TTK21 (CBP-p300 activator TTK21) is a small molecule activator of CBP/p300 histone acetyltransferase activity with a maximal effect at a concentration of 275 uM; induces acetylation of histones H3 and H4 in vitro but not H2B and H2A; promotes neurogenesis and extends memory duration in adult mice, promotes regeneration and sprouting of sensory and motor axons, as well as recovery of sensory and motor functions in both the mouse and rat model of spinal cord injury.
mGAT3/4-IN-1 (compound 19b) is a potent mGAT3/mGAT4 inhibitor, with pIC50 values of 5.31 and 5.24, respectively. mGAT3/4-IN-1 exhibits a significant tactile allodynia reduction in diabetic neuropathic mice[1].
Bismuth subgallate, a hemostatic agent, acts on coagulation factor XII (Hageman factor), leading to the activation of the coagulation cascade and improving early formation of a fibrin clot[1][2].
Hydroxy-PEG3-acrylate is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
LDV, a non-fluorescent derivative of LDV FITC, is a α4β1 integrin (VLA-4) ligand (Kd ~ 12 nM).
S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nM.
9-Dehydroxyeurotinone is an anthraquinone derivative that can be found in Eurotium rubrum. 9-Dehydroxyeurotinone shows cytotoxicity with an IC50 value of 25 µg/mL for SW1990 cells[1].
Odatroltide, as a nanoscale P-selectin inhibitor, is a nano-delivery system of 6,7-dihydroxyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid and KPAK to target the thrombus[1].
Pexopiprant is an oral antagonist of the prostaglandin D2 receptor 2 (DP2),Ki ＜ 100nM. Pexopiprant can be used in studies of asthma[1].
Cy5 is a reactive dye for the labeling of amino-groups in peptides, proteins, and oligonucleotides. This dye requires small amount of organic co-solvent (such as DMF or DMSO) to be used in labeling reaction. This reagent is ideal for very cost-efficient labeling of soluble proteins, as well as all kinds of peptides and oligonucleotides. This reagent also works well in organic solvents for small molecule labeling.Excitation (nm):649, Emission (nm): 670.
Pamabron is a common over-the-counter diuretic used for relief of menstrual-associated symptoms. The active diuretic ingredient in pamabrom is 8-bromotheophylline. Pamabrom is available in combination with acetaminophen (paracetamol) for various conditions such as back pain and menstrual relief. The acetaminophen helps reduce menstrual pains and the pamabrom reduces associated bloating.
Taxuspine B is a natural product, that can be isolated from Japanese yew Taxus. Taxuspine B exhibits appreciable taxol-like activity to reduce CaCl2-induced depolymerixation of microtubules among the taxoids[1].
Cetirizine D8 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1][2][3].
Poststerone is a nature product. Poststerone is a metabolite of insect metamorphosing substances from Cyathula capata[1].
Methyl-PEG4-acyl chloride is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Mal-C2-cyclohexylcarboxyl-hydrazide (TFA) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Raddeanin A is a natural triterpenoid saponin component of Anemone raddeana, with anti-cancer activities. Raddeanin A exerts anticancer effect on human osteosarcoma via the ROS/JNK and NF-κB signal pathway[1][2][3][4].
C6 NBD Sphingomyelin is a fluorescent short-chain analogue of Sphingomyelin (HY-113498). Chlamydia trachomatis acquires C6 NBD Sphingomyelin endogenously synthesizes from C6-NBD-ceramide and transportes to the chlamydial inclusion. C6 NBD Sphingomyelin can incorporate into the plasma membrane[1].
Andrastin A meroterpenoid compound, is a farnesyltransferase inhibitor. Andrastin A inhibits the efflux of anticancer compounds from multidrug-resistant cancer cells. Andrastin A can be isolated from Penicillium species[1][2].
Antitumor agent-65 (Compound 5) is an analogue/derivative of (-)-cleistenolide. Antitumor agent-65 has the potential for the research of cancer diseases[1].
OSS_128167 is a selective SIRT6 inhibitor with IC50s of 89, 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively.
7α-O-Ethylmorroniside is an iridoid[1].
Forsythoside H, a caffeoyl phenylethanoid glycoside (CPG) isolated from the fruits of Forsythia suspense (Thunb.) Vahl, may possesses anti-inflammatory activities[1].
D-Xylofuranose, 1,2,3,5-tetraacetate is the raw material for nucleotides synthesis[1].
RS Domain derived peptide is a biological active peptide. (This peptide is a substrate for Clk/Sty and is phosphorylated by Clk/Sty protein kinase (Km=102 microM).)
TS-011 is a selective inhibitor of 20-Hydroxyeicosatetraenoic acid synthesis.
CY 208-243 is a selective dopamine D1 receptor agonist which exhibits antiparkinsonian activity[1].
IKarisoside A(Icarisoside-A) is a natural compound isolated from Epimedium koreanum (Berberidaceae); has anti-inflammatory properties.IC50 value:Target: in vitro: Ikarisoside A inhibited the expression of LPS-stimulated inducible nitric oxide synthase (iNOS) and the production of nitric oxide (NO) in LPS-stimulated RAW 264.7 cells and mouse bone marrow-derived macrophages (BMMs) in a concentration-dependent manner. In addition, Ikarisoside A reduced the release of pro-inflammatory cytokines, such as tumor necrosis factor-alpha (TNF-alpha) and interleukin-1 beta (IL-1 beta). Furthermore, Ikarisoside A inhibited the activity of p38 kinase and nuclear factor-kappaB (NF-kappaB) [1]. Ikarisoside A is a potent inhibitor of osteoclastogenesis in RANKL-stimulated RAW 264.7 cells as well as in bone marrow-derived macrophages.The inhibitory effect of Ikarisoside A resulted in decrease of osteoclast-specific genes like matrix metalloproteinase 9 (MMP9), tartrate-resistant acid phosphatase (TRAP), receptor activator of NF-kappaB (RANK), and cathepsin K. Moreover, Ikarisoside A blocked the resorbing capacity of RAW 264.7 cells on calcium phosphate-coated plates. Ikarisoside A also has inhibitory effects on the RANKL-mediated activation of NF-kappaB, JNK, and Akt [2].
Direct Blue 86 (Solvent Blue 38) is a myelin-sheath stain, commonly utilized in microscopy to detect demyelination in the central nervous system. Direct Blue 86 also is a dye with various applications including as a commercial dye in the printing of cotton and mucilage glue fabrics[1].
Folinic acid is an adjuvant used in cancer chemotherapy involving the drug methotrexate.Target: AntifolateFolinic acid is a 5-formyl derivative of tetrahydrofolic acid. It is readily converted to other reduced folic acid derivatives (e.g., tetrahydrofolate), and, thus, has vitamin activity that is equivalent to that of folic acid. Since it does not require the action of dihydrofolate reductase for its conversion, its function as a vitamin is unaffected by inhibition of this enzyme by drugs such as methotrexate. In 1980s, however, folinic acid was found to reactivate the dihydrofolate reductase itself even when methotrexate exists. Although the mechanism is not very clear, the polyglutamylation of methotrexate and dihydrofolate in malignant cells is considered to play an important role in the selective reactivation of dihydrofolate reductase by folinic acid in normal cells [1]. Folinic acid is generally administered along with MTX as a rescue agent to decrease MTX-induced toxicity. However, information regarding the inhibitory effect of folinic acid against cytogenetic damage caused by MTX is limited. This study was conducted to assess the cytogenetic effect of MTX and its inhibition by folinic acid (FA) using the micronucleus and chromosomal aberration assays concurrently [2].