Kisspeptin 234 TFA, is a 10 amino acid peptide as well as a kisspeptin receptor (KISS1, GPR54) antagonist. Kisspeptin 234 TFA is an analog of Kisspeptin 10[1].
Pomalidomide is an anti-angiogenic agent and an immunomodulator. Pomalidomide inhibits TNF-α release in LPS stimulated human PBMC with an IC50 of 13 nM.
Metadoxine blocks adipocyte differentiation in association with inhibition of the protein kinase A-cAMP response element binding protein (PKA-CREB) pathway.
Carubicin hydrochloride is a microbially-derived compound. Carubicin hydrochloride is an effective inhibitor of VHL-defective (VHL−/−) CCRCC cell proliferation. Carubicin hydrochloride also induces apoptosis by a mechanism independent of p53 or hypoxia-inducible factor HIF2. Carubicin hydrochloride has the potential for the research of cancer diseases[1][2].
H-Leu-Leu-Ala-OH is a tripeptide composed of two L-leucine units joined to L-alanine by a peptide linkage. H-Leu-Leu-Ala-OH shows antioxidant activities[1].
Geniposidic acid is an effective anticancer and radioprotection agent.Target: OthersMice were given an intraperitoneal injection of Geniposidic acid (GA) (12.5, 25, 50 mg/kg) 1 h before receiving GA against d-galactosamine (GalN) (800 mg/kg)/LPS (40 μg/kg). Liver and blood samples were collected 1 and 8 h after GalN/LPS injection. The survival rate of the GA group was significantly higher than the control. GalN/LPS increased serum aminotransferase activity, serum tumor necrosis factor-α level and hepatic lipid peroxidation and decreased hepatic glutathione content [1]. GA enhanced significantly the postirradiation responses of splenic blastogenesis by PHA. In addition, GA is a potent tumor growth inhibitor when combined with the X-irradiation, though there was no significant synergetic effect on their combined antitumor activity. The preliminary results of GA on hematological and blastogenic observations in this study suggested that it may very well, partially, play a role in an effective anticancer product with the ability to decrease undesirable radiation damage to the hematologic tissue after high dose irradiation [2].
PKR-IN-C51(compound 51) is an ATP-competitive double-stranded RNA-activated protein kinase (PKR) inhibitor with an IC50 of 9 μM. PKR-IN-C51 inhibits intracellular PKR activation in a dose-dependent manner in primary mouse macrophages[1].
3’-Acetate-ATP, an ATP analogue, is ATP acetylation product with an maxima uv absorption at 259 nm in water at neutral pH. 3’-Acetate-ATP exerts a blocking effect on nucleic acid polymerization[1].
(S)-N-FMoc-2-(6'-heptenyl)alanine is a amino acid, which can be used in peptide synthesis[1].
BMS-986163 is a negative allosteric modulator of GluN2B. The prodrug BMS-986163 rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM).
C75 trans is an enantiomer of C75. C75 is a synthetic fatty-acid synthase (FASN) inhibitor; inhibits prostate cancer cells PC3 with an IC50 of 35 μM.
Ophiobolin B, a sesterterpene metabolite of Helminthosporium oryzae, inhibits proton extrusion from maize coleoptiles. Ophiobolin B inhibits fusicoccin (FC) promoted proton extrusion, potassium uptake and cell enlargement[1]. The MIC values with the antifungal effect of Ophiobolins B on different zygomycetes is 25–50 μg/mL[2].
Zonisamide is a 1,2 benzisoxazole derivative and the first agent of this chemical class to be developed as an antiepileptic drug.Target: Calcium channel inhibitor; Sodium channel inhibitorZonisamide is a sulfonamide anticonvulsant approved for use as an adjunctive therapy in adults with partial-onset seizures for adults; infantile spasm, mixed seizure types of Lennox-Gastaut syndrome, myoclonic, and generalized tonic clonic seizure. Zonisamide is a 1,2 benzisoxazole derivative and the first agent of this chemical class to be developed as an antiepileptic drug. It has shown activity in various animal models of epilepsy, and although a detailed mode of action awaits clarification it appears to block the propagation/spread of seizure discharges and to suppress the epileptogenic focus [1].Zonisamide 500 mg/day was significantly superior to placebo in reducing the frequency of complex partial seizures (-51% versus -16%), all partial seizures and all seizures, with dose-dependent benefit provided over a 100-500 mg/day dose range. Supporting trials have confirmed significant increases in reduction in median seizure frequency (up to 41%) and responder rates (35-42%) compared with placebo following zonisamide 400-600 mg/day, enabling 20-27% of patients to attain >or=75% reduction in seizure frequency [2].Clinical indications: Epilepsy; Lewy body dementia; Parkinsons diseaseToxicity: Anorexia; Somnolence; Dizziness; Irritability; Confusional state; Depression; Diplopia; Memory impairment
FAUC 365 is a highly dopamine D3 receptor-selective antagonist with Ki values of 0.5 nM, 340, 2600, and 3600 nM at D3, D4.4, D2short, and D2Long receptors, respectively. FAUC 365 can be used for the research of schizophrenia, and Parkinson's disease[1][2].
4-Hydroxymephenytoin is a metabolism of an antiepileptic drug mephenytoin, which is used as a CYP2C19 substrate.
Isotoosendanin is a limonoid isolated from Melia toosendan fruit. Isotoosendanin displays significant anti-inflammatory and analgesic activities[1].
S1R agonist 1 (Compound 6b) hydrochloride is a selective S1R agonist with Kis of 0.93 nM and 72 nM for S1R and S2R, respectively. S1R agonist 1 hydrochloride exhibits neuroprotection against ROS and NMDA-induced neurotoxicity[1].
Aristolactam A IIIa (Sch 546909) is an aristolactam-type alkaloid that can be isolated from Glycosmis chlorosperma. Aristolactam A IIIa is a DYRK1A Inhibitor. Aristolactam A IIIa inhibits platelet aggregation induced by arachidonic acid (AA), collagen and platelet-activating factor (PAF). Aristolactam A IIIa has strong cytotoxic effect on HeLa cells[1].
DHFR-IN-1 (compound 12) is a potent and selective DHFR (dihydrofolate reductase)inhibitor, with an IC50 of 40.71 nM. DHFR-IN-1 exhibits promising antibacterial activity against gram-positive and gram-negative bacteria. DHFR-IN-1 exhibits moderate antifungal activities. DHFR-IN-1 exhibits a high synergistic effect with Levofloxacin (HY-B0330), where the FIC (fractional inhibitory concentration index) value is 0.249[1].
Zilganersen sodium is a glial fibrillary acidic protein (GFAP) inhibitor. Zilganersen sodium can be used in Alexander disease (AxD) research[1][2].
2-Amino-1-phenylethanol is an analogue of noradrenaline.
Dafsolimab (SPV-T3a) is an IgG2a murine monoclonal antibody (anti-CD3). Dafsolimab can induce cell death through modulation and activation of the CD3/T cell receptor complex. Dafsolimab can be used for the research of graft-versus-host disease (GVHD)[1].
DDMAB is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
LY 163443 is a selective antagonist of leukotrienes D4 (LTD4) and E4 (LTE4). LY 163443 can antagonize LTD4-induced contractions of guinea pig ileum, trachea, and lung parenchyma. LY 163443 also inhibits tracheal contractions to LTE4[1][2].
Procaine Hydrochloride is a local anesthetic drug of the amino ester group.Target: OthersProcaine is a local anesthetic of the ester type that has a slow onset and a short duration of action.Procaine (0.01-100 microM) inhibited the 5-HT3 receptor-mediated inward current in the whole-cell patch clamp recording. Procaine appears to produce a competitive inhibition on 5-HT3 receptors with a KD of 1.7 microM [1]. Procaine is a DNA-demethylating agent that produces a 40% reduction in 5-methylcytosine DNA content as determined by high-performance capillary electrophoresis or total DNA enzyme digestion. Procaine can also demethylate densely hypermethylated CpG islands. Procaine also has growth-inhibitory effects in these cancer cells, causing mitotic arrest [2]. Procaine functions as an excitant of limbic system cells, and that procaine alters synaptic transmission in some, but not all, output pathways from the amygdale [3].
DC07090 dihydrochloride is a low toxicity, potent, reversible and competitive non-peptidyl human enterovirus 71 3C protease inhibitor with an IC50 and a Ki value for 21.72 μM and 23.29 μM. DC07090 dihydrochloride could also inhibit coxsackievirus A16 (CVA16) replication with an EC50 value of 27.76 μM[1].
Voruciclib hydrochloride is a clinical stage oral CDK9 inhibitor. Voruciclib hydrochloride represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL)[1].
Ala-Ala-Asn-PAB is a peptide cleavable ADC linker for antibody-drug conjugates (ADCs)[1].
PG-11047 (CGC-11047) is a polyamine analogue. PG-11047 can be used for the research of breast cancer[1].
GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus.