Although the dyes can bind to all nucleic acids, AT-rich double-stranded DNA strands enhance fluorescence considerably.Hoechst dyes are cell-permeable and can bind to DNA in live or fixed cells. Therefore, these stains are often called supravital, which means that cells survive a treatment with these compounds. Cells that express specific ATP-binding cassette transporter proteins can also actively transport these stains out of their cytoplasm.in vitro: N/A in vivo: N/AClinical trial: N/A
Vutiglabridin (HSG4112), a racemic compound, is a potent anti-obesity agent[1]. Vutiglabridin, an optimized structural analog of Glabridin, markedly supersedes Glabridin in weight reduction efficacy and chemical stability[1].
Propargyl-PEG2-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
PF-4950834 is a potent, selective, orally bioavailable, ATP-competitive rho kinase inhibitor with IC50 values of 8.35 nM and 33.12 nM against ROCK2 and ROCK1, respectively. PF-4950834 inhibits neutrophil migration[1].
Bis(4-Methoxyphenyl)methanone-d8 is the deuterium labeled Bis(4-Methoxyphenyl)methanone[1].
Glycyrrhizin-6′′-methylester (compound 22) is a glycyrrhizin that can be isolated from licorice root. Glycyrrhizin-6′′-methylester can participate as an aglycone in the formation of methyl glucuronate, producing a sweet and licorice taste, but no bitterness. This reveals the importance of the free carboxyl group on the glycoside cone-bound glucuronic acid for natural sweetness and licorice taste[1].
Dezamizumab (GSK 2398852) is a fully humanized recombinant monoclonal IgG1 anti-serum amyloid P component (SAP) antibody, with potential anti-amyloid activity. Dezamizumab triggers immunotherapeutic clearance of amyloid. Dezamizumab can be used in research of Amyloid light-chain (AL) amyloidosis[1].
PF-03049423 is a potent, selective, orally active, and brain penetrant inhibitor of PDE5 with IC50 of 0.2 nM; displays 158-fold and 2460-fold selectivity over PDE6 and PDE11, respectively; possesses an excellent potency and selectivity profile and demonstrates robust in vivo blood pressure lowering in a spontaneously hypertensive rat (SHR) model. Stroke Phase 2 Discontinued
Ro 8-4304 hydrochloride is a potent NMDA receptor antagonist. Ro 8-4304 hydrochloride is a NR2B selective, non-competitive, voltage-independent antagonist[1].