2-Amino-N,N-dimethyl-2′-C-methyladenosine 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].
Albutoin (BAX 422Z), an anticonvulsant agent, is a thiohydantoin derivative used for the research of grand mal epilepsies[1].
N-Salicyloyltryptamine acts on voltage-dependent Na+, Ca2+, and K+ ion channels inhibitor. N-Salicyloyltryptamine inhibits K+ currents with an IC50 value of 34.6 μM (Ito). N-Salicyloyltryptamine also exhibits anticonvulsant, anti-inflammatory, analgesic, and vasorelaxation effect[1]-[5].
Nitroflurbiprofen is a cyclooxygenase (COX) inhibitor with nitric oxide (NO)-donating properties, modulates the increased intrahepatic vascular tone in portal hypertensive cirrhotic rats.
Glutaminyl Cyclase Inhibitor 3 (compound 212 ), a designed anti-Alzheimer’s compound, is a potent human Glutaminyl Cyclase (GC) inhibitor, with an IC50 of 4.5 nM. Glutaminyl Cyclase-IN-1 (compound 212) significantly reduced the brain concentrations of pyroform Aβ and total Aβ and restored cognitive functions[1].
(2E,4E)-Hexa-2,4-dien-1-ol is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Taltobulin intermediate-3 is an intermediate in the synthesis of Taltobulin (HY-15584). Taltobulin is a common toxin component in ADC preparation (ADC Cytotoxin), and it is also a powerful tubulin (Microtubule/Tubulin) inhibitor. Taltobulin disrupts tubulin polymerization, induces mitotic arrest, and induces apoptosis[1].
Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH (Compound 21b) is an EZH2 degrader and can be used for the research of lymphoma[1].
(E)-Masticadienonic acid is a triterpene, can be isolated from the Vallesia glabra[1].
Boc-Glu(OBzl)-Ala-Arg-AMC 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].
CAM833 (CAM-833) is a potent, specific chemical inhibitor of the RAD51-BRCA2 interaction and RAD51 oligomerization with Kd of 366 nM;CAM833 inhibited RAD51 foci formation 6 h after exposure to 3 Gy IR, in a concentration-dependent manner with an IC50 of 6 uM, causeed a concentration-dependent decrease in RAD51 foci accompanied by increased DNA damage in A549 cells.CAM833 inhibted RAD51 molecular clustering at DNA damage sites visualized by SMLM, suppressed homologous recombination and potentiated cell-cycle arrest.CAM833 potentiated the growth suppressive effect of PARP1 inhibition in BRCA2 wild-type cells, as well as dose-dependent growth inhibition when combined with ionizing radiation.
Phytochelatin 4 (PC 4) is a short Cys-rich peptide with repeating γ-Glu-Cys motifs found in plants[1].
6-Mercaptopurine hydrate is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive drug.
SHP099 hydrochloride is a potent, selective and orally available SHP2 inhibitor with an IC50 of 70 nM.
Emixustat, a novel visual cycle modulator, is an inhibitor of the visual cycle isomerase with an IC50 value of 4.4 nM in vitro.
HAP-1 is a synovial-targeted transduction peptide. HAP-1 facilitates specific internalization of protein complexes into human and rabbit synovial cells. HAP-1 fused to an antimicrobial peptide, (KLAK)2, to generate a proapoptotic peptide DP2[1].
LM-4108 (N-(2-Phenylethyl)-indomethacin amide) is a selective and orally active COX-2 inhibitor with an IC50 of 0.06 μM for purified human COX-2. LM-4108 shows anti-inflammatory activity and may be effective in prevention of cancer. Half-lives for the disappearance of 10 μM LM-4108 in rat, human, and mouse liver microsomes were 11 min, 21 min, and 51 min, respectively[1].
Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone[1]. Cyclo(his-pro) TFA could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) TFA can cross the brain-blood-barrier and affect diverse inflammatory and stress responses[2].
DTNB(Ellman’s Reag) is a chemical used to quantify the number or concentration of thiol groups in a sample; can be used for measuring low-molecular mass thiols such as glutathione in both pure solutions and biological samples, such as blood.
1-Pyrenesulfonic acid sodium salt is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
BML-278 is a SIRT1 activator (EC150: 1 μM). BML-278 increases H3K9 methylation and inhibits H3K9 acetylation in both the paternal and maternal pronucleus. BML-278 improves early embryonic development. BML-278 arrests the cell cycle at the G1/S phase, and reduces senescence in primary human mesenchymal cells. BML-278 reduces tubulin acetylation in U937 cells. BML-278 also increases mitochondrial density in murine C2C12 myoblasts[1][2].
Fluroxypyr-meptyl (Fluroxypyr-1-methylheptyl ester), a synthetical phytohormone, is used as herbicide agent[1][2].
Sutidiazine (ZY-19489) is an orally active and antimalarial agent. Sutidiazine inhibits parasitemia-induced infection. Sutidiazine shows short half-lives (approximately 7 h) and an exposure effect[1].
DODMA, a cationic lipid, is used for the preparation of liposomes. DOTMA is an effective gene transfection agent in vitro and in vivo.
SOS1-IN-4 is a potent SOS1 inhibitor with an IC50 of 56 nM for KRAS-C12C/SOS1 interaction (WO2021228028 A1, example 65)[1].
Flumorph(SYP-L190) is a carboxylic acid amide (CAA) fungicide.IC50 value:Target: Fungicide agentFlumorph did not inhibit the synthesis of cell wall materials, but disturbed the polar deposition of newly synthesized cell wall materials during cystospore germination and hyphal growth. In flumorph-treated hyphae, the most characteristic change was the development of periodic swelling ("beaded" morphology) and the disruption of tip growth. Upon removing flumorph, normal tip growth and organized F-actin were observed again [1]. Flumorph had induced systemic genotoxicity in mammals as it caused DNA damage in all tested vital organs, especially in brain and spleen [2].
Dyclonine is an oral anaesthetic found in Sucrets, an over the counter throat lozenge.Target: Sodium ChannelDyclonine is an oral anaesthetic that is the active ingredient of Sucrets, an over the counter throat lozenge. It is also found in some varieties of the Cepacol sore throat spray. It is a local anesthetic, used topically as the hydrochloride salt. Dyclonine hydrochloride has been found to possess, in addition to its topical anesthetic properties, significant bactericidal and fungicidal activity. Self-sterilizing action manifested by preparations containing the drug was considerably enhanced upon the addition of chlorobutanol. Results of in vitro tests employing microorganisms commonly involved in local infections indicated that the two agents in combination act synergistically [1, 2].
Furamidine (DB75) is abisbenzamidine derivative and an antiparasite agent. Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also a selective and cell-permeable protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively)[1][2][3].
KKL-35 is a trans-translation tagging reaction inhibitor with an IC50 of 0.9 µM.
Trihexyphenidyl is a potent and selective M1 muscarinic receptor antagonist. Trihexyphenidyl shows anticholinergic activity, and can be used for Parkinson syndrome or dystonia research[1][2].