450191S is a new sleep inducer.
AP-C6 is a potent inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 6.5. AP-C6 concentration-dependently inhibits human cGKII activity in vitro. AP-C6 potentiate cAMP signaling by PDE inhibition[1].
Selenomethylene blue is an antioxidant and anti-inflammatory agent. Selenomethylene blue effectively inhibits the inflammatory paw edema in rats[1].
Thalidomide-O-C10-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
Spirolaxine is a plant growth inhibitor and possess significant anti-Helicobacter pylori activity. Spirolaxine exhibits cholesterol-lowering activity[1].
Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, and an antagonist of TRPV1 receptor with an IC50 of 562 nM.
T3Inh-1 is a potent and selective inhibitor of ppGalNAc-T3 (IC50=7 µM). T3Inh-1 reduces FGF23 hormone levels in both tissue cells and mice, without causing any toxic side effects. T3Inh-1 also prevents breast cancer cells. The enzyme ppGalNAc-T3 is implicated in at least two medically important pathways: cancer metastasis and stabilization of FGF23 (regulates phosphate levels in the bloodstream)[1].
Spectinomycin Dihydrochloride is a new parenteral antibiotic prepared from Streptomyces spectabilis.Target: AntibacterialSpectinomycin is an antibiotic produced by Streptomyces spectabilis. It is active against gram-negative bacteria and used for the treatment of gonorrhea. Spectinomycin binds to the 30S subunit of the bacterial ribosome and interrupts protein synthesis. One form of resistance has emerged in the 16S ribosomal RNA in Pasteurella multocida [1]. It is given by injection to treat gonorrhea, especially in patients who are allergic to penicillins. A resistance-conferring gene for spectinomycin can also be used as a selection marker in bacteria for molecular cloning purposes. Furthermore, Spectinomycin is used as a selection agent for transformed plant cells that contain the selectable marker gene Spcr [2].
Procyanidin B-5 3,3'-di-O-gallate is a potent inhibitor of squalene epoxidase with an IC50 of 0.55 μM. Procyanidin B-5 3,3'-di-O-gallate reduces cholesterol by inhibiting squalene epoxidase activity[1].
Funobactam (XNW4107) is a β-lactamase inhibitor, can be used for researching anti-bacteria[1].
Suc-AAA-pNA?is the substrate of analysis of the reversible inhibition of porcine pancreatic elastase (PPE)[1].
Epsilon-(gamma-glutamyl)-lysine is an N(6)-acyl-L-lysine derivative. The enzyme tissue transglutaminase (tTg) helps the formation of epsilon-(gamma-glutamyl)lysine bonds between ECM components in some disease, such as non-diabetic kidney, glaucoma filtration[1].
AKT-IN-2 is a potent, selective and orally bioavailable AKT inhibitor with an IC50 of 5 nM for AKT1[1].
Biotin-PEG4-amine is a biotin-labeled, PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Pulocimab is an anti-VEGFR2 monoclonal antibody (mAb). Pulocimab can be used for the research of cancers[1].
Boc-β-Lys(Z)-OH (dicyclohexylammonium) salt is a lysine derivative[1].
Azido-PEG9-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Cetilistat impurity 1 is an impurity of Cetilistat. Cetilistat, an inhibitor of pancreatic lipase, acts as an effective anti-obesity agent. Cetilistat inhibits rat and human pancreatic lipase activity with IC50s of 54.8 nM, and 5.95 nM, respectively[1].
(+)-Viroallosecurinine, isolated from Securinega virosa as a cytotoxic alkaloid, exhibits a MIC of 0.48 μg/mL for Ps. Aeruginosa and Staph. aureus[1]. Antibacterial activity[1].
NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction[1].
Zatebradine(UL-FS49) Hcl is a potent HCN channels antagonist, which decreased the heartbeat in a reversible manner; 92% inhibition of the hHCN1-mediated current at 10 uM.IC50 value: 10 uM(92% 92% inhibition of the hHCN1) [1]Target: hHCN channel antagonistThe pharmacological properties of hHCN1-mediated currents resembled those of native hyperpolarization-activated currents (I(h)), that is, blockade by Cs(+) (99% at 5 mm), ZD 7288 (98% at 100 microm) and zatebradine (92% at 10 microm) [1]. When voltage-clamp pulse trains were applied, cilobradine induced a use-dependent blockade of If that was stronger and faster than that with zatebradine. Recovery from blockade during prolonged hyperpolarization was significantly faster with zatebradine [2]. The selective HCN blocker zatebradine reduced the activity of oriens-lacunosum moleculare interneurons in wild-type but not HCN2(-/-) mice and decreased the frequency of spontaneous inhibitory currents in postsynaptic CA1 pyramidal cells [3].
Alpha-Naphthoflavone is a synthetic flavonoid, acts as a potent and competitive aromatase inhibitor with an IC50 and a Ki of 0.5 and 0.2 μM, respectively[1].
Zagociguat is the stimulator of soluble guanylate cyclase. Zagociguat increases nitric oxide (NO) signaling leading to an increase in cyclic guanosine monophosphate production. Zagociguat has the potential for the research of noncentral nervous system (CNS) disorders[1].
PXYD4 is a ribosomal protein S1 (RpsA) antagonist with Kds of 3.24 and 1.64 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb)[1].
TFAX 488,SE dilithium, an amine reactive green fluorescent dye, is insensitive to pH in the range 4-10. TFAX 488,SE dilithium forms bright and photostable conjugates with proteins and antibodies. TFAX 488,SE dilithium is suitable for use in flow cytometry, two-photon excitation microscopy (TPE), and super resolution microscopy techniques, such as dSTORM, SIM and STED. Excitation maximum=495 nm; emission maximum=515 nm; extinction coefficient=73,000 M-1cm-1; quantum yield=0.92.
IL-17A modulator-2 is a IL-17A modulator, extracted from patent WO2021239743+A1, example 27. IL-17A modulator-2 inhibits the biological action of IL-17A with a pIC50 of 8.3. IL-17A modulator-2 can be used for the research of diseases or disorders associated with modulation of IL-17A activity including diseases with an immune component or autoimmune pathol, cancer and neurodegenerative disorders[1].
TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with a Ki value of 5.3 nM for human PHD2. TP0463518 also inhibits human PHD1/PHD3 with IC50s of 18 and 63 nM as well as monkey PHD2 with an IC50 value of 22 nM[1].
Carfilzomib-d8 is deuterium labeled Carfilzomib. Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.
Dimethylamino-PEG3 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
(Rac)-Dencichin (2-Amino-3-(carboxyformamido)propanoic acid) is the racemate of Dencichin. Dencichin is a non-protein amino acid originally extracted from Panax notoginseng, and can inhibit HIF-prolyl hydroxylase-2 (PHD-2) activity[1].