Olaptesed pegol (NOX-A12) L-oligoribonucleotide aptamer targeting CXCL12 based on a pegylated structure. Olaptesed pegol neutralizes CXCL12, and CXCL12 inhibition mobilizes chronic lymphocytic leukemia cells into the circulation and prevents their homing into the protective microenvironment[1].
Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
OAB-14, is a Bexarotene (HY-14171) derivative, improves Alzheimer's disease-related pathologies and cognitive impairments by increasing β-amyloid clearance in APP/PS1 mice. OAB-14 effectively ameliorates the dysfunction of the endosomal-autophagic-lysosomal pathway in APP/PS1 transgenic mice[1][2].
Desmopressin(DDAVP) acetate is the synthetic analogue of the antidiuretic hormone arginine vasopressin. IC50 Value:Target: Vasopressin ReceptorThe antidiuretic properties of desmopressin have led to its use in polyuric conditions including primary nocturnal enuresis, nocturia, and diabetes insipidus. Desmopressin works by limiting the amount of water that is eliminated in the urine. Desmopressin binds to V2 receptors in renal collecting ducts, increasing water reabsorption. It also stimulates release of von Willebrand factor from endothelial cells by acting on the V2 receptor.
Tiaprost is a prostaglandin F2α (PGF2α) analogue.
Gomisin J is a small molecular weight lignan found in Schisandra chinensis and has been demonstrated to have vasodilatory activity[1]. Gomisin J suppresses lipid accumulation by regulating the expression of lipogenic and lipolytic enzymes and inflammatory molecules through activation of AMPK, LKB1 and Ca2+/calmodulin-dependent protein kinase II and inhibition of fetuin-A in HepG2 cells. gomisin J has potential benefits in treating nonalcoholic fatty liver disease[2].
Fast Black K Salt, a diazonium reagent, is a versatile thin-layer chromatographic visualisation reagent that can be used for the differentiation of aliphatic amines[1].
m-PEG5-CH2COOH is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
Norfluoxetine hydrochloride is an active N-demethylated metabolite of Fluoxetine. Fluoxetine is a selective serotonin (5-HT) reuptake inhibitor that is metabolized to Norfluoxetine hydrochloride by cytochrome P450 (CYP) 2D6, CYP2C19, and CYP3A4. Norfluoxetine hydrochloride inhibits 5-HT uptake and inhibits CaV3.3 T current (IC50 = 5 μM). Norfluoxetine hydrochloride has anticonvulsant activity[1][2][3][4].
Phrixotoxin 2 is a highly selective KV4.2 and KV4.3-channels blocker[1].
beta-1,4-N-Acetylgalactosaminyltransferase (GM2/GD2 synthase) is a key enzyme which catalyzes the conversion of GM3, GD3 and lactosylceramide (LacCer) to GM2, GD2 and asialo-GM2 (GA2), respectively. beta-1,4-N-Acetylgalactosaminyltransferase is a key enzyme to control the synthesis of brain-enriched complex gangliosides[1].
DB818 (DB-818, DB 818) is a small molecule inhibitor of HOXA9/DNA interaction through binding as minor groove DNA ligand on the HOXA9 cognate sequence; directly bind to HOXA9-cognate sequence with Kd value of 4.6 nM (HBS sequence); alters HOXA9-mediated transcription, cell survival and cell cycle inHOXA9-mediated HOXA9-expressing murine MigA9 cell line.
2-Hydroxy-3-methylanthraquinone (compound 1) is a natural compound isolated from a water extract of Hedyotis diffusa WILLD. 2-Hydroxy-3-methylanthraquinone shows inhibitory activity against protein tyrosine kinases v-src and pp60src, and induces growth arrest and apoptosis in the HepG2 cancer cells[1].
FTI-277 Hcl is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling.IC50 value:Target: FTase inhibitorin vitro: Treatment with FTI-277 (20 microM) for 48 h prior to irradiation led to a significant decrease in survival of radioresistant cells expressing the 24-kDa isoform (HeLa 3A) but had no effect on the survival of control cells (HeLa PINA). The radiosensitizing effect of FTI-277 is accompanied by a stimulation of postmitotic cell death in HeLa 3A cells and by a reduction in G(2)/M-phase arrest in both cell types [1]. Treatment of PC-3 cells with GGTI-298 and FTI-277 inhibited migration and invasion in a time- and dose-dependent manner [3].in vivo: FTI-277 treatment prevented increased PTP-1B and PTEN protein expression in burned mice as compared with vehicle alone. In contrast, FTI-277 did not significantly alter protein expression of PTP-1B and PTEN in sham-burned mice [2].
Nemifitide diTFA (INN 00835 diTFA) is a synthetic pentapeptide antidepressant with a potential for rapid onset of action[1]. Nemifitide diTFA is a peptide analog of melanocyte-inhibiting factor (MIF)[2]. Nemifitide diTFA can cross the blood-brain barrier[3].
Neotriptonoterpene, a compound isolated from T. regelii, shows weak cytotoxic activity against A2780, HepG2 and MCF-7 cells with IC50 values of 65.80, 35.45 and 64.80 µM respectively[1].
FR179642 is a key intermediate in the synthesis of the echinocandin antifungal Micafungin[1]. FR179642 is the cyclic peptide nucleus of the echinocandin-like antifungal lipopeptide FR901379[2].
MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3, with a Kd of 27.7 μM. MS37452 can derepress transcription of polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells[1].
Mal-amido-PEG6-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Propargyl-NH-PEG3-C2-NHS ester is a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
1,3-Oxazolidine-2-thione, a free oxazolidinethione, increases thyroid size and severely depresses hepatic trimethylamine oxidase activity in the laying diet domestic fowl[1].
3-Chlorobenzoic acid-d4 is the deuterium labeled 3-Chlorobenzoic acid-d4[1].
Talampanel is a potent and selective AMPA-receptor antagonist, is a potential new antiepileptic drug (AED). Target: AMPA [1]in vitro: Talampanel is a glutamate receptor inhibitor with anti-seizure activity.in vivo： Talampanel reduces motoneuronal calcium in a mouse model of ALS, but its effi cacy declines as the disease progresses, suggesting that medication initiation in the earlier stages of the disease might be more effective. [2]
cis-Clopidogrel-MP Derivative (Clopidogrel-MP-AM) is a 3’-methoxyacetophenone derivative of Clopidogrel active metabolite[1]. Clopidogrel is an orally active platelet inhibitor that targets P2Y12 receptor[2].
TJ-M2010-5 is a MyD88 inhibitor that binds to the TIR domain of MyD88 to interfere with its homodimerization, and the TLR/MyD88 signal pathway[1][2]. TJ-M2010-5 can be used for the research of myocardial ischemia/reperfusion injury (MIRI)[2].
Clinofibrate (S-8527) is a hypelipidemic agent and a HMG-CoA reductase inhibitor.
Isoconazole nitrate is a broad-spectrum antimicrobial agent with a highly effective antimycotic and gram-positive antibacterial activity, a rapid rate of absorption and low systemic exposure potential. Isoconazole nitrate is effective against pathogens involved in dermatomycoses, with minimum inhibitory concentrations well below the concentration of ISN in skin and hair follicles.
Neuropeptide Y (1-24) (human) is a neuropeptide with potencies in inhibiting the electricity stimulated twitch response of rat vas deferens. Neuropeptide Y (1-24) (human) stimulates N-methyl-D-aspartate (NMDA)-induced neuronal activation in the rat CA3 region of the dorsal hippocampus in vivo[1][2].
Rafutrombopag is a thrombopoietin (TPO) agonist extracted from patent CN113929668 A.