kinetic

LC kinetic stabilizer-1 is a potent, selective kinetic stabilizer for amyloidogenic immunoglobulin light chains, demonstrating EC50 values of 140 nM for WIL-FL* and 74.1 nM for WIL-FL*T46L F49Y, respectively. Notably, WIL-FL represents an amyloidogenic FL LC dimer.

LC Kinetic Stabilizer-2 is a powerful stabilizer for amyloidogenic immunoglobulin light chains (LC), demonstrating significant efficacy with an EC50 of 24 nM.

Adipokinetic hormone II (Locusta migratoria) (Lom-AKH-II), an insect adipokinetic hormone (AKH), elevates fat body cAMP levels in vitro. These hormones (AKHs) regulate the mobilization of carbohydrates and lipids from fat body reserves for flight by activating AKH receptor(s) that stimulate cAMP production and glycogen phosphorylase through the stimulatory guanine nucleotide-binding protein (Gs) [1] [3].

Adipokinetic hormone I (Locusta migratoria) (Lom-AKH-I), an insect adipokinetic hormone (AKH), increases fat body cAMP levels in vitro and regulates the mobilization of carbohydrates and lipids from fat body stores for flight, through AKH receptor(s)' association with cAMP production and glycogen phosphorylase activation via the stimulatory guanine nucleotide-binding protein (Gs) [1] [3].

Prokineticin 2 Isoform 2 (human), a hypothalamic neuropeptide, regulates thermoregulation and energy metabolism while decreasing food intake in rodents. This isoform is implicated in the study of metabolic syndrome (MetS), obesity, and hyperglycemia [1].

Adipokinetic Hormone (Apis mellifera ligustica, Bombyx mori, Heliothis zea, Manduca sexta), a peptide shared by diverse insects, elicits a potent adipokinetic hypertrehalosemic response but lacks the function to mobilize glycogen and maintains an inadequate glycogen reserve in the fat body for effective utilization [1].

Adipokinetic hormone Gryllus bimaculatus (Grybi-AKH), an adipokinetic hormone, mobilizes lipids and carbohydrates from the insect fat body, regulating energy homeostasis. It also enhances the locomotor activity of the two-spotted cricket and has potential applications in human medical studies for body weight regulation, weight loss induction, and alleviation of glycogen storage disorders [1] [2] [3].

Adipokinetic Hormone (AKH) (24-32), locust (TFA), is a neurohormone extracted from the corpora cardiaca of locusts that regulates lipid utilization during flight [1].

Adipokinetic Hormone (AKH) (24-32), locust, is a peptide hormone isolated from locusts.

Sulfamonomethoxine is a long-acting sulfonamide antibacterial agent, blocks the synthesis of folic acid by inhibiting synthetase of dihydropteroate.

5-bromo-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione (5-bromo-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione) is a synthetic compound. It has been used as a catalyst and as a tool in enzyme kinetic studies; it has also been used in studies of enzyme inhibition, as well as in drug receptor interaction studies.

Eribulin (B1939) is a nonpaclitaxel microtubule kinetic inhibitor with anticancer activity that inhibits polymerization of microtubule protein subunits by preventing lengthening and shortening of microtubules during cell division.Eribulin is used in the study of metastatic breast cancer and solid tumors.

Sulfamonomethoxine D4 is a deuterium labeled Sulfamonomethoxine. Sulfamonomethoxine is an agent of long acting sulfonamide antibacterial, used in blood kinetic studies,and blocks the synthesis of folic acid by inhibiting synthetase of dihydropteroate.

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).

TMC647055 Choline Hydroxide Salt is a novel and potent non-nucleoside inhibitor of the HCV NS5B polymerase which potentially for the treatment of HCV infection. It has nanomolar cellular potency (EC(50) of 82 nM) with minimal associated cell toxicity (CC(

Diisopropyl tartrate is a reagent for kinetic resolution of racemic allylic alcohols and α-furfuryl amides. It acts by enantioselective epoxidation.

CBS-3595 is a potent and dual Inhibitor of p38α MAPK/PDE-4 with a superior profile regarding its anti-inflammatory effects. CBS-3595 features moderate inhibition of p38α MAPK and PDE-4 in the higher nanomolar range in combination with excellent kinetic pr

Adenosine 3',5'-diphosphate sodium salt is an inhibitor of hydroxysteroid sulfotransferases, which are adenine nucleotides containing a phosphate group at the 3' and 5' positions of the pentose ribose.Adenosine 3',5'-diphosphate (sodium salt) is the product of 3'-phosphoadenosine 5'-phosphosulfonate (PAPS), a cofactor of sulfotransferases (SULTs). diphosphate disodium is the product of 3'-phosphoadenosine 5'-phosphosulfonate (PAPS), a cofactor for sulfotransferases (SULTs), which has been used to study the kinetic properties and structure of SULTs.

(E)-Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities.1,2,3,4It is active against Gram-positive and Gram-negative bacteria (MICs = 10-250 and 150->500 μg/ml, respectively) and fungi (MICs = 15-50 μg/ml).1(E)-Ajoene inhibits proliferation of a variety of cancer cells, including MDA-MB-231 breast, HeLa cervical, and WHCO1 esophageal cancer cells (IC50s = 18.6, 61, and 39.2 μM, respectively).2It also inhibits human glutathione reductase andT. cruzitrypanothione reductase when used at a concentration of 200 μM.3(E)-Ajoene (25 mg/kg) is neuroprotective in a gerbil model of ischemia-reperfusion injury, reducing reactive astrocytosis and microgliosis in the hippocampal CA1 region.4 1.Yoshida, H., Iwata, N., Katsuzaki, H., et al.Antimicrobial activity of a compound isolated from an oil-macerated garlic extractBiosci. Biotechnol. Biochem.62(5)1014-1017(1998) 2.Kaschula, C.H., Hunter, R., Hassan, H.T., et al.Anti-proliferation activity of synthetic ajoene analogues on cancer cell-linesAnticancer Agents Med. Chem.11(3)260-266(2011) 3.Gallwitz, H., Bonse, S., Martinez-Cruz, A., et al.Ajoene is an inhibitor and subversive substrate of human glutathione reductase and Trypanosoma cruzi trypanothione reductase: Crystallographic, kinetic, and spectroscopic studiesJ. Med. Chem.42(3)364-372(1999) 4.Yoo, D.Y., Kim, W., Nam, S.M., et al.Neuroprotective effects of Z-ajoene, an organosulfur compound derived from oil-macerated garlic, in the gerbil hippocampal CA1 region after transient forebrain ischemiaFood Chem. Toxicol.721-7(2014)

Ensartinib (X-396) is a potent and orally active dual ALK MET inhibitor for the treatment of ALK-positive non-small cell lung cancer (NSCLC).

Coumarin-quinone conjugate is a fluorescent substrate for NADH:ubiquinone oxidoreductases.1It is comprised of a coumarin fluorophore conjugated to a ubiquinone analog that can be reduced by NADH:ubiquinone oxidoreductases. It has been used to measure the kinetic parameters of apoptosis-inducing factor mitochondria-associated 2/ferroptosis suppressor protein 1 (AIFM2/FSP1). 1.Doll, S., Freitas, F.P., Shah, R., et al.FSP1 is a glutathione-independent ferroptosis suppressorNature575(7784)693-698(2019)

Acoramidis hydrochloride (Alxn2060 hydrochloride) is an orally active and selective kinetic stabilizer of WT and V122I- TTR (transthyretin) . Acoramidis hydrochloride is used in the study for transthyretin amyloidosis.

Tafamidis (Fx-1006A) is a kinetic stabilizer of transthyretin (TTR) that prevents amyloidogenesis by wild-type and mutant TTRs. It binds to TTR with negative cooperativity (Kd1: 3 nM; Kd2: 278 nM) to stabilize the TTR dimer-dimer interface and inhibit tetrameric dissociation. Tafamidis stabilizes wild-type and clinically significant V30M and V122I mutant TTR amyloidogenic homotetramers (EC50s: 2.7-3.2 μM) under fibril-promoting, denaturing, and physiological conditions in vitro. It stabilizes TTR heterotetramers containing wild-type and mutant subunits ex vivo in human plasma derived from patients carrying V30M or V1221 mutations when used at a concentration of 7.2 μM. Formulations containing tafamidis have been used for the treatment of familial amyloid polyneuropathy.

1. Corylifol A (Corylinin) displays cytotoxic activity against HepG2 and Hep3B hepatocellular carcinoma cell lines, with IC50 values of 4.6 and 13.5 ug ml, respectively. 2. Corylifol A and Biochanin A can be the potential uncouplers of neuronal nitric oxide synthase-postsynaptic density protein-95. 3. Corylifol A and bavachin are strong inhibitors of UDP-glucuronosyltransferase 1A1 (UGT1A1) with the inhibition kinetic parameters (Ki) values lower than 1 uM.4. Corylifol A and bakuchiol are naturally occurring potent inhibitors of hCE2, with low Ki values ranging from 0.62uM to 3.89 uM. 5. Corylifol A shows an inhibitory effect on IL-6-induced STAT3 promoter activity in Hep3B cells with IC50 values of 0.81 ± 0.15 uμ, it also inhibits STAT3 phosphorylation induced by IL-6 in Hep3B cells, suggests that corylifol A has antiinflammatory activity.