Talotrexin (PT523), an analog of Aminopterin (HY-14518), is a nonpolyglutamatable classic antifolate. Talotrexin is a RFC (reduced folate carrier) specific inhibitor and selectively inhibits RFC transport. Talotrexin shows antitumor activity by targeting DHFR to inhibit tumor growth[1][2].
Bis-PEG4-PFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
D-AP4 (D-APB; D-2-Amino-4-phosphonobutyric acid), a phosphono analogue of glutamate, is an NMDA broad spectrum excitatory amino acid receptor antagonist. D-AP4 also is an agonist for a quisqualate-sensitized AP6 site in hippocampus. D-AP4 inhibits AMPA receptor-stimulated 57Co2+ influx in cultured cerebellar granule cells (IC50 ≥ 100 μM)[1][2][3].
[His7] Corazonin, a neurohormone, induces dark color in the cuticle and epidermis of Locusta migratoria[1].
Enhanced Green Fluorescent Protein (EGFP) (200-208) is a marker gene product derived from the jellyfish Aequorea Victoria. Enhanced Green Fluorescent Protein (EGFP) (200-208) is a common reporter protein and is easy to detect[1].
Betonicine (Achilleine), an alkaloid, has cell protectant activity. Betonicine protects Bacillus subtilis against extremes in osmolarity and growth temperatures[1].
Boc-D-Cyclopropylglycine is a small molecule peptide, it can be used for compounds synthesis[1].
AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM.
BMVC2 (o-BMVC) is a bisubstitute carbazole derivative of BMVC. BMVC2 is a G-quadruplex (G4) stabilizer[1].
2,3,4'-Trihydroxy-3',5'-dimethoxypropiophenone, isolated from Parinari hypochrysea (Chrysobalanaceae), exhibits antioxidant and lipoxygenase inhibition[1].
EMD638683 R-Form is the R-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.
(-)-Isobicyclogermacrenal is a natural sesquiterpene hydrocarbon[1].
AMP-PNP (Adenylyl imidodiphosphate) is a non-hydrolysable ATP analogue[1].
Carpinontriol B is a natural diarylheptanoid compound[1].
PI3KC2α-IN-1 is a potent PI3KC2α inhibitor (IC50: 95 nM). PI3KC2α-IN-1 interacts with the ATP-binding site of PI3KC2α. PI3KC2α-IN-1 can be used in the research of thrombosis, diabetes and cancers[1].
AT-121 hydrochloride is a bifunctional nociception and mu opioid receptor agonist, with Kis of 3.67 and 16.49 nM, respectively. AT-121 hydrochloride is a safe, non-addictive analgesic, and shows antinociceptive and antiallodynic effects[1].
6-Chloro-N1-(trimethylsilylethoxymethyl)pseudouridine is a uridine analog. Uridine has potential antiepileptic effects, and its analogs can be used to study anticonvulsant and anxiolytic activities, as well as to develop new antihypertensive agents[1].
Revusiran (ALN-TTRSC) is a 1st-generation short interfering RNA, which directed against transthyretin (TTR) mRNA. Revusiran can be used for transthyretin (TTR)-mediated amyloidosis research[1].
Icenticaftor (QBW251) is an orally active CFTR channel potentiator, with EC50s of 79 nM and 497 nM for F508del and G551D CFTR, respectively. Icenticaftor can be used for chronic obstructive pulmonary disease (COPD) and cystic fibrosis research[1].
Euphoscopin C is a diterpenoid found in Euphorbia helioscopia. Euphoscopin C can significantly enhance the killing activity of NK cells against H1299 -luci cells and A549-luci cells[1].
Pocenbrodib (compound II) is a CBP/p300 family of bromodomain inhibitor. Pocenbrodib has the potential for cancer research[1].
Ceftolozane (CXA-101) sulfate is an antipseudomonal cephalosporin. Ceftolozane sulfate inhibits P. aeruginosa PAO1 with an MIC of 0.5 μg/mL. Ceftolozane sulfate can also inhibit β-lactam-resistant P. aeruginosa[1][2].
Catharanthine inhibits nicotinic receptor mediated diaphragm contractions with IC50 of 59.6 μM.Target: nAChRCatharanthine evokes a concentration-dependent attenuation of carbachol responses in the rat ileum preparation, producing rightward curve displacements and decreases in maximal agonist responses. The mixture of serpentine, plus ajmalicine and catharanthine reveals a concentration-dependent inhibitory effect of acethylcholinesterase (AchE), with an IC50 at ca. 2.25 μg/Ml [1]. Catharanthine can induce the self-association of tubulin into linear indefinite polymers with an efficacy that is 75% that of vinblastine or vincristine. Catharanthine binds to tubulin alpha-beta dimer with binding constant of 2.8 mM [2]. Catharanthine stimulates release of amylase from pancreatic fragments and to cause extensive degranulation of pancreatic acinar cells with accumulation of membrane material in the Golgi region. Catharanthine induces a delayed release of Ca2+ from prelabeled pancreatic fragments as compared to bethanechol [3]. Catharanthine inhibits epibatidine-induced Ca(2+) influx in TE671-α, -β, -γ, -δ cells in a noncompetitive manner with similar potencies IC50 of 17 mM-25 mM. Catharanthine inhibits [3H]TCP binding to the desensitized Torpedo AChR with higher affinity compared to the resting AChR. Catharanthine enhances [3H]cytisine binding to resting but activatable Torpedo AChRs, suggesting desensitizing properties [4].
YG1702 is a potent ALDH18A1-specific inhibitor. YG1702 attenuates the growth of MYCN-amplified NB and down-regulates MYCN. YG1702 physically interacts with ALDH18A1 with a high affinity and might potentially affect its enzymatic activity[1].
Oxypaeoniflorin is a natural product derived from Radix Paeoniae Rubra and Radix Paeoniae Alba.
Metamizole sodium is a non-opioid compound with excellent analgesic and antipyretic effects. Metamizole (sodium) is a cyclooxygenase-3 (COX-3) inhibitor[1][2].
Otamixaban(FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa.IC50 value:Target: Factor Xa Otamixaban is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa. In vivo experiments have demonstrated that Otamixaban is highly efficacious in rodent, canine and porcine models of thrombosis. In addition, recent clinical findings indicate that Otamixaban is efficacious, safe and well tolerated in humans and therefore has considerable potential for the treatment of acute coronary syndrome. This review article chronicles the discovery and pre-clinical data surrounding the fXa inhibitor Otamixaban as well as the recent clinical findings in humans.
Venlafaxine-d6-1 is deuterium labeled Venlafaxine. Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1].
MR2938 is a potent AChE inhibitor, with an IC50 of 5.04 μM. MR2938 also suppresses NO production obviously (IC50 = 3.29 μM). MR2938 suppresses the neuroinflammation through blocking MAPK/JNK and NF-κB signaling pathways. MR2938 can be used for Alzheimer’s disease (AD) research[1].
MAT2A-IN-1 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally high in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-1 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-1 has the potential for the research of cancer diseases (extracted from patent WO2021139775A1, compound 64)[1].