spatial

Bucladesine sodium (DC2797) is a cAMP analog with cell-permeable properties. Bucladesine sodium is also a cAMP-dependent protein kinase (PKA) activator and a phosphodiester (PDE) inhibitor. Bucladesine sodium has anti-inflammatory activity.

SB 202190 (FHPI) is a p38 MAPK inhibitor that inhibits p38α and p38β2 (IC50=50/100 nM) selectively and cell-permeably. SB 202190 has antitumor activity and also induces the differentiation of human embryonic stem cells into cardiomyocytes.

CGP 35348 is a selective antagonist of GABAB receptor (EC50 = 34 μM). CGP 35348 can be used in studies of neuromuscular coordination and spatial learning after neonatal brain damage in albino mice.

Androsta-1,4,6-triene-3,17-dione is a lipophilic and specific aromatase inhibitor (Ki: 0.18 μM) that inhibits estrogen biosynthesis, exhibits antifertility effects, and induces impairment of spatial memory.

Ginsenoside Rg1 (Panaxoside Rg1) is a class of steroid glycosides, and triterpene saponins found exclusively in the plant genus Panax (ginseng). It improves spatial learning and increase hippocampal synaptophysin level in mice, plus demonstrates estrogen-like activity.

3-Aminopropyltriethoxysilane (APTES) immobilizes biomolecules on silicon-based materials, such as Si3N4, while acting as a spacer to provide spatial freedom and higher activity for immobilized biomolecules to build analytical platforms for biosensing, recognition and more.

Amylose is a polysaccharide composed of α-D-glucose units linked by α(1→4) glycosidic bonds, accounting for about 20% of the total amount of starch. Amylose spatial conformation curls into a helix and forms a blue complex with iodine, which is widely used in the food industry, and can be used in a variety of researches as a natural product and a biochemical reagent.

RMC-6291 is an orally active, covalent inhibitor of KRAS G12C (ON) that forms a tri-complex within tumor cells between KRAS G12C (ON) and cyclophilin A (CypA), thereby preventing KRAS G12C (ON) from signaling via steric blockade of RAS effector binding and eliciting deep and durable suppression of RAS pathway activity in KRAS G12C tumor models [1].

CYCLOHEPTENE compounds belong to the category of cycloolefin organic compounds. Its seven-membered ring that have moderate spatial tension, higher chemical stability, and is less likely to undergo side reactions such as spontaneous ring opening.

ZIP acetate is a novel, cell-permeable inhibitor of protein kinase Mζ (PKMζ), a constitutively active, atypical PKC isozyme involved in LTP maintenance. Selectively blocks PKMζ-induced synaptic potentiation in hippocampal slices in vitro. Reverses late-ph

H-89 is a selective and potent protein kinase A inhibitor (IC50: 48 nM), a candidate cardioprotectant, induces spatial learning impairment in rats, and can be used to study myocardial infarction.

(S)-MCPG ((+)-MCPG) is a class I/II metabotropic glutamate receptors (mGluRs) antagonist that blocks spatial learning and long-term enhancement of the dentate gyrus in vivo in rats, and can be used to study neurological disorders.

Adekalant (also known as H 345/52) is an innovative antiarrhythmic compound characterized by minimal proarrhythmic activity. It blocks HERG-mediated currents in a concentration-dependent manner, with a half-maximal inhibitory concentration (IC50) of 230 nM. Adekalant binds preferentially to open channels and exhibits rapid kinetic behavior, being trapped when channels close. Its voltage-independent properties have been observed during square pulse and action potential clamp protocols. Research suggests that delaying the repolarization of human cardiac muscle through I(Kr) blockage is the primary mechanism of Adekalant’s action. It effectively blocks I(Kr) while having relatively low efficacy in blocking I(Ca), delaying ventricular repolarization without significantly increasing temporal or spatial dispersion and without inducing early afterdepolarizations or torsades de pointes (TdP).

AChE/BChE-IN-25 (Compound 6e) is an orally active inhibitor of hAChE and eqBChE, with IC50 values of 7.9 nM and 0.79 nM, respectively. This compound exhibits antioxidant activity, effective in scavenging free radicals with an IC50 of 22.91 μM. AChE/BChE-IN-25 demonstrates neuroprotective effects by reducing mitochondrial and cellular oxidative stress in a Drosophila Alzheimer's model and improves spatial and cognitive memory impairments induced by Scopolamine in mouse models.

hAChE/hBuChE-IN-1 (compound C2) acts as a dual inhibitor of cholinesterases, exhibiting IC50 values of 514 nM for hAChE and 358 nM for hBuChE. It is orally active and capable of enhancing cognitive function and spatial memory.

β-CCM is a benzodiazepine receptor inverse agonist with anxiogenic and convulsant effects. It enhances emotional reactivity and reduces interference sensitivity in spatial working memory tasks. β-CCM is applicable in research related to anxiety disorders.

BChE/p38-α MAPK-IN-1 is a selective dual inhibitor targeting hBChE (IC50 = 772 nM) and p38α MAPK (IC50 = 191 nM). It reduces the production of pro-inflammatory cytokines (IL-1β, IL-6, IL-8, TNF-α) in cells, improves scopolamine-induced cognitive impairment, alleviates LPS-induced spatial learning deficits, and exhibits anti-neuroinflammatory effects in mice, making it applicable for Alzheimer's disease (AD) research.

PI3K/AKT/ERK/CREB activator 1 is an orally active agent that stimulates the PI3K/AKT/ERK/CREB signaling pathway. It supports neuronal survival and function, enhances neuron proliferation, and revives the activity of damaged neurons, while also aiding in synapse formation. By reducing pro-inflammatory cytokine levels, it alleviates neuroinflammation and preserves synaptic ultrastructure, thereby restoring spatial memory in Alzheimer's disease models. PI3K/AKT/ERK/CREB activator 1 serves as a valuable tool for Alzheimer's disease research.

POLRMT-IN-3 is a photoactivatable inhibitor of mitochondrial RNA polymerase (POLRMT). In its inactive form in darkness, POLRMT-IN-3 rapidly releases the active parent compound LJ03 when exposed to 405 nm light, enabling precise spatial and temporal inhibition of POLRMT. It exhibits anti-tumor activity and is useful for research in cancers like pancreatic and ovarian tumors.

BDM71230 is an orally active inducer of the Insulin-Degrading Enzyme (IDE), with an EC50 of 1.9 μM for human IDE. This compound binds to the IDE dimer interface, enhancing IDE's catalytic activity through spatial interaction. BDM71230 boosts the hydrolysis of insulin by IDE while slightly diminishing insulin's hypoglycemic effect. It serves as a pharmacological tool for investigating IDE functions, particularly in studies related to glucose intolerance.

JC-D7 is a selective fluorescent probe designed for the specific labeling of synthetic polyphosphate in vitro as well as endogenous polyphosphate in living cells, enabling high-sensitivity visualization, spatial tracking, and functional analysis of polyphosphate dynamics in cellular metabolism and signaling research.

Guanfacine-13C,15N3 is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine (T22824) is an α2-adrenergic receptor (α2-AR) agonist with Kivalues of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.1It has EC50values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki= 19 nM in a radioligand binding assay).2Guanfacine (0.3-5 mg/kg) binds to adrenergic receptors in the central nervous system and lowers blood pressure in hypertensive rats in a dose-dependent manner.3It also improves spatial working memory deficits induced by hypobaric hypoxia in rats.4Formulations containing guanfacine are used in the treatment of high blood pressure and attention deficit hyperactivity disorder (ADHD).

para-amino-Blebbistatin is a more water-soluble form of (S)-4'-nitro-blebbistatin , which is a more stable and less phototoxic form of (-)-blebbistatin .1,2,3 (-)-Blebbistatin is a selective cell-permeable inhibitor of non-muscle myosin II ATPases that rapidly and reversibly inhibits Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species (IC50s = 0.5-5 μM), while poorly inhibiting smooth muscle myosin (IC50 = 80 μM).2,3,4 Through these effects, it blocks apoptosis-related bleb formation, directed cell migration, and cytokinesis in vertebrate cells. However, prolonged exposure to blue light (450-490 nm) results in degradation of blebbistatin to an inactive product via cytotoxic intermediates, which may be problematic for its use in fluorescent live cell imaging applications.5,6 The addition of a 4'-amino group increases its water solubility, decreases the inherent fluorescence, stabilizes the molecule to circumvent its degradation by prolonged blue light exposure, and decreases its phototoxicity while retaining the in vitro and in vivo activity of blebbistatin.7 para-amino-Blebbistatin has the same stereochemistry as the active (-)-blebbistatin enantiomer. |1. Várkuti, B.H., Képiró, M., Horváth, I.á., et al. A highly soluble, non-phototoxic, non-fluorescent blebbistatin derivative. Sci. Rep. 6:26141, (2016).|2. Straight, A.F., Cheung, A., Limouze, J., et al. Dissecting temporal and spatial control of cytokinesis with a myosin II inhibitor. Science 299(5613), 1743-1747 (2003).|3. Kovács, M., Tóth, J., Hetényi, C., et al. Mechanism of blebbistatin inhibition of myosin II. J. Biol. Chem. 279(34), 35557-35563 (2004).|4. Limouze, J., Straight, A.F., Mitchison, T., et al. Specificity of blebbistatin, an inhibitor of myosin II. J. Muscle Res. Cell Motil. 25(4-5), 337-341 (2004).|5. Kolega, J. Phototoxicity and photoinactivation of blebbistatin in UV and visible light. Biochem. Biophys. Res. Commun. 320(3), 1020-1025 (2004).|6. Sakamoto, T., Limouze, J., Combs, C.A., et al. Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light. Biochemistry 44(2), 584-588 (2005).|7. Verhasselt, S., Roman, B.I., Bracke, M.E., et al. Improved synthesis and comparative analysis of the tool properties of new and existing D-ring modified (S)-blebbistatin analogs. Eur. J. Med. Chem. 136, 85-103 (2017).

st-Ht31 P is the negative control peptide for st-Ht31; it contains a proline substituted for isoleucine to prevent the formation of an amphiphilic helix and has no effect on neurite outgrowth. st-Ht31 is cell-permeable and can disrupt the interaction between AKAP (A-kinase anchoring protein) and PKA, thereby preventing phosphodiesterase-mediated downregulation of cAMP and PKA signaling and promoting axonal growth.