SARS-CoV-2-IN-44, a inhibitor of SARS-CoV-2, inhibits viral replication, with an EC50 of 0.6μM. SARS-CoV-2-IN-44 has no evident cytotoxic effect in Calu-3 cells and can be used for antiviral research[1].
m-PEG7-CH2CH2CHO is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
STL5-T-0057 (compound 68) is an selective ALDH1 B1 inhibitor with an IC50 value of 30 nM. STL5-T-0057 inhibits cell growth of SW480 cells in adherent and spheroid conditions with IC50 values of 2.46 and 0.39 μM, respectively. STL5-T-0057 can be used for the research of cancer[1].
Linagliptin-d4 is deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.
24:0 L-carnitine-d4 is deuterium labeled 24:0 L-carnitine.
ZGN-1061 (Aclimostat) is a novel potent, selective Methionine aminopeptidase 2 (MetAP2) inhibitor being investigated for treatment of diabetes and obesity; reduces body weight in diet-induced obese (DIO) insulin-resistant mice, also produced improvements in metabolic parameters, including plasma glucose and insulin, and, in HepG2 cells, initiated gene changes similar to beloranib; does not increase coagulation markers in dogs and ZGN-1061 had a greatly improved safety profile in rats relative to beloranib. Diabetes Phase 2 Clinical
(R)-FT709 is an active compound. (R)-FT709 can be used for the research of cancers[1].
p53 Activator 7 is a p53 mutation Y220C (MDM-2/p53) activator with an EC50 of 104 nM. p53 Activator 7 can bind to p53 mutant and restore its ability to bind DNA (WO2022213975A1; Example B-1)[1].
Secologanin, a secoiridoid glucoside, is a pivotal terpenoid intermediate in the biosynthesis of biologically active monoterpenoid indole alkaloids such as reserpine, ajmaline, and vinblastine. Secologanin synthase (cytochrome P450 isoform CYP72A1) catalyzes the oxidative cleavage of loganin into Secologanin[1][2].
DMPE is the dimyristoylphosphatidylcholine. DMPE is a liposome used to deliver drugs[1].
Z-Gly-Gly-Phe-OH is an active compound. Z-Gly-Gly-Phe-OH can be used for the synthesis of enzymic peptide[1].
α-(Methylamino)isobutyric acid is a specific substrate for amino acid transport system A (ATA1). ATA mediate the uptake of short-chain neutral amino acids in a Na+-dependent manner[1].
N-(azide-PEG3)-N'-(Amine-C3-Amide-PEG4)-Cy5 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM.Target: Potassium Channelgliclazide further characterize its mechanism of hypoglycemic effect: the observed improvements in insulin sensitivity and in GLUT4 translocation indicate that gliclazide counters the hydrogen peroxide-induced insulin resistance in 3T3L1 adipocytes and also would further augment the hypoglycemic effect of this drug as insulinotropic sulfonylurea [1]. Gliclazide blocked whole-cell beta-cell KATP currents with an IC50 of 184 +/- 30 nmol/l (n = 6-10) but was much less effective in cardiac and smooth muscle (IC50s of 19.5 +/- 5.4 micromol/l (n = 6-12) and 37.9 +/- 1.0 micromol/l (n = 5-10), respectively). In all three tissues, the action of the drug on whole-cell KATP currents was rapidly reversible. In inside-out patches on beta-cells, gliclazide (1 micromol/l) produced a maximum of 66 +/- 13 % inhibition (n = 5), compared with more than 98 % block in the whole-cell configuration. Gliclazide is a high-potency sulphonylurea which shows specificity for the pancreatic beta-cell KATP channel over heart and smooth muscle. In this respect, it differs from glibenclamide [2].
Daphnilongeranin A is a natural product, that can be isolated from Daphniphyllum longeracemosum[1].
AZD-0284 is an inverse agonist of the nuclear receptor RORγ. In development for the treatment of plaque psoriasis vulgaris and respiratory tract disorders[1].
PROTAC BRD9 Degrader-4 is a BRD9 bifunctional degrader for treating cancer.
Hydroxyethylamine (Compd VII) is a SARS-CoV-2 3CLpro inhibitor with an IC50 of ~10 μM in the spread assay. Hydroxyethylamine has potent antiviral activities[1].
Nurr1 agonist 7 (compound 110) is a Nurr1 agonist with an EC50 value of 0.12 μM[1].
(3S,5R)-Rosuvastatin is the (3S,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM[1]. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM[2]. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels[3].
Amino Tadalafil is an analog of tadalafil. Tadalafil is a potent inhibitor of phosphodiesterase 5 with applications in several conditions, including erectile dysfunction, pulmonary arterial hypertension, and lower urinary tract dysfunction.
Clonidine hydrochloride is an agonist of α2-adrenoceptor and potent antihypertensive agent.
7-Aminocoumarin is a pH-insensitive blue fluorophore. 7-Aminocoumarin is widely used as laser dyes in the blue-green region. 7-Aminocoumarin can be used to tag recombinant proteins on the cell surface and inside living cells through PRIME (probe incorporation mediated by enzymes). 7-Aminocoumarin can be visualized in acidic organelles such as endosomes[1][2].
(R)-Ethyl 2-((tert-butoxycarbonyl)amino)-3-hydroxypropanoate is a serine derivative[1].
8-Azido-octanoyl-OSu is a click chemistry reagent containing an azide group. Used as a building block to introduce 8-azidooctanoic acid (CAS 217180-76-2) fragment. This fragment is used for further modifications using Click-chemistry (CuAAC), as a protected aminogroup or is used in physico-chemical investigations[1].
MrgprX2 antagonist-8 (example 5b) is a MrgprX2 antagonist. MrgprX2 antagonist-8 can be used for the research of inflammatory disorders[1].
Thalidomide-4-O-C10-COOH is a E3 ligase ligand-linker conjugate that can be used in the synthesis of PROTACs.
(+)-Pinoresinol monomethyl ether O-β-D-glucoside (Compound 6) is a natural product that can be isolated from the stems of Tinospora sinensis[1].
LY393615 (NCC1048) is a novel neuronal Ca2+ (calcium channel) and Na + channel (sodium channel) blocker with IC50s of 1.9 μΜ and 5.2 μΜ for α1A and α1B calcium channel subunits. LY393615 has good brain penetration and neuroprotective effects in models of in cerebral ischemia that can be used for neurological disease research[1].