T-3764518 is a novel and potent stearoyl coenzyme A desaturase (SCD) inhibitor with an IC50 of 4.7 nM.
SP-8356, an anti-inflammatory synthetic verbenone derivative, is a potent, orally active cluster of differentiation 147 (CD147) inhibitor. SP-8356 inhibits CD147-cyclophilin A (CypA) interaction and reduces MMP-9 activity. SP-8356 exerts anti-breast cancer effects by inhibiting NF-κB signaling. Anti-atherosclerotic effects[1][2][3].
3,3'-Diaminobenzidine(DAB) is an organic compound that is both chemically and thermodynamically stable; DAB has been used in immunohistochemical staining of nucleic acids and proteins.
7-Hydroxycoumarin-4-acetic acid, a pH-indicator dye, is covalently bound to bovine serum albumin (BSA) at the positions of reactive amino groups (λmax=326 nm)[1].
Prepro-Atrial Natriuretic Factor (26-55) (human) is a polypeptide that increases renal cortical and medullary cyclic GMP levels. Prepro-Atrial Natriuretic Factor (26-55) (human) increases renal guanylate cyclase activity[1].
Pyrazoloacridine (NSC 366140), an intercalating agent with anti-cancer activity, inhibits the activity of topoisomerases 1 and 2. Pyrazoloacridine (NSC 366140) exhibits an IC50 of 1.25 μM in K562 myeloid leukemia cells for 24 h treatment[1][2].
L-749372 is the beta 3 adrenergic receptor 3-Pyridyloxypropanolamine agonist.
PXYC12 is a ribosomal protein S1 (RpsA) antagonist with Kds of 2.67 and 4.67 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb)[1].
TMC310911 is a potent and orally active HIV type-1 (HIV-1) protease inhibitor with EC50 values ranged from 2.2 nM to 14.2 nM for wild-type HIV-1. TMC310911 has potent activity against a wide spectrum of recombinant HIV-1 isolates. TMC310911 has strong antiviral activity[1][2].
bpV(phen) is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B. bpV(phen) is an insulin-mimetic agent following insulin-receptor tyrosine kinase hyperphosphorylation and activation. bpV(phen) activates HIV-1 transcription and replication via NF-κB-dependent and independent mechanisms. bpV(phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity[1][2][3][4][5].
Temafloxacin (TMFX) is a quinolone antimicrobial agent that has a broad antibacterial spectrum against Gram-positive, Gram-negative and anaerobic bacteria[1][2].
UDP-Galactose disodium is a monosaccharide and a P2Y14 receptor agonist with an EC50 value of 0.67 μM. UDP-Galactose disodium is a substrate for the transferase beta-1, 4 galactosyltransferase V (B4GALT5)[1][2].
Pelecopan (BCX9930) is a potent, selective, orally active inhibitor of complement factor D with an IC50 value of 14.3 nM. Pelecopan can target factor D to prevent both intravascular and extravascular hemolysis in PNH. Pelecopan also be used for other alternative pathway (AP) mediated diseases[1][2].
M-L-Triguluronic acid is a linear polysaccharide copolymer composed of three L-guluronic acid (G) and can be used to from Alginate[1]. Alginate is a generic name of unbranched polyanionic polysaccharides and can be used for the research of antifungal agents delivery carries[2].
3-Mercaptopropanyl-N-hydroxysuccinimide ester is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Mepixanox is an analeptic drug used in respiratory and cardiorespiratory insufficiency.
SHR-1701 (Retlirafusp alfa) is a bifunctional fusion protein targeting PD-L1 and TGF-β for cancer research[1].
Alitame (anhydrous) is a high-intensity sweetener formed from the amino acids L-aspartic acid and D-alanine, and an amine derived from thietane[1].
Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).
N6-Bz-5’-O-DMTr-2’-O-hexadecanyl adenosine 3’-CED phosphoramidite 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].
Coenzyme Q0 (CoQ0) is a potent, oral active ubiquinone compound can be derived from Antrodia cinnamomea. Coenzyme Q0 induces apoptosis and autophagy, suppresses of HER-2/AKT/mTOR signaling to potentiate the apoptosis and autophagy mechanisms. Coenzyme Q0 regulates NFκB/AP-1 activation and enhances Nrf2 stabilization in attenuation of inflammation and redox imbalance. Coenzyme Q0 has anti-angiogenic activity through downregulation of MMP-9/NF-κB and upregulation of HO-1 signaling[1][2][3].
Myristoyl tetrapeptide Ala-Ala-Pro-Val is a biological active peptide. (stimulates the expression of ECM proteins and inhibits the expression of metalloproteinases (MMPs))
Tiliquinol (NSC 130828) is a non-absorbed anti-amoebic luminal agent. Tiliquinol is used in combination with tibroquinol. Tiliquinol can be used for the research of amebic liver abscess[1][2].
DM4 is is an antitubulin agent that inhibit cell division. DM4 can be used in the preparation of antibody drug conjugate.
Difloxacin-d3 (hydrochloride) is the deuterium labeled Difloxacin (hydrochloride)[1].
Alvelestat (AZD9668) is a novel, oral inhibitor of neutrophil elastase (NE) with the pIC50 of 7.9 for Human NE.IC50 Value: 7.9 ± 0.12 (pIC50, Human NE); 4.9 nM (Ki value, Human NE) [1]Target: Neutrophil elastasein vitro: AZD9668 had a high binding affinity for human NE (KD = 9.5 nM) and potently inhibited NE activity. The calculated pIC50 (IC50) and Ki values for AZD9668 for human NE were 7.9 (12 nM) and 4.9 nM, respectively. In contrast to earlier NE inhibitors, the interaction between AZD9668 and NE was rapidly reversible. AZD9668 was also highly selective for NE over other neutrophil-derived serine proteases. In cell-based assays, AZD9668 inhibited plasma NE activity in zymosan-stimulated whole blood. In isolated human polymorphonuclear cells, AZD9668 inhibited NE activity on the surface of stimulated cells and in the supernatant of primed, stimulated cells.AZD9668 showed good crossover potency to NE from other species [1]. in vivo: Six hundred and fifteen patients were randomised: placebo (302), AZD9668 60 mg bid (313). AZD9668 showed no effect on lung function: change in mean pre-bronchodilator FEV1 versus placebo was 0.01L (95% confidence interval: -0.03, 0.05; p=0.533). AZD9668 did not significantly improve respiratory signs and symptoms, SGRQ-C score or time to first exacerbation. Adverse events were similar for AZD9668 and placebo [2]. AZD9668 was well tolerated at single doses up to 150 mg and multiple doses up to 70 mg twice daily. PK were dose linear; median time to peak plasma concentration was reached at 0.5 - 1.5 hours and the short elimination half-life was consistent with twice daily dosing. Steady state was reached by Day 2 of twice daily dosing with negligible accumulation. Approximately 40% of AZD9668 was eliminated renally as unchanged compound. Ex vivo zymosan-stimulated inhibition of NE activity was dose-dependent, with maximal inhibition achieved at 60 mg [4].Toxicity: A total of 838 patients were randomised to AZD9668 5 mg bid (212 patients), 20 mg bid (206 patients), 60 mg bid (202 patients) or placebo (218 patients). AZD9668 showed no effect on lung function, respiratory signs and symptoms, QoL or biomarkers [3].Clinical trial: Phase II study of a neutrophil elastase inhibitor (AZD9668) in patients with bronchiectasis.
Schisanlignone D is a chemical component of Schisandra viridis a. c. sm[1].
Z-LYS-SBZL (monohydrochloride) is a lysine derivative[1].
Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a 5GABAA partial agonist. Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors[1].
Azido-PEG4-nitrile is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].