K 01-162 (K162) binds and destabilizes AβO (β-amyloid), with an EC50 of 80 nM. IC50 value: 80 nM (EC50)Target: Amyloid-βin vitro: The active drug candidate K162 (EC50 = 0.080 μM), stabilizes hydrophobic core I of Aβ42 peptide (residues 17-21) to its α-helical conformation by interacting specifically in this region. [1] K01-162 shows full MC65 protection at 125 nM, an EC50 of 80 nM, and no cytotoxicity up to 50 μM. [2]in vivo:K01-162 can reduce the brain amyloid burden that exists in both fibrillar and RIPA-soluble, non-fibrillar forms.[2]
Bruceoside A, an abundant quassinoid glycoside in Fructus Bruceae, possesses anti-cancer activity[1].
Iohexol is a contrast agent.Target: OthersIohexol is a contrast agent. The osmolality of iohexol ranges from 322 mOsm/kg-approximately 1.1 times that of blood plasma-to 844 mOsm/kg, almost three times that of blood. Despite this difference, iohexol is still considered a low-osmolality contrast agent; the osmolality of older agents, such as diatrizoate, may be more than twice as high. From Wikipedia.
NEP-IN-1 is a neutral endopeptidase (NEP) inhibitor with IC50 of 2 nM for dNEP.
Atorvastatin acetonide is an impurity of Atorvastatin, and extracted from patent WO2011131605A1, Compound 4. Atorvastatin is an orally active HMG-CoA reductase inhibitor and has the ability to effectively decrease blood lipids[1].
Ginsenoside Rb2 is one of the main bioactive components of ginseng extracts. Rb2 can upregulate GPR120 gene expression.
Uty HY Peptide (246-254), derived from the ubiquitously transcribed tetratricopeptide repeat gene on the Y chromosome (UTY) protein as an H-Y epitope, H-YDb, is a male-specific transplantation antigen H-Y[1].
Tipranavir-d4 (PNU-140690-d4) is the deuterium labeled Tipranavir. Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM[1][2]. Tipranavir inhibits SARS-CoV-2 3CLpro activity[3].
trans-Nerolidol is a sesquiterpene alcohol. It can be isolated from f aerial parts of Warionia saharae ex Benth. trans-Nerolidol improves the anti-proliferative effect of Doxorubicin (HY-15142A) against intestinal cancer cells in vitro. trans-Nerolidol also has anti-fungal activity[1][2].
Stephavanine is a compound isolated from the roots of Stephania abyssinica[1].
N-(2,4-Dichlorobenzoyl)glycine is a Glycine (HY-Y0966) derivative[1].
5-Aza-7-deazaguanine is a substrate for wild-type (WT) E. coli purine nucleoside phosphorylase and its Ser90Ala mutant in the synthesis of base-modified nucleosides[1].
AHR antagonist 3 is a 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compound and an aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 192, has an IC50 of 341 nM. AHR antagonist 3 has anti-cancer effects[1].
Boc-NH-PEG1-CH2CH2COOH is a cleavable (1 unit PEG) ADC linker and also a PEG- and Alkyl/ether-based PROTAC linker can be used in the synthesis of antibody-drug conjugates (ADCs) or PROTACs[1][2].
Maresin 2 is an anti-inflammatory and pro-resolving mediator from human macrophages. Maresins are a new family of anti-inflammatory and pro-resolving lipid mediators biosynthesized from docosahexaenoic acid (DHA) by macrophages[1].
NSC 190686-d3 is the deuterium labeled NSC 190686[1].
Fmoc-Ser-OMe (Fmoc-L-Ser-OMe) is a hydroxylated L-amino acid protected with a 9-fluorenylmethyloxycarbonyl (Fmoc) group. Fmoc-Ser-OMe involves in chlorophyll–amino acid conjugates synthesis, and acts as a chromo/fluorophores modified protein and emits visible to near-infrared lights efficiently. Fmoc-Ser-OMe glycosylates and produces small mucin-related Olinked glycopeptides, as an alcohol acceptor[1][2].
Acetylhydrolase-IN-1 is a 1-Alkyl-2-acetylglycerophosphocholine esterase (Alkylacetyl-GPC: acetylhydrolase) inhibtor.
Fluorescent Red Mega 480 is a dye that is specifically designed for multicolor techniques. Fluorescent Red Mega 480 is characterized by an extremely large stoke′s shift between excitation and emission maxima[1].
IACS-52825 is a potent and selective DLK inhibitor with Kd of 1.3 nM, useful for the study of chemotherapy-induced peripheral neuropathy[1].
Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase[1].
Barpisoflavone A is a natural product from Apios americana[1].
(E)-4-Hydroxytamoxifen, the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator.
MBD (7-(p-Methoxybenzylamino)-4-nitrobenz-2,1,3-oxadiazole), a new fluorescent probe for protein and nucleoprotein conformation, is applied to bacterial ribosomes and to bovine trypsinogen and trypsin. MBD is strongly fluorescent upon binding to a hydrophobic area of a macromolecule[1][2].
5-Methylfurfural is a naturally occurring substance, found in cigarette smoke condensate, licorice essential oil, stored dehydrated orange powder, baked potato flour, volatile compounds of roast beef, aroma concentrate of sponge cake. bread and in coffee, tea and cocoa[1]. A flavoring agent.
UNC10217938A is a 3-deazapteridine analog with strong oligonucleotide enhancing effects. UNC10217938A enhances oligonucleotides effects by modulating their intracellular trafficking and release from endosomes. UNC10217938A also enhances the effects of antisense and siRNA oligonucleotides[1].
CWI1-2 hydrochloride is an IGF2BP2 inhibitor that binds IGF2BP2 and inhibits its interaction with m6A-modified target transcripts, induces apoptosis and differentiation, and shows promising anti-leukemic effects[1].
Stevioside is a natural sweetener extracted from leaves of Stevia rebaudiana, with anticancer activity[1].
HAV 3C proteinase-IN-1 is a inhibitor of Hepatitis A virus 3C proteinase.
CBR-6672 is a mycobacterium tuberculosis (Mtb) type II NADH dehydrogenase inhibitor, with the MIC of 0.14 μM against Mtb[1].