Blumenol B, a C13 nor-isoprenoid, can be isolated from the leaves of Casearia sylvestris[1].
pTH (73-84) (human) is a biologically active peptide.
Benin is a potent cytostatic drug that can be used for the treatment of generalized carcinoma of the breast.
2-(Phosphonooxy)benzoic acid is a non-acetylated salicylic acid derivative which is used for treating inflammatory disease as well as in analgesic therapy[1].
RQ-00203078 is a highly selective, potent and orally available TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively), exhibits >350-fold selectivity for TRPM8 over TRPV4, TRPV1 and TRPA1. IC50 value: 5.3 nM (for rat channel), 8.3 nM nM ( for human channel)Target: TRPM8in vitro: RQ-00203078 reduces HSC3 and HSC4 oral squamous carcinoma cell migration and invasion.in vivo: RQ-00203078 demonstrates excellent in vivo activity in a dose dependent manner with an ED50 value of 0.65 mg/kg in the icilin-induced wet-dog shakes model in rats after oral administration and may become an important pharmacological tool for fully assessing the potential therapeutic use of the targets activated by cold stimulation. RQ-00203078 also attenuates icilin-induced wet dog shakes in rats.
17-Hydroxyneomatrine, extracted from Sophora flavescens, can well inhibit the growth of human cervical carcinoma Hela cells, has the wide-range antibacterial, anti-allergy, anti-tumor, anti-arrhythmia, swelling-subsiding diuresis, immunizing, and biological regulation functions[1].
Turmeronol A is a sesquiterpenoid compound.Turmeronol A has anti-inflammatory activity. Turmeronol A prevents macrophage activation and the production of inflammatory mediators by inhibiting the activation of NFκB. Turmeronol A can be used to prevent chronic inflammatory diseases [1].
Boc-PEG2-sulfonic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
TR-14035 is a a dual alpha4beta7(IC50=7 nM)/alpha4beta1 (IC50=87 nM) integrin antagonist .IC50 Value: alpha(4)beta(7)/alpha(4)beta(1)=7/87 nM [1]Target: integrinTR14035 blocked the binding of human alpha(4)beta(7) to an (125)I-MAdCAM-Ig fusion protein with IC(50) values of 0.75 nM. TR14035 blocked binding of human alpha(4)beta(7)-expressing RPMI-8866 cells or murine mesenteric lymph node lymphocytes to MAdCAM-Ig with IC(50) values of 0.1 microM [2]. TR14035 blocked adhesion to HEVs [ED(50) of 0.01-0.1 mpk i.v.].TR-14035 was taken up by rat and human hepatocytes by an apparently single saturable mechanism with K(m) of 6.7 and 2.1 microM, respectively, and taurocholate and digoxin reduced this uptake [3].
Emapunil(AC-5216;XBD-173) is a translocator protein[TSPO (18 kDa)] ligand.IC50 value:Target: TSPO ligandXBD173 enhanced gamma-aminobutyric acid-mediated neurotransmission and counteracted induced panic attacks in rodents in the absence of sedation and tolerance development. XBD173 also exerted antipanic activity in humans and, in contrast to benzodiazepines, did not cause sedation or withdrawal symptoms [1]. The selective TSPO ligand, XBD173 (AC-5216, Emapunil), exerts anxiolytic effects not only in animal models, but also in human volunteers [2].
Mesaconinean, an ingredient from Aconitum carmichaelii Debx., has cardiac effect[1].
2,4,6-Tribromophenol-d2 is the deuterium labeled 2,4,6-Tribromophenol[1].
ML241 is a potent, selective and competitive p97 ATPase inhibitor with an IC50 of 0.11 μM. ML241 can be used for the research of cancer[1].
Glucosylsphingosine (lyso-Gb1) is a deacylated form of glucosylceramide and is also degraded by the glucocerebrosidase. Glucosylsphingosine is a very promising, reliable and specific biomarker for monitoring Gaucher disease[1].
Bufotalin is a cardiotoxic bufanolide steroid, cardiac glycoside analogue, secreted by a number of toad species; a novel anti-osteoblastoma agent.IC50 value:Target:in vitro: bufotalin induced osteoblastoma cell death and apoptosis in dose- and time-dependent manners. Further, bufotalin induced endoplasmic reticulum (ER) stress activation in osteoblastoma cells, the latter was detected by the induction of C/EBP homologous protein (CHOP), phosphorylation of inositol-requiring enzyme 1 (IRE1) and PKR-like endoplasmic reticulum kinase (PERK), as well as caspase-12 activation [1]. Bufotalin was the most potent active compound among these four bufadienolides, and it exerted stronger inhibitory effect on the viability of doxorubicin-induced multidrug resistant liver cancer cells (R-HepG2) than that of their parent cells HepG2. bufotalin treatment induced cell cycle arrest at G(2)/M phase through down-regulation of Aurora A, CDC25, CDK1, cyclin A and cyclin B1, as well as up-regulation of p53 and p21. Bufotalin treatment also induced apoptosis which was accompanied by decrease in mitochondrial membrane potential, increases in intracellular calcium level and reactive oxygen species production, activations of caspase-9 and -3, cleavage of poly ADP-ribose polymerase (PARP) as well as changes in the expressions of bcl-2 and bax [2]. Bufotalin promoted death receptor-mediated cell death, especially TRAIL-induced apoptosis, through activation of caspase-3 and PARP-1. Cotreatment of bufotalin with TRAIL resulted in the downregulation of anti-apoptotic proteins, including Bcl-XL, Mcl-1, survivin and XIAP, and the up-regulation of MAPKs and TRAIL receptor DR5. In addition, phosphorylation of STAT1 was strongly inhibited by bufotalin [3]. externalization of phosphatidylserine, accumulation of sub-G(1) cells, fragmentation of DNA, and formation of apoptotic bodies were observed in bufotalin-treated Hep 3B cells [4].
(S)-3-Hydroxy Midostaurin ((S)-CGP52421) is a potent kinases inhibitor with IC50 values of <400 nM for 13 kinases (VEGFR-2, TRK-A, FLT3, et). (S)-3-Hydroxy Midostaurin is a minor metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (S)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML)[1].
NLRP3-IN-15 is a potent and selective NLRP3 inflammasome inhibitor. NLRP3-IN-15 inhibits IL-1β release with an IC50 of 0.114 μM. NLRP3-IN-15 can be used for the research of inflammation[1].
PAT-1251 Hydrochloride is a potent, selective and oral lysyl oxidase-like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively).
Chromium picolinate (Chromium (III) picolinate) reduces insulin resistance and is widely used in prevention and treatment of type 2 diabetes mellitus[1].
Methyl reserpate (NSC 81464) is a Yohimbine (HY-12715) type alkaloid, that can be isolated from Rauwolfia vomitoria roots and leaves[1].
Ala-Ala-Ala-Ala is a poly-L-alanine (PLA) sequences. PLA is a kind of key element of the crystalline domains of spider dragline and wild silkworm silks[1].
Ethyl linoleate inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators[1].
S-MTC is a selective type I nitric oxide synthase (NOS) inhibitor.
Teprotumumab is an IGF-1 receptor (IGF-1R) blocking human monoclonal antibody. Teprotumumab binds to the ligand binding extracellular α-subunit domain of IGF-1R. Teprotumumab inhibits TSH and IGF-1 action in fibrocytes. Teprotumumab attenuates TSH-dependent IL-6 and IL-8 expression and Akt phosphorylation. Teprotumumab can be used for thyroid-associated ophthalmopathy research[1].
CEF7, Influenza Virus NP (380-388) is a HLA-B*08 restricted influenza virus nucleoprotein epitope. Influenza virus NP functions as a key adapter molecule between virus and host cell processes[1][2].
7-O-methylepimedonin G is a prenylated 2-phenoxychromone that can be isolated from Epimedium brevicornum[1].
Hydroxyamine hydrochloride is a selective monoamine oxidase (MAO) inhibitor used for inhibiting of platelet aggregation. Hydroxyamine hydrochloride is an intermediate of organic synthesis[1].
SCD1-IN-1 is a SCD1 inhibitor (IC50: 5.8 nM). SCD1-IN-1 can be used in the research of dermatologic condition[1].
H-Trp-Phe-Tyr-Ser(PO3H2)-Pro-Arg-pNA is a chromogenic substrate for Pin1. Pin1 is an essential and conserved mitotic peptidyl-prolyl isomerase, and can recognize the phosphoserine-proline bonds present in mitotic phosphoproteins[1][2].