stabilizing

Compound 3l, a paclitaxel derivative known as Microtubule Stabilizing Agent-1, effectively enhances tubulin polymerization and demonstrates antitumor efficacy [1].

Deucravacitinib (BMS-986165) inhibits IL-12/23 and type I IFN pathways[1][2]. BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases. Which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain.

Valproic acid sodium salt (Sodium Valproate) is the sodium salt form of valproic acid with anti-epileptic activity. Valproic acid sodium salt is converted into its active form, valproate ion, in blood. Although the mechanism of action remains to be elucidated, Valproic acid sodium salt increases concentrations of gamma-aminobutyric acid (GABA) in the brain, probably due to inhibition of the enzymes responsible for the catabolism of GABA. This potentiates the synaptic actions of GABA. Valproic acid sodium salt may also affect potassium channels, thereby creating a direct membrane-stabilizing effect.

Isomalt (Palatinitol) is a mixture of 1,6-mannitol glucopyranoside and 1,6-sorbitol glucopyranoside

K201 (JTV-519) is a Ca2+-dependent blocker and prevents abnormal Ca(2+) leak from the sarcoplasmic reticulum in the ischemic heart and skeletal muscle (SkM) by stabilizing the ryanodine receptors.

360A is a stabilizing G-Quadruplex ligand, and also inhibits telomerase activity for telomerase in TRAP-G4 assay(IC50 : 300 nM).

Davunetide acetate is derived from activity-dependent neuroprotective protein existing in the mammalian CNS. Davunetide acetate is a microtubule-stabilizing peptide and inhibits Aβ aggregation and Aβ-induced neurotoxicity. Davunetide acetate possesses neuroprotective, neurotrophic, and cognitive protective properties.

EC5026 (BPN-19186) has the potential to relieve pain by stabilizing natural analgesic and anti-inflammatory mediators.

Simotaxel is a semi-synthetic, orally bioavailable, third-generation taxane derivative and microtubule-stabilizing agent, with potential antineoplastic activity.

Benperidol (Anquil) is a butanone analog with antipsychotic and stabilizing properties, and has been shown to be effective in blocking D2 receptors.Benperidol can be used in positron emission tomography (PET) scanning to measure D(2) dopamine receptor binding in vivo.Benperidol has been shown to be effective in blocking D2 receptors in vivo.Benperidol has been shown to be effective in blocking D2 receptors in vivo.

AOH1996 is an orally active ligand for the replicasome component PCNA (proliferating cell nuclear antigen), targeting the transcription-replication conflict (TRC).AOH1996 interferes with the interaction of PCNA with its binding proteins, leading to DNA replication stress and apoptosis.AOH1996 causes proteasome-dependent rpb1 degradation and lethal DNA damage by stabilizing the interaction between PCNA and RNA polymerase II.AOH1996 acts synergistically with DNA damaging agents to inhibit tumor cell growth. AOH1996 inhibits tumor cell growth by stabilizing the interaction between PCNA and RNA polymerase II, leading to proteasome-dependent rpb1 degradation and lethal DNA damage.AOH1996 acts synergistically with DNA damaging agents.

Microtubule destabilizing agent-1 (Compound 12b), a hydroxamic acid-based microtubule destabilizing agent (MDA), exhibits potent antitumor activity, favorable metabolic stability, and high bioavailability, making it a promising candidate for further investigation as an MDA [1].

Carteolol hydrochloride (Abbott-43326) is a synthetic quinolinone derivative, antihypertensive Carteolol Hydrochloride is a nonselective beta-adrenoceptor blocking agent for beta-1 and beta-2 receptors with no membrane-stabilizing activity but moderate intrinsic sympathomimetic effects. It is used for the treatment of hypertension and certain arrhythmias and as an anti-angina and antiglaucoma agent.

Necrostatin-34 (2-{[3-cyano-4-(4-methylphenyl)-6-oxo-1,4) is a RIPK1 kinase inhibitor, stabilizing RIPK1 kinase in an inactive conformation by occupying a distinct binding pocket in the kinase domain.

2,3-Diphosphoglyceric acid (2,3-DPG), an intermediate of the glycolytic pathway, allosterically binds to deoxygenated hemoglobin, stabilizing it and facilitating oxygen release at tissue sites. This binding decreases hemoglobin's oxygen affinity, promoting oxygen delivery to tissues [1] [2].

Becatecarin is a water-soluble, diethylaminoethyl analog of the antineoplastic antibiotic rebeccamycin. It intercalates into DNA, stabilizing the DNA-topoisomerase complex. This results in the potent catalytic inhibition of both topoisomerases I and II, initiating DNA cleavage and apoptosis. Becatecarin, alone or in combination with other compounds, has anti-cancer as well as myelosuppressive effects in vivo. It is also a transport substrate of the ATP-binding cassette (ABC) transporter ABCG2.

Ceratamine A is an antimitotic heterocyclic alkaloid isolated from the marine sponge Pseudoceratina sp., acts as a microtubule-stabilizing agent with cytotoxicity against human cancer cell lines.

Poly(I:C):Kanamycin (1:1) is a compound comprising an equal mixture of synthetic double-stranded RNA (dsRNA), specifically Poly(I:C), a Toll-like receptor 3 (TLR3) agonist, and kanamycin, a positively charged (poly-NH3) antibiotic. The positive charge of kanamycin interacts with the negatively charged Poly(I:C), stabilizing the molecule.

Taurohyocholic acid (THCA) is a taurine-conjugated form of the porcine-specific primary bile acid hyocholic acid .1THCA inhibits precipitation of cholesterol crystals by stabilizing cholesterol in the liquid-crystalline phase.2It prevents cholestasis and cellular necrosis induced by taurolithocholic acid in isolated rat livers.3THCA levels are increased in the urine of patients with hepatitis B-induced cirrhosis.4

Vitronectin, a multifunctional glycoprotein found in blood and the extracellular matrix, interacts with glycosaminoglycans, collagen, plasminogen, and the urokinase-receptor, in addition to stabilizing the inhibitory conformation of plasminogen activation inhibitor-1. It is utilized in research related to wound healing and tumor progression [1].

Octyl glucose neopentyl glycol (OGNG) is a detergent derived from neopentyl glycol, intended for stabilizing membrane proteins [1].

Azaphilone-9 (AZA-9) functions as an inhibitor of the HuR-ARE RNA interaction, with an inhibition constant (IC50) of 1.2 μM, by targeting the RNA-binding protein Hu antigen R (HuR). As HuR-RNA interactions play a critical role in stabilizing oncogenic mRNAs within tumors, Azaphilone-9 exhibits potential in inhibiting cancer cell growth and progression.

Flavipin, an aryl hydrocarbon receptor (Ahr) agonist, activates Ahr downstream gene expression in mouse CD4+ T cells and CD11b+ macrophages. This compound disrupts the stabilizing effect of Arid5a on the newly identified target mRNA, Il23a 3′UTR. Additionally, Flavipin demonstrates significant antioxidant properties, evidenced by its DPPH free radical scavenging capability with an IC50 value of 7.2 μM, and exhibits potent α-glucosidase inhibitory activity with an IC50 value of 33.8 μM.

SAHM1 TFA is a chemical compound that acts as a Notch pathway inhibitor by stabilizing a hydrocarbon-stapled alpha helical peptide. It specifically targets the protein-protein interface, effectively preventing the assembly of the Notch complex.

Taccalonolide A is the first microtubule stabilizing agent to be discovered from a plant since identification of the mechanism of action of paclitaxel and it is the first natural product steroid identified to have these cellular effects,with cytotoxic and antimalarial activities. Taccalonolide A causes G2-M accumulation, Bcl-2 phosphorylation and initiation of apoptosis. Taccalonolide A is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug resistance protein 7 (MRP7), with an IC50 of 622 nM for SK-OV-3 cells.

SARS-CoV-2-IN-39 is a SARS-CoV-2 inhibitor with an EC50 of 1 μM. SARS-CoV-2-IN-39 has antiviral activity and inhibits SARS-CoV-2 by inhibiting SKP2 protein and stabilizing BECN1.

Disoxaril (BRN 3626820, WIN 51711) is an anti-picornavirus agent that inhibits enterovirus replication by binding to a hydrophobic bag within the VP1 coat protein, thereby stabilizing virions and preventing their uncoating. When used in combination with A

Bupranolol is a non-selective beta blocker without intrinsic sympathomimetic activity (ISA), but with strong membrane stabilizing activity. Its potency is similar to propranolol. Bupranolol is quickly and completely absorbed from the gut. Over 90% undergo first-pass metabolism. Bupranolol has a plasma half life of about two to four hours, with levels never reaching 1 µg/l in therapeutic doses. The main metabolite is carboxybupranolol, 4-chloro-3-[3-(1,1-dimethylethylamino)-2-hydroxy-propyloxy]benzoic acid – that is, the methyl group at the benzene ring is oxidized to a carboxyl group –, of which 88% are eliminated renally within 24 hours.

13C-d3-AOH1996 is the 13C and deuterated compound of AOH1996. 13C-AOH1996 has a CAS number of 2089314-64-5. AOH1996 is an orally active ligand for the replicasome component PCNA (proliferating cell nuclear antigen), targeting the transcription-replication conflict (TRC).AOH1996 interferes with the interaction of PCNA with its binding proteins, leading to DNA replication stress and apoptosis.AOH1996 causes proteasome-dependent rpb1 degradation and lethal DNA damage by stabilizing the interaction between PCNA and RNA polymerase II.AOH1996 acts synergistically with DNA damaging agents to inhibit tumor cell growth. AOH1996 inhibits tumor cell growth by stabilizing the interaction between PCNA and RNA polymerase II, leading to proteasome-dependent rpb1 degradation and lethal DNA damage.AOH1996 acts synergistically with DNA damaging agents.

Irinotecan-d10 Hydrochloride is a deuterated compound of Irinotecan Hydrochloride. Irinotecan Hydrochloride has a CAS number of 100286-90-6. Irinotecan Hydrochloride is the hydrochloride salt of a semisynthetic derivative of camptothecin. Irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. One thousand-fold more potent than its parent compound irinotecan, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Because ongoing DNA synthesis is necessary for irinotecan to exert its cytotoxic effects, it is classified as an S-phase-specific agent.

Triclosan methyl-d3 (methoxy-d3) is a deuterated compound of Triclosan methyl. Triclosan methyl has a CAS number of 4640-01-1. Triclosan-methyl is a transformation product of triclosan. Triclosan is a bactericide in personal care products such as toothpaste, shampoos, and soaps. Triclosan is also a stabilizing agent in a multitude of detergents and cosmetics.

1. Apiin (Apioside) is the reducing and stabilizing agent. 2. Apiin has inhibitory activity in-vitro on iNOS expression and nitrite production when added before LPS stimulation in the medium of J774.A1 cells.

Larotaxel (XRP9881) is a taxane analogue that has anticancer activity, exerts its cytotoxic effects by promoting tubulin assembly and stabilizing microtubules, and ultimately induces cell death through apoptosis. Larotaxel (XRP9881) is a compound that crosses the blood-brain barrier and has a higher affinity for Docetaxel than P-glycoprotein 1, which can be used to study breast and bladder cancer.

Aβ-IN-7 (compound 5a) acts as a potent inhibitor of Aβ aggregation, stabilizing Aβ monomers at 50 μM concentration to prevent them from forming larger oligomers and delaying the nucleation phase. Comparative studies demonstrate that Aβ-IN-7 more effectively inhibits Aβ fibril formation than Aβ-IN-8 at identical 50 μM concentrations [1].

G-9807 acts as an allosteric RNase activator by stabilizing the active dimeric unit， significantly increasing the RNase activity of IRE1-KR-0P.

Castor oil (Xenaderm) is a vegetable oil pressed from the seeds of the castor bean, Ricinus communis, used as a laxative and as an excipient in medicinally.

Inhibits neural Wiskott-Aldrich syndrome protein (N-WASP) by stabilizing the autoinhibited state of the protein. Blocks phosphatidylinositol 4,5-bisphosphate (PIP2)-stimulated actin assembly (IC50 ~ 2 μM) but does not directly inhibit actin polymerization

Guar gum is a galactomannan polysaccharide extracted from guar beans, it has stabilizing and thickening properties useful in food, feed, and industrial applications.

BTTAA, a Cu(I)-stabilizing ligand, performs potently with ubiquitin Glu18AzF.

Phenytoin (5,5-Diphenylhydantoin) is a hydantoin derivative and a non-sedative antiepileptic agent with anticonvulsant activity. Phenytoin potentially acts by promoting sodium efflux from neurons located in the motor cortex reducing post-tetanic potentiation at synapses. The reduction of potentiation prevents cortical seizure foci spreading to adjacent areas, stabilizing the threshold against hyperexcitability. In addition, this agent appears to reduce sensitivity of muscle spindles to stretch causing muscle relaxation.

P516-0475 is a novel chemical inducer of Streptococcus quorum sensing acts by inhibiting the pheromone-degrading endopeptidase PepO. This compound induces quorum sensing by stabilizing SHP pheromones in culture.

Epothilone A (Epo A) is a microtubule-stabilizing agent with EC0.01 of 2 μM.

Mesdopetam hemitartrate (IRL790 hemitartrate) is an antagonist of dopamine D3 receptor (Ki=90 nM; IC50=9.8 μM for human recombinant D3 receptor). It has psychomotor stabilizing properties.

Pindolol-d7 is a deuterated compound of Pindolol. Pindolol has a CAS number of 13523-86-9. Pindolol is a moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity.

Shield-2 is a potent FKBP-derived destabilizing domain stabilizing ligand.

DL-071-IT (Afurolol Hydrochloride) is a potent non-selective beta-adrenoceptor antagonist. DL-071-IT showed intrinsic sympathomimetic activity and weak membrane stabilizing activity.

6-PPD, a substituted p-phenylenediamine, functions as an ozone scavenger by forming nitroxyl radicals. It impacts zebrafish embryos by decreasing hatchability by 25.6% and 78.9% at concentrations of 0.022 mg/L and 0.22 mg/L, respectively. Additionally, 6-PPD reduces embryo motility and body length, and induces developmental malformations and oxidative stress. Its use in rubber formulations as stabilizing additives and antiozonants has been established.

Dictyostatin ((-)-Dictyostatin; Dictyostatin 1) is a potent microtubule-stabilizing and anti-cancer agent that exhibits antiproliferative activity and has potential for tauopathy research.

GUN35758, also known as 4'-Carboxybenzo-18C6, is a novel transthyretin (ttr) amyloidogenesis inhibitor, stabilizing the ttr tetramer by binding to the allosteric sites on the molecular surface of the ttr tetramer. This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming).

Zoledronate disodium is an inhibitor of osteoclastogenesis and macrophage recruitment, decreasing bone turnover and stabilizing the bone matrix, exhibiting diverse anti-tumor effects in osteosarcoma.