HO-PEG5-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Nelfinavir(AG-1341) is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection. IC50 Valur: 2 nM (Ki for HIV-1 protease) [2]Target: HIV Proteasein vitro: In vitro exposure (72 hours) of HAECs to NEL (0.25-2 μg/mL) decreased both basal (2.5-fold) and insulin-induced NO production (4- to 5-fold). NEL suppressed insulin-induced phosphorylation of both Akt and eNOS at serine residues 473 and 1177, respectively. NEL decreased tyrosine phosphorylation of IR-β, IRS-1, and PI3K. Coexposure to troglitazone (TRO; 250 nM) ameliorated the suppressive effects of NEL on insulin signaling and NO production. Coexposure to TRO also increased eNOS expression in NEL-treated HAECs [1]. AG1343 is a potent enzyme inhibitor (Ki = 2 nM) and antiviral agent (HIV-1 ED50 = 14 nM). An X-ray cocrystal structure of the enzyme-AG1343 complex reveals how the novel thiophenyl ether and phenol-amide substituents of the inhibitor interact with the S1 and S2 subsites of HIV-1 protease, respectively [2].in vivo: In vivo studies indicate that AG1343 is well absorbed orally in a variety of species and possesses favorable pharmacokinetic properties in humans [2].
CER7-2’R,6R-d9 is deuterium labeled CER7-2’R,6R.
Vixarelimab (KPL-716) is a human anti-oncostatin M (OSM) monoclonal antibody that binds to the beta chain of the OSM receptor and inhibits IL-31 and OSM signalling. Vixarelimab can be used in studies of inflammatory skin diseases such as atopic dermatitis and itchy nodular rash[1].
FRATtide is a peptide derived from the GSK-3 binding protein that inhibits the phosphorylation of Axin and β-catenin. FRATtide inhibits GSK-3 binding to Axin[1].
Benzobicyclon is a pro-herbicide, which acts as an inhibitor of 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) in plant, and leads to bleaching and death[1].
Epicholesterol-2,2,3,4,4,6-d6 is the deuterium labeled Epicholesterol-2,2,3,4,4,6.
Vitamin B5-13C3,15N (hemicalcium hemihydrate) is the deuterium labeled Vitamin B5 (hemicalcium hemihydrate)[1].
WAY 163909 is a potent and selective 5-HT(2C) receptor agonist with a Ki of 10.5±1.1 nM.
NOSO-502 (NOSO502) is a novel inhibitor of bacterial translation, has MIC values of 0.5-4 ug/ml against standard Enterobacteriaceae strains and carbapenem-resistant Enterobacteriaceae (CRE) isolates that produce KPC, AmpC, or OXA enzymes and metallo-β-lactamases; interacts strongly with a specific site on the 30S subunit of bacterial ribosomes but has no significant activity against any of the 55 cell surface receptors, transporters, or ion channels; NOSO-502 is active against a panel of Gram-positive and Gram-negative bacteria, including carbapenem-resistant and polymyxin-resistant strains, and exhibits promising in vivo activity in various murine infection models, a favorable in vitro safety profile, and a low potential for resistance development.
NTR 368 is a peptide derived from p75 neurotrophin receptor (p75NTR) corresponding to residues 368-381 of the human receptor. NTR 368 has helix forming propensity in the presence of micellar lipid. NTR 368 is a potent inducer of neural apoptosis[1].
(±)-LY367385 is the racemate of LY367385. LY367385 is a highly potent and selective mGluR1a antagonist. LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with > 100 μM for mGlu5a[1][2].
H-DL-Phe-OMe.HCl is an alanine derivative[1].
Chloroquinoxaline sulfonamide (Chloroquinoxaline), a structural analogue of sulfaquinoxaline, is a topoisomerase II alpha/beta poison. Chloroquinoxaline sulfonamide is used to control coccidiosis in poultry, rabbit, sheep, and cattle[1]. Antitumor activity[2].
LL-37 SKE is an active fragment of LL-37[1].
Goshuyuamide-I (compound 4) is a kind of alkaloid. Goshuyuamide-I can be isolated from the fruits of Euodia rutaecarpa. Goshuyuamide-I can be used in the research of analgesics[1].
Adenosine-13C5 is the 13C labeled Adenosine[1]. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation[2][3].
AZD5582 is a novel class of dimeric Smac mimetics as potent IAP antagonist; binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP (IC50 = 15, 21, and 15 nM, respectively). IC50 value: 15/21/15 nM (cIAP1/cIAP2/XIAP) [1]Target: IAPs inhibitorAZD5582 causes cIAP1 degradation and induces apoptosis in the MDA-MB-231 breast cancer cell line at subnanomolar concentrations in vitro. When administered intravenously to MDA-MB-231 xenograft-bearing mice, AZD5582 results in cIAP1 degradation and caspase-3 cleavage within tumor cells and causes substantial tumor regressions following two weekly doses of 3.0 mg/kg. Antiproliferative effects are observed with AZD5582 in only a small subset of the over 200 cancer cell lines examined, consistent with other published IAP inhibitors [1]. AZD5582 significantly enhanced apoptosis induced by the death receptor (DR) agonist tumour necrosis factor-related apoptosis-inducing ligand (TRAIL). Importantly, killing by TRAIL plus AZD5582 was independent of adverse prognostic features including TP53 deletion which is strongly associated with chemoresistance in CLL [2].
Albendazole-2-Aminosulfone-d3 (hydrochloride) is the deuterium labeled Albendazole-2-Aminosulfone (hydrochloride).
Oxprenoate potassium is a potent mineralocorticoid (MR) antagonist. Oxprenoate potassium accentuates DEX (dexamethasone)-induced apoptosis[1].
Hexadecane-1-thiol-d33 is the deuterium labeled Hexadecane-1-thiol[1].
NDMC101 is a potent osteoclastogenesis inhibitor and inhibits osteoclast differentiation via down-regulation of NFATc1-modulated gene express. NDMC101 is similar to the DPP4 substrate and is a significant inhibitor of early T-cell activation via DPP4 inhibition. NDMC101can be used for study of bone disorders, such as rheumatoid arthritis, and synovial inflammation et al[1].
ZAP-180013 is a zeta-chain-associated protein kinase 70 (ZAP-70) inhibitor with an IC50 of 1.8 μM. ZAP-180013 inhibits the interaction of ZAP-70 SH2 domain with immunoreceptor tyrosine-based activation motif (ITAMs)[1].
Benzyloxy-C5-PEG1 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
SLK/STK10-IN-1 is a potent and selective inhibitor of SLK and STK10 with nanomolar potency.
Aurantio-obtusin β-D-glucoside (Glucoaurantio-obtusin), isolated from Cassiae Semen (seeds of Cassia tora), is a glucoside of aurantio-obtusin[1].
Bemesetron (MDL 72222) is a selective 5-HT3 receptor antagonist with an IC50 of 0.33 nM[1]. Neuroprotective effects[2].
Cytochalasin O (compound 13) is a secondary metabolite of the phytopathogenic fungus P. sp. CIB-109[1].
L-739594 is a HIV-1 protease inhibitor, with an IC50 of 1.8 nM[1].