Berberine has shown to be effective in inhibiting cell proliferation and promoting apoptosis in various cancerous cells; MAPK and Wnt/β-catenin pathways affected by Berberine.IC50 value:Target: Anticancer agentThe plant-based alkaloid berberine has potential therapeutic applications for breast cancer, although a better understanding of the genes and cellular pathways regulated by this compound is needed to define the mechanism of its action in cancer treatment. In this review, the molecular targets of berberine in various cancers, particularly breast cancer, are discussed. Berberine was shown to be effective in inhibiting cell proliferation and promoting apoptosis in various cancerous cells. Some signaling pathways affected by berberine, including the MAP (mitogen-activated protein) kinase and Wnt/β-catenin pathways, are critical for reducing cellular migration and sensitivity to various growth factors [1]. Treatment with BBR(Berberine) in rats on the atherogenic diet reduced plasma total cholesterol and nonHDL cholesterol levels by 29%-33% and 31%-41%, respectively, with no significant differences being observed among the three doses [2]. Berberine induced both apoptotic and autophagic death of HepG2 cells, which was associated with a significant activation of AMPK and an increased expression of the inactive form of acetyl-CoA carboxylase (ACC) [3]. Berberine did not show major effects on viability of HEK-293 embryonic kidney and HCT116 colon carcinoma cells and was not toxic in concentrations up to 20 μM. Berberine inhibited β-catenin transcriptional activity and attenuated anchorage-independent growth. As a result of berberine treatment, cellular levels of active β-catenin were reduced concomitant with an increase in the expression of E-cadherin [4].
BOC-D-GLU-OH is a glutamic acid derivative[1].
CP681301 is a potent CDK5 inhibitor. CP681301 shows antiproliferative activity. CP681301 decreases the expression of CD133, OLIG2, SOX2, KI67, pCDK5 protein level in GSCs (Glioma stem cells). CP681301 reduces self-renewal in mouse glioma xenografts. CP681301 shows anti-tumor activity in Drosophila[1].
UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity[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].
Atorolimumab (P3x22914G4) is a monoclonal antibody used for immunotherapies targeting programmed death-1 (PD-1)[1].
Aminopeptidase-IN-1 (compound 16o) is a potent insulin-regulated aminopeptidase (IRAP) inhibitor with an Ki value of 7.7 μM. Aminopeptidase-IN-1 can be used tor research cognitive and memory impairments[1].
Midodrine D6 hydrochloride is deuterium labeled Midodrine, which is a vasopressor/antihypotensive agent.
Budesonide impurity C is an impurity of Budesonide. Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist[1][2].
Diphenyleneiodonium chloride is a NADPH oxidase (NOX) inhibitor and also functions as a TRPA1 activator with an EC50 of 1 to 3 μM.
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
Sodium octyl sulfate(Reagent for Ion-Pair Chromatography,99%)-d17 is the deuterium labeled Sodium octyl sulfate(Reagent for Ion-Pair Chromatography,99%)[1].
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].
Sophoricoside is an isoflavone glycoside isolated from Sophora japonica and has anti-inflammatory, anti-cancer and immunosuppressive effects.
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].
Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE;IC50=1.7 nM), and serotonin (5-HT;IC50=11 nM), and with potentials as an anti-obesity agent[1]. Tesofensine is a CNS acting anti-obesity agent[2].
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
Lacidipine-d10 is the deuterium labeled Lacidipine. Lacidipine (Lacipil, Motens) is a L-type calcium channel blocker[1][2].
Ro 8-4304 hydrochloride is a potent NMDA receptor antagonist. Ro 8-4304 hydrochloride is a NR2B selective, non-competitive, voltage-independent antagonist[1].
Nadolol D9 is the deuterium labeled Nadolol(SQ-11725), which is a non-selective beta blocker.
Phenylethanolamine A acts as a β-adrenergic agonist. Phenylethanolamine A is a byproduct during the Ractopamine synthesis process[1].
VUF-10497 is a histamine H4 receptor inverse agonist (pKi = 7.57). VUF-10497 was found to possess anti-inflammatory properties in vivo in the rat. VUF-10497 also possesses a considerable affinity for the human histamine H1 receptor.
Difluprednate(Durezol) is a corticosteroid, approved difluprednate for the treatment of post-operative ocular inflammation and pain.IC50 value:Target: Difluprednate ophthalmic emulsion 0.05% is also being studied in other ocular inflammatory diseases, including a U.S. Phase 3 study evaluating difluprednate for the treatment of anterior uveitis.
2'-F-2'-ara-N2-ibu-dG Phosphoramidite is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7)[1].
N-Azido-PEG4-N-Boc-N-PEG3-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].