Ezurpimtrostat hydrochloride (compound 2-3) is a potent and orally active anti-fibrotic agent. Ezurpimtrostat hydrochloride reduces significantly the liver fibrosis in DEN (diethyl nitrosamine) cirrhotic rat model. Ezurpimtrostat hydrochloride can be used for the research of fibrosis, cancer, autophagy and cathepsins B (CTSB), L (CTSL) and D (CTSD) related diseases [1].
Levomefolic acid-13C,d3is the deuterium labeledLevomefolic acid(HY-14781)[1]. Levomefolic acid (5-MTHF) is an orally active, brain-penetrant natural active form of folic acid and is one of the most widely used folic acid food supplements[2][3].
Bleomycin A5 (Pingyangmycin) is an orally active glycopeptide antibiotics. Bleomycin A5 has a role as an antineoplastic agent, an Apoptosis inducer and a bacterial metabolite[1][2].
MrgprX2 antagonist-2 is an MrgprX2 antagonist extracted from patent WO2021092262A1, example E163. MrgprX2 antagonist-2 can be used for the research of inflammatory disorders of the skin[1].
MKC3946 is a potent and soluble IRE1α inhibitor, used for cancer research.
c-Met-IN-2 is a potent, selective and orally available c-Met inhibitor, with an IC50 of 0.6 nM, with antitumor activity.
ODN 21158 is a potent G-modified TLR3 andTLR9inhibitor. ODN 21158 shows no cytotoxic. ODN 21158 nhibits IFN-α secretion in a dose dependent manner[1].
Quinagolide hydrochloride is a selective dopamine D2 receptor agonist, also is a prolactin inhibitor. Target: dopamine D2 receptor, prolactinQuinagolide is a selective, D2 receptor agonist (or prolactin-release inhibitor) that is used for the treatment of elevated levels of prolactin. Quinagolide is helpful in reducing prolactin levels to reduce milk production for certain medical reasons and to treat some types of infertility, breast problems and menstrual disorders. Quinagolide exerts a strong and specific inhibitory effect on prolactin release by acting directly on the prolactin-secreting cells of the anterior pituitary without reducing the levels of other pituitary hormones.
Tacrine hydrochloride is a potent inhibitor of both AChE and BChE, with IC50s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC50 of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease[1][2].
Indomethacin (Indometacin) sodium is a potent, orally active COX1/2 inhibitor with IC50 values of 18 nM and 26 nM for COX-1 and COX-2, respectively. Indomethacin sodium has anticancer activity and anti-infective activity. Indomethacin sodium can be used for cancer, inflammation and viral infection research.[1][2][3].
ML 10302 hydrochloride is a potent and selective 5-HT4 receptor agonist, with an EC50 of 4 nM。ML 10302 hydrochloride displays more than 680-fold selectivity over 5-HT3 receptor in binding assay[1][2].
Apigenin-7-glucoside exhibits significant anti-proliferative and antioxidant activity, scavengers of ROS.In vitro: exhibits significant anti-proliferative activity against B16F10 melanoma cells after 24 and 48 h of incubation. Apigenin-7-glucoside provoks an increase of subG0/G1, S and G2/M phase cell proportion with a significant decrease of cell proportion in G0/G1 phases. Apigenin-7-glucoside enhances melanogenesis synthesis and tyrosinase activity of B16F10 melanoma cells. [1] Api7G specifically induced the differentiation of CD34+ cells towards the erythroid lineage and inhibited the myeloid differentiation. [2] APIG had strong antioxidant activity against reactive oxygen species (ROS) in vitro in a concentration-dependent manner.
WRNA10 is a potent HIV-1 TAR RNA binder with an IC50 of 10 µM and an CC50 of 40 µM[1].
AM841 is a high-affinity electrophilic ligand. AM841 interacts covalently with a cysteine in helix six and activates the CB1 cannabinoid receptor. AM841 reduces Forskolin (HY-15371)-stimulated cAMP accumulation. AM841 also slows gastrointestinal motility[1][2].
Argininosuccinic acid disodium participates in the fourth step of the urea cycle and is cleaved into arginine and fumarate by argininosuccinate lyase (ASL). Argininosuccinic acid disodium reduces reduced glutathione (GSH) concentrations and increases reactive oxygen species production in the cerebral cortex and striatum. Argininosuccinic acid disodium causes lipid peroxidation and protein oxidation and also induces oxidative stress in the developing rat brain[1][2].
NEK6 inibitor 8 (ZINC05007751) is a novel inhibitor of the NIMA-related kinase NEK6 with IC50 of 3.4 uM, compound 8 is very selective against NEK1 and NEK6, while no signifcant activity was observed against NEK2, NEK7, and NEK9; dispalys antiproliferative activity against a panel of human cancer cell lines (IC50 <100 uM).
Revdofilimab (ABBV-368) is a human IgG1 agonist monoclonal antibody against OX40. Among them, OX40 is a member of the TNF receptor superfamily expressed on activated and memory T cell subsets and T regulatory cells[1].
CID5721353 is an inhibitor of BCL6 with an IC50 value of 212 μM, which corresponds to a Ki of 147 μM.
Selachyl alcohol is an orally active antihypertensive agent. Selachyl alcohol has similar activities with antihypertensive neutral renomedullary lipid (ANRL). Selachyl alcohol is an alkylglycerol compound in shark liver oil mixture with properties that reduce lung metastasis. Selachyl alcohol can be used for cardiovascular disease research[1][2].
Monomethyl lithospermate activates the PI3K/AKT pathway, which plays a protective role in nerve injury. Monomethyl lithospermate can improve the survival ability of SHSY-5Y cells, inhibit the breakdown of mitochondrial membrane potential (MMOP) and inhibit cell apoptosis. Monomethyl lithospermate also reduced the level of oxidative stress in the brain tissue of rats with middle artery occlusion (MCAO) and improved nerve damage in rats with ischemic stroke (IS)[1].
Hydroxydione has an effect of general anesthetic. Hydroxydione is a neuroactive steroid it can be used for anaesthesia related research[1][2].
LY231617 is a potent and blood-brain barrier penetrable antioxidant. LY231617 is a neuroprotective agent in brain, it can be used for the research of nervous disease[1][2].
[6]-Gingerol is an active compound isolated from Ginger (Zingiber officinale Rosc), exhibits a variety of biological activities including anticancer, anti-inflammation, and anti-oxidation.
PARP1-IN-7 is an inhibitor of poly(ADP-ribose) polymerase-1 (PARP1) as an anticancer agent.
Cbz-Tyr-Ala-OH is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development[1].
Petunidin 3-rutinoside is a natural product that can be isolated from Sambucus canadensis[1].
Cefepime (BMY-28142) chloride is a broad-spectrum and cross the blood-brain barrier cephalosporin. Cefepime chloride shows antibacterial effects against both Gram-positive and Gram-negative aerobic bacteria. Cefepime chloride induces neurotoxicity[1][2][3][4].
MASM7 is a mitofusin activator, and can achieve mitochondrial fusion via mitofusins[1].
AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib (HY-10205)[1].
OMDM-3 is a selective and metabolically stable inhibitor of anandamide cellular uptake (ACU), with a Ki of 16.6 μM[1].