Arginase inhibitor 1 is a potent inhibitor of human arginases I and II with IC50s of 223 and 509 nM, respectively.
Ladanetin-6-O-β-(6′′-O-acetyl)glucoside is a flavonoid isolated from the whole plants of Dracocephalum tanguticum, with antioxidant ability. Flavonoids from Dracocephalum tanguticum show cardioprotective effects against Doxorubicin (HY-15142A)-induced toxicity in H9c2 cells[1].
7'-O-DMT-morpholino thymine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
TRPM4-IN-2 (NBA) is a potent transient receptor potential melastatin 4 (TRPM4) inhibitor with an IC50 value of 0.16 μM. TRPM4-IN-2 can be used for researching prostate cancer and colorectal cancer[1][2].
Brevinin-1Ea is an antimicrobial peptide derived from the skin secretions of Rana esculenta[1].
Paullinic acid is a long-chain fatty acid that has been detected in multiple biofluids, such as blood and urine.
Cardanol monoene (Cardanol C15:1) is a phenolic compound which can be found in cashew nut shell liquid. Cardanol monoene can induce mitochondria-associated apoptosis in human melanoma cells[1].
SSAO inhibitor-3 (Compound 2) is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor with IC50s of <10 nM, and 0.1-10 μM for human SSAO and AOC1, respectively. SSAO inhibitor-3 can be used for the research of atherosclerosis, diabetes and its complications, obesity, stroke, chronic kidney disease, retinopathy, chronic obstructive pulmonary disease (COPD), autoimmune diseases, multiple sclerosis, etc[1].
Antitumor Compound 1 is a potent compound which comprises a new imidazopyridine having excellent antitumor activity as an active ingredient.Reference:Polymer-linked imidazopyridines useful as tumor-targeting cytotoxic agentsBy Kasuya, Hiroshi; Miyazaki, Hideki; Hayakawa, Ichio; Kanno, Yuichi; Watanabe, KazuyoshiFrom Jpn. Kokai Tokkyo Koho (2004), JP 2004002826 A 20040108. Pharmaceuticals containing imidazopyridines for prophylactic and therapeutic treatment of tumorBy Hayakawa, Ichio; Kanno, Yuichi; Azuma, Toshiki; Furukawa, Hidehiko; Naruto, Shunji; Kurakata, ShinichiFrom Jpn. Kokai Tokkyo Koho (2003), JP 2003313126A 20031106.Preparation of imidazopyridine derivatives as antitumor agentsBy Hayakawa, Ichiro; Sugano, Yuichi; Agatsuma, Toshinori; Furukawa, Hidehiko; Kurakata, Shinichi; Naruto, ShunjiFrom PCT Int. Appl. (2002), WO 2002034748 A1 20020502.
CVT-313 is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM.
FGF basic (93-110) (human, bovine) 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].
Beclomethasone 17-propionate (Beclomethasone-17-monopropionate), an active metabolite of Beclomethasone dipropionate (HY-13571), is a glucocorticoid receptor (GR) agonist. Beclomethasone 17-propionate exhibits greater affinity for GR than Beclomethasone dipropionate. Beclomethasone 17-propionate effectively suppresses cytokine production in chronic obstructive pulmonary disease (COPD) lung macrophages[1][2][3].
Diapocynin (Dehydrodiacetovanillone), a dimeric derivative of Apocynin, is an orally active NADPH oxidase inhibitor. Diapocynin has anti-inflammatory, neuroprotection and antioxidant activities[1].
Morusin is a prenylated flavonoid isolated from M. australis with various biological activities, such as antitumor, antioxidant, and anti-bacteria property. Morusin could inhibit NF-κB and STAT3 activity.
Adrenocorticotropic Hormone (ACTH) (1-39), rat is a potent melanocortin 2 (MC2) receptor agonist.
DB1976 hydrochloride is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 hydrochloride potently inhibits PU.1 binding (IC50 of 10 nM) and strongly inhibits the PU.1/DNA complex (with high DB1976-λB affinity, KD of 12 nM) in vitro. DB1976 hydrochloride has apoptosis-inducing effect[1][2][3].
Acetyl-PHF6YA amide is a biologically active peptide.
Kisspeptin-54 (27-54) (human) is a polypeptide that can be used for compound synthesis and pharmaceutical research[1][2].
KL001 is a cryptochrome protein (CRY) stabilizer which specifically interacts with CRY1 and CRY2. KL001 prevents ubiquitin-dependent degradation of CRY, resulting in lengthening of the circadian period. KL001 has the potential to control fasting hormone-induced gluconeogenesis[1][2].
(rel)-Eglumegad ((rel)-LY354740) is the racemic isomer of Eglumegad (HY-18941). Eglumegad is a highly potent and selective group II (mGlu2/3) receptor agonist with EC50s of 5 and 24 nM for transfected human mGlu2 and mGlu3 receptors, respectively[1].
Eribulin (E7389; ER-086526), a synthetic analogue of halichondrin B in phase III clinical trials for breast cancer, binds to tubulin and microtubules.Target: Microtubule/TubulinEribulin suppressed centromere dynamics at concentrations that arrest mitosis. At 60 nmol/L eribulin (2 x mitotic IC(50)), the relaxation rate was suppressed 21%, the time spent paused increased 67%, and dynamicity decreased 35% (but without reduction in mean centromere separation), indicating that eribulin decreased normal microtubule-dependent spindle tension at the kinetochores, preventing the signal for mitotic checkpoint passage [1]. [(3)H]eribulin binds soluble tubulin at a single site; however, this binding is complex with an overall K(d) of 46 microM, but also showing a real or apparent very high affinity (K(d) = 0.4 microM) for a subset of 25% of the tubulin. Eribulin also binds microtubules with a maximum stoichiometry of 14.7 +/- 1.3 molecules per microtubule (K(d) = 3.5 microM), strongly suggesting the presence of a relatively high-affinity binding site at microtubule ends. At 100 nM, the concentration that inhibits microtubule plus end growth by 50%, we found that one molecule of eribulin is bound per two microtubules, indicating that the binding of a single eribulin molecule at a microtubule end can potently inhibit its growth. Eribulin does not suppress dynamic instability at microtubule minus ends [2]. Eribulin's in vivo superiority derives from its ability to induce irreversible mitotic blockade, which appears related to persistent drug retention and sustained Bcl-2 phosphorylation [3].
Adenylyl cyclase type 2 agonist-1 (Compound 73) is a potent agonist of adenylyl cyclase type 2 (AC2) with the EC50 of 90 nM. Adenylyl cyclase type 2 agonist-1 inhibits expression of Interleukin-6, making it a potential lead compound against respiratory diseases[1].
Acridine Orange base is a cell-permeable fluorescent dye that stains organisms (bacteria, parasites, viruses, etc.) bright orange and, when used under appropriate conditions (pH=3.5, Ex=460 nm), distinguishes human cells in green for detection by fluorescence microscopy. Acridine Orange base fluoresces green when bound to dsDNA (Ex=488, Em=520-524) and red when bound to ssDNA (Ex=457, Em=630-644) or ssRNA (Ex=457, Em=630-644), also can be used in cell cycle assays[1][2][3].
PKCd (8-17) is a biological active peptide. (This peptide is derived from the V1 domain of protein kinase C (PKC)d. It inhibits phorbol 12-myristate 13-acetate (PMA)-induced PKCd translocation and activation. Inhibition of PKCd reduces ischemia damage in cardiac and cerebral cells, induces proliferation of fibroblasts, and inhibits graft coronary artery disease in mice.)
WU-04 is a non-covalent inhibitor of SARS-CoV-2, targeting the 3CLpro protein. WU-04 has high inhibitory effect on the 3CLpro protein of 6 SARS-CoV-2 variants (Alpha, Beta, Gamma, Delta, Lambda and Omicron) and 2 coronaviruses (SARS-CoV and MERS-CoV)[1].
3-Hydroxyvaleric acid is a 5-carbon ketone body. 3-Hydroxyvaleric acid is anaplerotic, meaning it can refill the pool of TCA cycle intermediates.
6-Amino-5-nitropyridin-2-one is a pyridine base and used as a nucleobase of hachimoji DNA, in which it pairs with 5-aza-7-deazaguanine[1].
Oxyphenonium bromide is an antiacetylcholine compound. Oxyphenonium bromide is an antagonist of mAChR. Oxyphenonium bromide protects against the bronchial obstructive effects[1][2][3].
Todralazine hydrochloride (Ecarazine hydrochloride) is an anti-hypertensive agent, acts as a β2AR blocker, with antioxidant and free radical scavenging activity[1].
Apelin-36(rat, mouse) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ[1][2].