IMP2-IN-2 (compound 6) is a potent and selective IMP2 inhibitor, with IC50s of 120.9 μM and 236.7 μM for IMP2 interaction with RNA_A and RNA_B, respectively. IMP2-IN-2 can be used for the research of cancer[1].
Aflatoxin M1 is a major metabolite of Aflatoxin B1. Aflatoxin M1 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2[1].
Glutaric anhydride-d6 is the deuterium labeled Glutaric anhydride[1].
Mapenterol hydrochloride is a type of β2-adrenoceptor agonist[1].
Sodium Picosulfate inhibits absorption of water and electrolytes, and increases their secretion.Target: OthersSodium Picosulfate displays cytotoxic effects on cultured liver cells. 800 and 1600 mg/mL induces dose-dependently vacuolic and fatty change as well as necrosis combined with a lowered mitotic activity and a slight increase in LDH values of the rapidly growing cultured liver cells of rabbit. Comparable but less severe effects are observed in 4-day old liver cell cultures of rat, while liver cells cultured for 6 to 11 days tolerate 1600 mg/mL Sodium Picosulfate. In human liver cultures the number of cells is slightly lowered at 800 and 1600 mg/mL and the number of nuclei in division is decreased dependent on dose [1]. Sodium Picosulphate has no major influence on ileal and colonic epithelial cell proliferation. In a 12 weeks study, 10 mg/kg Sodium Picosulphate continuously treatment does not influence the labeling index of Brdu (LI) in the ileum and induces no statistically significant increase of the LI when the treated groups are compared with the control group. The proliferative pattern along the crypts remains unchanged with sodium picosulphate treatment throughout the study [2]. Sodium Picosulphate does not induce chronic changes in colonic motility in rats under long-term treatment. 10mg/kg/day Sodium Picosulphate pretreated for 23 weeks does not induce any significant change in the duration of long spike bursts (LSB) which are associated with phasic contractions, or in LSB frequency in the fasted state or after a 3-gram meal [3].
PSMA-11 is a positron emission tomography (PET) tracer. PSMA-11 detects prostate cancer relapses and metastases by binding to the extracellular domain of prostate-specific membrane antigen (PSMA)[1].
6a,12a-Dehydro-α-toxicarol is a natural product that can be isolated from Amorpha fruticosa[1].
Opioid receptor modulator 1 is a opioid receptor modulator extracted from patent WO2014072809A2, Compound RA11 in EXAMPLE 7.
8-Hydroxypinoresinol is a tetrahydrofurofuran lignan that has cytoprotective effects against peroxynitrite-induced LLC-PK1 cell damage[1].
Fenoterol-d6 hydrobromide (Th-1165a-d6) is the deuterium labeled Fenoterol hydrobromide. Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research[1][2].
Seneciphylline is a toxic pyrrolizidine alkaloid in Senecio plants[1]. Seneciphylline significantly increases the activities of epoxide hydrase and glutathione-S-transferase but causes reduction of cytochrome P-450 and related monooxygenase activities[2].
Bryodulcosigenin is an extract of the roots of Bryoniadioica with anti-inflammatory effect[1].
CPI-1328 is an EZH2 inhibitor with a Ki value of 63 fM.
Nosantine racemate is the racemate of Nosantine. Nosantine is an inducer of IL-2 or enhancer of IL-2 induction by phytohemagglutinin (PHA).
KY-1044 (Alomfilimab; SAR 445256) is a fully human IgG1 antibody targeting inducible costimulatory receptor (ICOS). KY-1044 depletes ICOShigh cells via antibody-dependent cellular cytotoxicity (ADCC) through the engagement of FcgRIIIa. KY-1044 act as a costimulatory molecule on cells expressing lower ICOS levels, such as CD8+ TEff cells (through FcgR-dependent clustering). KY-1044 exploit the differential expression of ICOS on T-cell subtypes to improve the intratumoral immune contexture and restore an antitumor immune response[1].
Medicarpin is a flavonoid isolated from Medicago sativa. Medicarpin induces apoptosis and overcome multidrug resistance in leukemia P388 cells by modulating P-gp-mediated efflux of drugs[1].
SQ 28853 is an inhibitor of ACE with diuretic properties.
Palvanil is a capsaicin analogue, shows strong desensitizing capability against the TRPV1 receptor. Palvanil shows anti-nociceptive and anti-inflammation effects[1][2].
Citalopram hydrobromide is an antidepressant drug of the selective serotonin reuptake inhibitor (SSRI) class. It has US FDA approval to treat major depression.
Gemcitabine monophosphate (Gemcitabine 5′-phosphate) is one of the active intermediates of Gemcitabine (HY-17026). Gemcitabine monophosphate shows synergistic anti-cancer effects[1][2].
Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 1.94 nM.Target: ACEEnalaprilat has high affinity for human endothelial ACE with IC50 of 1.94 nM in vitro binding assay by displacing a saturating concentration of [125I]351A, a radiolabeled lisinopril analogue from ACE binding sites, and shows bradykinin/angiotensin I selectivity ratio of 1.00 calculated from double displacement experiments [1]. Enalaprilat attenuates the IGF-I induced neonatal rat cardiac fibroblast growth (30% reduction) in a concentration-dependent fashion, with IC50 of 90 mM [2].Administration of Enalaprilat induces a significant reduction of MAP at 70 minutes compared with the placebo group during haemorrhagic shock in rats, and results in a 50% reduction of CO, a general tendency of EB extravasation which is significant in the kidney and lungs, and a significant increase in ileal EB extravasation (53%) [3].
C12-NBD Sphinganine is a fluorescent ceramidase substrate. C12-NBD Sphinganine can be used for the measurement of alkaline and neutral ceramidase activity from a variety of sources[1][2][3].
SSR69071 is a potent, orally active and selective inhibitor of neutrophil elastase. SSR69071 reduces myocardial infarct size following ischemia-reperfusion injury[1]. SSR69071 displays a higher affinity for human elastase (Ki=0.0168 nM) than for rat (Ki=3 nM), mouse (Ki=1.8 nM), and rabbit (Ki= 58 nM) elastases[2].
NFAT Inhibitor (VIVIT peptide) is a selective inhibitor of calcineurin-mediated dephosphorylation of nuclear factor of activated T cells (NFAT). Sequence: Met-Ala-Gly-Pro-His-Pro-Val-Ile-Val-Ile-Thr-Gly-Pro-His-Glu-Glu;MAGPHPVIVITGPHEE.
Felbamate-d5 is the deuterium labeled Felbamate[1]. Felbamate (W-554) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA)[2][3].
SARS-CoV-2 Mpro-IN-6 is a covalent, irreversible and selective SARS-CoV-2 Mpro inhibitor with an IC50 of 0.18 μM. SARS-CoV-2 Mpro-IN-6 does not inhibit human cathepsins B, F, K, and L, and caspase 3[1].
A potent and selective inhibitor of FAK phosphorylation with biochemical IC50 of 1.2 pM (pFAK Y397), cellular IC50 of 1 nM; displays 8-fold selectivity over PYK2, 26-fold selectivity over RSK1/2 , and >1000-fold selectivity over SRC, AURKA, AURKB, INSR, and KDR; suppresses pFAK Y397 and pFAK Y861 in tumors and liver, shows tumor growth inhibition in TOV21G xenografts in mice.
Benzyl D-serinate hydrochloride is a serine derivative[1].
Fluphenazine decanoate is a long-acting phenothiazine neuroleptic that used to treat schizophrenia. Fluphenazine decanoate is also a high and continuous dopamine D2 receptor blocker[1][2][3].
Picrotoxin is a noncompetitive antagonist of GABAA receptor.