3,5-Diiodothyropropionic acid is a thyroid hormone analog, induces α-myosin heavy chain mRNA expression, binds to thyroid hormone receptor (TR), with Ka of 2.40 and 4.06 M-1 for TRα1 and TRβ1, respectively[1].
THK-5105, an arylquinoline derivative, displays high binding affinity to tau fibrils. THK-5105 has high binding affinity to tau protein aggregates and tau-rich Alzheimer disease (AD) brain homogenates. 18F-THK-5105 has the potential to act as a tau imaging PET probe[1].
Cryptotanshinone is a natural compound extracted from the root of Salvia miltiorrhiza Bunge that shows antitumor activities. Cryptotanshinone inhibits STAT3 with an IC50 of 4.6 μM.
Anticancer agent 93 is a 4-Hydroxycoumarin derivative. Anticancer agent 93 can inhibit invasion and migration of lung cancer cells by modulating expression of epithelial-mesenchymal transition (EMT) effectors[1].
SSE15206 is a microtubule polymerization inhibitor, with a GI50 of 197 nM in a SRB proliferation assay in HCT116 cells.
Compound 48/80 trihydrochloride (C48/80 trihydrochloride) is a mixture of condensation products of N-methyl-p-methoxyphenethylamine with formaldehyde. Compound 48/80 trihydrochloride is also a histamine releaser and a mast cell degranulator. Compound 48/80 inhibits phosphatidylinositol-specific phospholipase C activity from human platelets [1][2][3].
Brevinin-1 is an antimicrobial peptide derived from the skin secretions of Rana esculenta[1].
HPK1-IN-15 is a potent and selective inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPKl) originally cloned from hematopoietic progenitor cells is a member of MAP kinase kinase kinase kinases (MAP4Ks) family. HPK1-IN-15 is useful in researching, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer (extracted from patent WO2018049200A1, compound 50)[1].
2,5-Hexanedione-d10 is the deuterium labeled 2,5-Hexanedione[1].
5-Methyl-2-thiouridine (2-Thio-5-methyluridine) is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
DL-Cystine is a cysteine derivative[1].
Hosenkoside N is a baccharane glycoside isolated from lmpatiens buhamina[1].
Benzyl salicylate is a salicylic acid benzyl ester. It can be used as a fragrance additive or UV light absorber.
α-Synuclein (32-37) (human) 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].
Chlorpromazine Hydrochloride is an antagonist of the dopamine D2, 5HT2A, potassium channel andsodium channel. Chlorpromazine binds with D2 and 5HT2A with Kis of 363 nM and 8.3 nM, respectively.
Antiviral agent 19 (Compound 3) is a selective inhibitor against Zika virus infection with an EC50 of 1.3 µM. Antiviral agent 19 has low cytotoxicity[1].
Pyrene azide 3 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors[1][2].
(E)-Osmundacetone is the isomer of Osmundacetone. Osmundacetone significantly suppresses the phosphorylation of MAPKs, including JNK, ERK, and p38 kinases. Osmundacetone has a neuroprotective effect against oxidative stress[1].
4’-C-Methyl-5-methoxyuridine is a uridine analogue. Uridine has potential antiepileptic effects, and its analogs can be used to study anticonvulsant and anxiolytic activities, as well as to develop new antihypertensive agents[1].
Proparacaine Hydrochloride is a voltage-gated sodium channels antagonist with ED50 of 3.4 mM.IC50 Value: 3.4 mM(ED50) [1]Target: Sodium Channelin vitro: Proparacaine is more potent and less toxic than cocaine [1]. Proparacaine significantly increases in FHV-1 (P < 0.01), C. felis, and 28S rDNA Ct values when fusidic acid is used [2].in vivo: Proparacaine inhibits corneal epithelial migration and adhesion through alteration of the actin cytoskeleton [3]. Proparacaine acts like bupivacaine or lidocaine and produces dose-related spinal blockades of motor function, proprioception and nociception. Intrathecal proxymetacaine also produces longer sensory blockade than motor blockade [4].
Quercetagitrin (Quercetagetin-7-O-glucoside), isolated from the flowers of the African Marigold (Tagetes erecta), has anti-inflammatory activity[1][2].
Ganoderenic acid B is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderenic acid B exhibits potent reversal effect on ABCB1-mediated multidrug resistance of HepG2/ADM cells to Doxorubicin[1].
Meclizine is a histamine H1 receptor antagonist used to treat nausea and motion sicknessTarget: Histamine H1 ReceptorMeclizine is a histamine H1 receptor antagonist used to treat nausea and motion sickness, possesses anticholinergic, central nervous system depressant, and local anesthetic effects [1]. Meclizine is an agonist ligand for mouse CAR (constitutive androstane receptor), and an inverse agonist for human CAR. Meclizine increases mCAR transactivation in a dose-dependent manner, stimulates binding of steroid receptor coactivator 1 to the murine receptor in vitro. In contrast, meclizine suppresses hCAR transactivation and inhibits the phenobarbital-induced expression of the CAR target genes, cytochrome p450 monooxygenase (CYP)2B10, CYP3A11, and CYP1A2, in primary hepatocytes derived from mice expressing hCAR, but not mCAR [2].
5-Aza-3’-deoxycytidine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Efineptakin alfa (NT-17) is a long-acting recombinant human IL-7. Efineptakin alfa supports the proliferation and survival CD4+ and CD8+ cells in both human and mice. Efineptakin alfa can be used for glioblastoma research[1].
DYKDDDDK peptide (FLAG) is a useful tool for investigating the function and localization of proteins whose antibodies (Abs) are not available. Often it is also used in a 3X FLAG format (3x DYKDDDDK Tag) for purifying difficult proteins that accumulate in low abundance [1][2].
Tat-NR2B9c (TFA) is a 20-aa peptide, which acts as a postsynaptic density-95 (PSD-95) inhibitor, with an EC50 of 6.7 nM for PSD-95d2 (PSD-95 PDZ domain 2), and 670 nM for PSD-95d1[1]. Tat-NR2B9c also reduces NMDA-induced p38 activation, and possesses neuroprotective efficacy[2].
Azido-PEG11-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Reserpine hydrochloride is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).