MSX-122 is a partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC50 of ∼10 nM; MSX-122 has anti-inflammatory and anti-metastatic activity.
Ep300/CREBBP-IN-2 (Example 73) is a potent and orally active Ep300 and CREBBP inhibitor with IC50s of 0.052 and 0.148 μM, respectively. Ep300/CREBBP-IN-2 can be used for the research of cancer[1].
Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders[1].
Aripiprazole lauroxil, an N-acyloxymethyl prodrug of aripiprazole, is a Long-acting injectable (LAI) typical antipsychotic for schizophrenia. Aripiprazole lauroxil is cleaved by body’s enzyme esterase to N-hydroxymethyl aripiprazole (plus lauric acid) and then to aripiprazole (plus formaldehyde), no toxicity[1].
Methyl β-D-glucopyranoside is used to synthesize natural glycophenolics via enzymatic caffeoylation[1].
Linaclotide is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation.
Gomisin L1 is a lignan, shows inhibitory effect on cell viability of A2780 and Ishikawa cells, with IC50s of 39.06 μM and 74.16 μM, respectively[1].
Ciprofloxacin hydrochloride is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
Calpain-2-IN-1 is a calpain-2 selective inhibitor that enhances learning & memory by prolonging ERK activation.
A potent inhibitor of developmental angiogenesis in the zebrafish eye, and a cysteinyl leukotriene 1 and 2 receptor (CysLT1 and 2) antaognist with IC50 of 1.2 and 52 uM, respectively; demonstrates significant anti-angiogenic activity in human endothelial cell, murine aortic ring, and murine oxygen-induced retinopathy models of angiogenesis; does not directly target VEGFRs, and inhibits angiogenesis in a range of cell and tissue systems.
Bis-propargyl-PEG6 is a PEG-based PROTAC linker used in the synthesis of PROTACs. Bis-propargyl-PEG6 can be used to synthesize the polymer linked multimers of guanosine-3', 5'-cyclic monophosphates[1].
Ambucetamide is an antispasmodic agent. Ambucetamide alleviates menstrual pain[1][2].
GLP-1 receptor agonist-1 is a glucagon-like peptide-1 receptor (GLP-1R) agonist.
DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ) inhibitor with an IC50 of 1.43 μM. DJ001 displays no inhibitory activity against other phosphatases, with only modest inhibitory activity against Protein Phosphatase 5. DJ001 promotes promote hematopoietic stem cell regeneration[1].
Defibrotide sodium is a complex mixture of single stranded polydeoxyribonucleotides. Defibrotide sodium has liver protection, anti-inflammatory, antithrombotic, profibrinolytic, and anti-ischemic properties. Defibrotide sodium can be used for sinusoidal obstruction syndrome (SOS)/veno-occlusive disease (VOD) research[1].
Remibrutinib, is a potent and orally active bruton tyrosine kinase (BTK) inhibitor with an IC50 value of 1 nM. Remibrutinib inhibits BTK activity with an IC50 value of 0.023 μM in blood[1]. Remibrutinib has the potential for Chronic urticaria (CU) treatment[2].
PU02, a derivative of 6-MP (HY-13677), is a negative allosteric modulator (NAM) of 5-HT3 receptor, with IC50 values of 0.36 and 0.73 μM in HEK293 cells transfected with human 5-HT3A and 5-HT3AB receptors respectively[1][2].
JPS014 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 degrades class I histone deacetylase (HDAC). JPS014 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells[1].
Dinactin, an antibiotic ionophore produced by Streptomyces species, as an effective small molecule targeting Wnt/β-catenin signaling pathway in cancer cells. Dinactin shows marked inhibition of HCT-116 cell growth with an IC50 of 1.1 µM. Dinactin shows anti-proliferative activity against the cancer cells in apoptosis-independent manner. Dinactin is also an effective agent for the research of neuropathic pain[1].
BCL6 PROTAC 1 is a selective B-cell lymphoma 6 (BCL6) PROTAC. BCL6 PROTAC 1 inhibits BCL6 cell reporter with an IC50 value of 8.8 µM. BCL6 PROTAC 1 significantly degrades BCL6 in diffuse large B-cell lymphoma (DLBCL) cell lines. BCL6 PROTAC 1 can be used in tumor related research[1].
Amebucort is a synthetic glucocorticoid corticosteroid, may used for the research of inflammatory disorders.
Galactinol dihydrate is a marker for seed longevity. Galactinol dihydrate can scavenge hydroxyl radicals and protect plant cells from oxidative damage caused by MV treatment, salinity, or chilling[1].
DS-7423 is a novel potent, small-molecule dual inhibitor of PI3K/mTOR with IC50 of 15.6, 1143, 249, 262 and 34.9 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, and mTOR respectively; exerts anti-tumor effect against a panel of nine OCCA cell lines with IC50 of <75 nM, regardless of the mutational status of PIK3CA; suppresses the tumor growth of OCCA in a dose-dependent manner in mouse xenograft models. Solid Tumors Phase 1 Discontinued
QCC374 is a selective agonist of IP[1].
Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].
6-Chloro-7-hydroxy-4-methylcoumarin (compound 3) an intermediate of pharmaceutical synthesis[1].
Fmoc-Glu-OAll is a glutamic acid derivative[1].
LDN-212320(OSU-0212320) is a glutamate transporter EAAT2 activator; enhances EAAT2 levels by > 6 fold at concentrations < 5 μM after 24 h.IC50 value: 1.83 uM(EC50) [2]Target: EAAT2 activatorin vitro: LDN/OSU-0212320 increased EAAT2 protein levels in a dose-dependent(EC50=1.83 ± 0.27 μM) and time-dependent manner. LDN/OSU-0212320 increased EAAT2 protein levels and glutamate uptake function, but did not affect EAAT1 or EAAT3 protein levels. LDN/OSU-0212320 treatment markedly prevented neuronal loss and degeneration, as assessed by MAP2 immunostaining [2]. in vivo: After a single i.p. 40-mg/kg dose of LDN/OSU-0212320, EAAT2 protein levels and associated glutamate uptake increased by approximately 1.5- to 2-fold at 2 hours and by approximately 2- to 3-fold between 8 and 24 hours after injection. Even 72 hours after injection, an approximately 1.5-fold increase in EAAT2 protein levels could still be detected (data not shown). In addition, we found that LDN/OSU-0212320–induced EAAT2 protein levels and glutamate uptake were dose dependent [2].Small-molecule activator of glutamate transporter EAAT2 translation provides neuroprotectionBy Kong, Qiongman; Chang, Ling-Chu; Takahashi, Kou; Liu, Qibing; Schulte, Delanie A.; Lai, Liching; Ibabao, Brian; Lin, Yuchen; Stouffer, Nathan; Das Mukhopadhyay, Chitra; et alFrom Journal of Clinical Investigation (2014), 124(3), 1255-1267. Structure-activity relationship study of pyridazine derivatives as glutamate transporter EAAT2 activatorsBy Xing, Xuechao; Chang, Ling-Chu; Kong, Qiongman; Colton, Craig K.; Lai, Liching; Glicksman, Marcie A.; Lin, Chien-Liang Glenn; Cuny, Gregory D. From Bioorganic & Medicinal Chemistry Letters (2011), 21(19), 5774-5777.
Dexamethasone phosphate (Dexamethasone 21-phosphate) is a biologically inactive compound which undergoes dephosphorylation by intra-erythrocyte enzymes. The active metabolite, dexamethasone, is then released into the circulation by simple passive diffusion through cell membranes. Dexamethasone phosphate-encapsulated erythrocyte has the potential for steroid-dependent ulcerative colitis research[1].
Orobanchyl acetate, a natural strigolactone, is a germination stimulant for root parasitic plants[1].