Glimepiride sulfonamide is a intermediate, and can be used to synthesize Glimepiride (HY-B0104) (antidiabetic agent)[1].
JH-131e-153, a diacylglycerol (DAG)-lactone, is a small molecule activator of Munc13-1, targeting the C1 domain. The activation sequence of JH-131e-153 on Munc13-1 is WT>I590≈R592A≈W588A. The C1 domain of Munc13-1 and protein kinase C (PKC) are homologous in sequence and structure. The activation sequence of JH-131e-153 on Munc13-1 and PKC was PKCα>Munc13-1>PKCε. JH-131e-153 regulates neuronal processes through Munc13-1 and can be further used in the study of neurodegenerative diseases[1].
Dehydrotrametenolic acid is a sterol isolated from the sclerotium of Poria cocos. Dehydrotrametenolic acid induces apoptosis through caspase-3 pathway. Dehydrotrametenolic acid has anti-tumor activity, anti-inflammatory, anti-diabetic effects[1].
UIAA-II-232 (compound 19b) is a potent DNA gyrase catalytic inhibitor with an IC50 value of 3.5 µM[1].
PK44 phosphate is a potent dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 value of 15.8 nM[1].
Periplocin is a cardiotonic steroid isolated from Periploca forrestii. Periplocin promotes tumor cell apoptosis and inhibits tumor growth. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase[1][2].
Camaric acid can be isolated from the root of Lantana montevidensis and has antibacterial activity[1].
CC-90003 is an irreversible and selective inhibitor of ERK 1/2 with antitumor activity.
N-Boc-piperazine is a Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183)[1].
Hematin, an iron-containing porphyrin, inhibits the activity of clotting factors and also fibrin clot lysis through the mechanism of binding to and inactivation of hemostatic proteins[1]. Hematin can be used for the research of acute porphyrias and cancer[1][2][3][4][5].
UNC-926 is a methyl-lysine (Kme) reader domain inhibitor; inhibits L3MBTL1 with an IC50 of 3.9 μM.
Topoisomerase II inhibitor 16 (compound CT3) is a selective, orally active, brain-penetrant and irreversible trypanosomal topoisomerase II inhibitor by stabilizing double-stranded DNA:enzyme cleavage complexes. Topoisomerase II inhibitor 16 has the potential for Chagas disease research[1].
Acifluorfen, a protoporphyrinogen oxidase (PROTOX) inhibitor herbicide, promotes the accumulation of protoporphyrin IX (PPIX), and induces tumors in the rodent liver. Acifluorfen causes strong photooxidative destruction of pigments and lipids in sensitive plant species[1][2].
Cefamandole nafate is a second-generation broad-spectrum cephalosporin antibiotic.
INT-747 is a potent and selective farnesoid X receptor (FXR) agonist with an EC50 of 99 nM.
Cisatracurium Besylate is a nondepolarizing neuromuscular blocking agent, antagonizing the action of acetylcholine by inhibiting neuromuscular transmission.Target: AChR alpha-2Cisatracurium is a neuromuscular-blocking drug or skeletal muscle relaxant in the category of non-depolarizing neuromuscular-blocking drugs, used adjunctively in anesthesia to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. It is a bisbenzyltetrahydroisoquinolinium agent with an intermediate duration of action. Cisatracurium is one of the ten isomers of the parent molecule, atracurium. Moreover, cisatracurium represents approximately 15% of the atracurium mixture [1, 2].
(rac)-Antineoplaston A10 is the racemate of Antineoplaston A10. Antineoplaston A10 is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer[1].
Tramiprosate is a small, orally-administered compound that binds to soluble Aβ and reduces amyloid aggregation and subsequent depositiontarget: AβIn vitro: Tramiprosate provides neuroprotection against Aβ-induced neurotoxicity in neuronal and mouse organotypic hippocampal cultures, and reverses Aβ-induced long-term potentiation (LTP) inhibition in rat hippocampus, in part, through activation of β-aminobutyric acid A (GABA-A) receptors. Tramiprosate dose-dependently provides neuroprotection against ischemic stroke.In vivo: Tramiprosate produced dose-dependent reductions of Aβ in the brain of transgenic mice (hAPP-TgCRND8). Clinical studies show that tramiprosate was safe and tolerable. In mild-to-moderate AD patients tramiprosate also reduced Aβ42 levels in CSF.The reference for animal administration is 50 mg/kg.
CPT2 (Carnitine palmitoyltransferase 2), an enzyme that participates in fatty acid oxidation, also is a colorectal cancer (CRC) prognostic biomarker. CPT2 overexpression can activate p-p53 to increase p53 expression, thereby inhibiting tumor proliferation and promoting apoptosis. CPT2 deficiency results in the most common inherited disorder of long-chain fatty acid oxidation affecting skeletal muscle. Downregulation of CPT2 is also highly correlated with the progression of various cancers and has potential for cancer research[1][2].
Hederacoside D is one of the bioactive saponins from Hedera helix, and plays pivotal roles in the overall biological activity.
Boc-2-methoxy-L-phenylalanine is a phenylalanine derivative[1].
Sulfadimethoxine sodium (Sulphadimethoxine sodium) is a sulfonamide antibiotic used to treat many infections[1][2].
Ganoderic acid AM1 (GAAM1) is a natural product that can be found in ganoderma lucidum. Ganoderic acid AM1 shows cytotoxicity with an IC50 value of 19.8 µM for HeLa cells[1].
MAO-B-IN-1 is an inhibitor of monoamine oxidase B, used for the research of neurological diseases.
Isoeugenol acetate, an essential oil constituent of nutmeg, clove, and cinnamon, shows excellent inhibitory effects against some metabolic enzymes such as acetylcholinesterase (AChE) enzymes (IC50=77 nM; Ki=16 nM), α-glycosidase (IC50=19.25 nM; Ki=21 nM), and α-amylase (IC50=411.5 nM). Isoeugenol acetate is used medical and cosmetics industries for its antioxidant, anticancer, antimicrobial and anti-inflammatory properties[1][2].
SN05 is a potent amino acid transport (AAT) inhibitor with Kis of 2.77 μM, 0.73 μM, 0.87 μM, 3.7 μM, 7.25 μM, 7.23 μM and 2.22 μM for human ASCT1, rat ASCT2, human ASCT2, EAAT1, EAAT2, EAAC1 and EAAT5, respectively. SN05 can be used for researching anticancer[1].
Diatrizoic acid is an iodinated radiocontrast agent.
M617 is a selective galanin receptor 1 (GAL1) agonist, with Kis of 0.23 and 5.71 nM for GAL1 and GAL2, respectively. M617, acting through its central GAL1, can promote GLUT4 expression and enhance GLUT4 content in the cardiac muscle of type 2 diabetic rats[1][2].
5,7-Dihydroxycoumarin 7-O-β-D-glucopyranoside is a natural product that can be isolated from the roots of Morus nigra[1].