Rehmannioside B is a desacyl derivative of Picrorhizaoside B, which can be isolated from the methanol extract of the rhizomes of Picrorhiza kurroa Royle ex Benth. (Plantaginaceae)[1].
Idasanutlin (RG7388) is a potent and selective MDM2 antagonist, inhibiting p53-MDM2 binding, with an IC50 of 6 nM.
Caprazol is a core structure of Caprazamycin (HY-N9425)[1].
5-HT1A modulator 2 hydrochloride, a derivative of 8-OH-DPAT (HY-112061), is a modulator of 5-HT1A with a Ki of 53 nM for 5-HT1A binding[1].
Eudesmane K exhibits insecticidal activity against main pests to crops Lipaphis erysimi, Sitobion avenae, Rhopalosiphum padi, and Aphis craccivora[1].
GCN2-IN-1 is a potent general control nonderepressible 2 kinase (GCN2) inhibitor with IC50s of <0.3 μM in the enzyme and cell assay.
BMS CCR2 22 is a potent, specific and high affinity CC-type chemokine receptor 2 (CCR2) antagonist with excellent binding affinity (binding IC50 of 5.1 nM) and potent functional antagonism (calcium flux IC50 of 18 nM and chemotaxis IC50 of 1 nM)[1][2].
MAGL-IN-6 is a potent MAGL inhibitor with an IC50 of 4.71 nM. MAGL-IN-6 can be used for neurological disorders research (WO2020065613A1; example 234)[1].
Mirtazapine is a potent tetracyclic antidepressant.Target: 5-HT ReceptorMirtazapine, the novel antidepressant, has a dual mode of action. It is a noradrenergic and specific serotonergic antidepressant (NaSSA) that acts by antagonizing the adrenergic alpha2-autoreceptors and alpha2-heteroreceptors as well as by blocking 5-HT2 and 5-HT3 receptors [1].Mirtazapine appears to have a substantial ameliorating effect on hot flushes and perspiration bouts. It is postulated that the 5-HT(2A) blocking properties of mirtazapine is accounted in the symptomatic relief of hot flushes [2]. After 4-24 weeks of treatment, mirtazapine induced downregulation of platelet alpha(2A)-adrenoceptors (up to 34%) and Galphai proteins (up to 28%), and the upregulation of GRK 2 (up to 30%). Treatment with mirtazapine reversed this abnormality and induced downregulation of alpha(2A)-adrenoceptor/Galphai complex [3].
LY450108 is an alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor potentiator. IC50 value: Target: AMPA receptors mediate most of the excitatory neurotransmission and play a key role in synaptic plasticity in the mammalian central nervous system (CNS). Recent evidence has shown that in addition to modulating fast synaptic plasticity and memory processes, AMPA receptor potentiators alter downstream signalling pathways and may thereby have utility in other CNS disorders.
N-Octanoyl-DL-homoserine lactone is a member of N-acyl homoserine lactones (AHLs) family, also one of the signal molecule of quorum-sensing (QS) signals. N-Octanoyl-DL-homoserine lactone can regulate the production of siderophores and present positive correlation in Aeromonas sobria strain AS7. N-Octanoyl-DL-homoserine lactone can also regulate the secretion of proteases and stimulate the production of total volatile basic nitrogen (TVB-N)[1].
RAD51-IN-6 is a potent inhibitor of RAD51. RAD51 is a eukaryote gene. RAD51-IN-6 has the potential for the research of conditions involving mitochondrial defects (extracted from patent WO2021164746A1, compound 23)[1].
Ph-HTBA is a high-affinity, brain-penetrating modulator for CaMKIIα. Ph-HTBA has binding affinity for CaMKIIα with a Kd value of 757 nM. Ph-HTBA can be used for the research of ischemia and neurodegenerative disorders[1].
Reltecimod (AB-103) is a T-cell-specific surface glycoprotein CD28 (TP44) antagonist. Reltecimod has beneficial effects against different bacterial infections, their exotoxins and endotoxins, and ionizing radiation. Reltecimod modulates the inflammatory response by targeting and attenuating the critical CD28/B7-2 co-stimulatory pathway, without inhibiting it. Reltecimod can be used to research necrotizing soft-tissue infections (NSTIs)[1][2].
PS 210 is a potent, specific activator of PDK1 that target the PIF-binding pocket of PDK1, does not alter the activity of any of the 121 kinases (S6K, PKB/Akt or GSK3).
Somatostatin-25 is a endogenous neuropeptide hormone that shows inhibitory activity against secretion of growth hormone.
3’,5’-Bis-O-benzoyl-2’-deoxy-2’-fluoro-β-D-arabinouridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Calmodulin-Dependent Protein Kinase II (290-309) is a potent CaMK antagonist with an IC50 of 52 nM for inhibition of Ca2+/calmodulin-dependent protein kinase II.
2'-Hydroxylagarotetrol is a phenylethychromone derivative[1].
Deacetylanisomycin is a potent growth regulator in plants and an inactive derivative of Anisomycin. Anisomycin is a potent protein synthesis inhibitor [1].
Oct3/4-inducer-1 (compound 2) is a potent Oct3/4 inducer. Oct3/4-inducer-1 promotes expression and stabilization of Oct3/4, and enhances its transcriptional activity in diverse human somatic cells[1].
4-Phenylbutyric acid-d2 is the deuterium labeled 4-Phenylbutyric acid[1]. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
AST 7062601 (AST070) is a Ucp1 inducer that strongly induces endogenous Ucp1 expression in primary mouse brown adipocytes. Ucp1 refers to uncoupling protein, found in brown and beige fat cells. In mammals, UCP1 oxidizes fatty acids and uncouples ATP production in mitochondria to promote energy dissipation as heat. AST 7062601 can be used to study thermogenic, uncoupled respiration[1].
2',4',5'-Trimethoxy-2'',2''-dimethylpyrano[5'',6'':6,7]isoflavone is an isoflavone[1].
A novel potent, selective CDK8 inhibitor with IC50 of 0.5 uM against recombinant Cyclin C/CDK8 complex; displays no activity against several CDKs involved in cell cycle including CDK19 (IC50>30 uM); inhibits IFNγ-induced phosphorylation of STAT1 at Ser 727 site in BMDCs, selectively upregulates IL-10 with EC50 of 1 uM.
Gadobutrol is a medicinal product used in diagnostic magnetic resonance imaging (MRI) in adults and children. It provides contrast enhancement during cranial, spinal, breast, or other investigations. In the central nervous system, Gadobutrol works by highlighting any areas with disrupted blood brain barrier (BBB) and/or abnormal vascularity. In breast tissue, Gadobutrol exposes the presence and extent of malignant breast disease. Similarly, gadobutrol is also used in contrast-enhanced magnetic resonance angiography (CE-MRA) for the diagnosis of stroke, detection of tumor perfusion, and presence of focal cerebral ischemia.
HCV-IN-30 (compound 48) is a HCV NS5A replication complex inhibitor, with IC50s of 901 and 102 nM for genotypes 1a and 1b replicons, respectively[1].
Iproniazid is a non-selective, irreversible monoamine oxidase (MAO) inhibitor of the hydrazine class. Iproniazid has antidepressive activity[1].
Taltobulin intermediate-4 is an intermediate in the synthesis of Taltobulin (HY-15584). Taltobulin is a common toxin component in ADC preparation (ADC Cytotoxin), and it is also a powerful tubulin (Microtubule/Tubulin) inhibitor. Taltobulin disrupts tubulin polymerization, induces mitotic arrest, and induces apoptosis[1].
BODIPY-cholesterol is an intrinsically lipophilic, and cell-permeable analog of cholesterol with a fluorescent BODIPY group. BODIPY-cholesterol can be used to monitor sterol uptake and inter-organelle sterol flux in cells. (Excitation/Emission: 480/508 nm)[1].