Apigenin triacetate is a metabolite of F. graminearum. Apigenin triacetate can be downregulated in F. graminearum by chitosan treatment. Apigenin triacetate derives from apigenin[1].
2-Amino-6-chloro-9-(3-deoxy-3-fluoro-beta-D-ribofuranosyl)-9H-purine ((2R,3S,4S,5R)-2-(2-Amino-6-chloro-9H-purin-9-yl)-4-fluoro-5-(hydroxymethyl)tetrahydrofuran-3-ol) 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].
APOBEC3G-IN-1 (MN136.0185) is a potent HIV inhibitor, targeting APOBEC3G[1].
Cdc7-IN-4 (compound I-C) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-C. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle[1].
Glibornuride is a blocker of ATP-sensitive K+ channels (KATP channel) with a pKi of 5.75[1]. Antidiabetic agent[2].
Z62954982 is a potent, specific Rac1 inhibitor, reduces the intracellular levels of Rac1-GTP in a concentration-dependent manner with IC50 of 12 uM, 4 times more effective than NSC23766 (IC50=50 uM); causes a concentration-dependent decrease in transendothelial electrical resistance (TER) in both HDMEC and HUVEC.
Antofloxacin is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin is a weak, reversible inhibitor of CYP1A2 for the treatment of infections caused by a diverse group of bacterial species[1][2][3].
Echothiopate iodide is a potent hBChE (human butyrylcholinesterase) inhibitor. Echothiopate iodide is a long-acting anticholinesterase agent. Echothiopate iodide can be used for glaucoma research[1][2].
Glepidotin B is a dihydroflavonol compound isolated from the extracts of American licorice, Glycyrrhiza lepidota (Leguminosae). Glepidotin B is an antimicrobial agent[1].
m-Se3 is a potent and selective c-MYC transcription inhibitor that can inhibit tumor growth and has anti-cancer activity[1].
FLT3-IN-16 is a potent FLT3 inhibitor with an IC50 of 1.1 μM. FLT3-IN-16 can be used for researching acute myeloid leukemia[1].
Helioxanthin 8-1 is an analogue of helioxanthin, exhibites significant in vitro anti-HBV/HCV/HSV-1/HIV activity with EC50 of >5/10/1.4/15 uM.IC50 value: >5/10/1.4/15 uM(HBV/HCV/HSV-1/HIV) [1]Target: Antiviral agentThe cyclic hydrazide 28(Helioxanthin 8-1) showed the most potent antiHBV activity among those helioxanthin analogues tested. In addition, compound 28 exhibited moderately potent activity against HIV. It would therefore be promising to study helioxanthin analogues that contain a six-membered ring instead of the five-membered ring found in the lactam [1]. 8-1 exhibited effective inhibition on DHBV replication. The combination of 8-1 with 3TC resulted in additional anti-DHBV activity. Viral induced cells displayed higher susceptibility to 8-1 treatment than non-induced cells. HBV X protein might not be an essential factor in the initiation of the biological activity of 8-1, as demonstrated by its absence in DHBV [2].
VIP (1-12), human, porcine, rat, ovine is a vasoactive intestinal peptide (VIP) fragment. VIP (1-12), human, porcine, rat, ovine is a ligand for the CD4 (T4)/human immunodeficiency virus receptor[1][2].
TAS0728 is a potent, selective, oral active, irreversible and covalent-binding HER2 inhibitor, binds to HER2 at C805, inhibits its kinase activity, with an IC50 of 13 nM. TAS0728 shows IC50s of 4.9, 8.5, 31, 65, 33, 25, 86 and 36 nM for BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and human HER2, respectively. TAS0728 also inhibits the phosphorylation of HER2, HER3, and downstream effectors, shows no obvious effect on EGFR. Antitumor activity[1].
Phe-Met-Arg-Phe amide trifluoroacetate is an activator of K+ current, with ED50 of 23 nM in the peptidergic caudodorsal neurons.
Nogapendekin alfa is a superagonist of IL-15. Nogapendekin alfa promotes the proliferation and viability of immune cells. Nogapendekin alfa combines with Inbakicept (HY-P99661) at a ratio of 2:1, to form ALT-803, an IL-15 cytokine antibody fusion protein. ALT-803 reduces tumor burden by activation of NK cells and CD8+ T cells[1].
Tpl2 Kinase Inhibitor 1 (Compound 1) is a potent and selective Tpl2 (COT kinase, MAP3K8) inhibitor, plays an important role in the regulation of the inflammatory response and the progression of some cancers[1].
3-Methylpyrazole is used as a nitrification inhibitor of nitrification in soil[1].
Fmoc-NH-PEG4-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
α-Cyanopyridine-d4 is the deuterium labeled α-Cyanopyridine[1].
Propargyl-PEG4-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-IAP PROTACs Ibrutinib (HY-10997)-based PROTAC 2 and an analogue PROTAC 3. PROTAC 3 causes BTK degradation with a DC50 of 200 nM in THP-1 cells[1].
Yohimbine is a potent and relatively nonselective alpha 2-adrenergicreceptor (AR) antagonist, with IC50 of 0.6 μM. IC50 value: 0.6 uM [1]Target: alpha 2-adrenergic receptorin vitro: Yohimbine inhibits alpha2-receptor antagonist with Ki of 1.05 nM, 1.19 nM, and 1.19 nM for α2A, α2B, α2C, respectively. Yohimbine also inhibits 5-HT1B with Ki of 19.9 nM. Yohimbine acts to block the lowering of cAMP by alpha-2 adrenoceptor agonists. yohimbine actually causes a pronounced lowering of tyrosinase activity. [3]in vivo: Yohimbine is an antagonist at alpha2-noradrenaline receptors with putative panicogenic effects in human subjects, was administered to Swiss-Webster mice at doses of 0.5, 1.0, and 2.0 mg/kg. Yohimbine potentiates active defensive responses to threatening stimuli in Swiss-Webster mice.[2]
CCI-006 is a selective inhibitor and chemosensitizer of MLL-rearranged leukemia cells, by inhibits mitochondrial respiration resulting in insurmountable mitochondrial depolarization and a pro-apoptotic unfolded protein response (UPR) in a subset of MLL-r leukemia cells[1].
Carbaryl-d3 is the deuterium labeled N6-(carboxymethyl)-L-lysine[1].
LY 292728 is a potent leukotriene B4 (LTB4) receptor antagonist. LY 292728 binds to human neutrophils with a Ki of 0.47 nM and binds to guinea pig lung membranes with a Ki of 0.04 nM[1].
Arctigenin is a lignan found in certain plants of the Asteraceae; it has shown antiviral and anticancer effects in glass; it is the aglycone of arctiin.IC50 value: Target: anticancer agentArctiin and its aglucone, arctigenin from the fruits of Arctium lappa L. showed potent in vitro antiviral activities against influenza A virus (A/NWS/33, H1N1) (IFV). Based on the data from time-of-addition experiments and on release tests of progeny viruses, arctigenin was assumed to interfere with early event(s) of viral replication after viral penetration into cells, and to suppress the release of progeny viruses from the host cells [1]. arctigenin treatment reduced viability of bladder cancer T24 cells in a dose- and time-dependent manner after treatment with arctigenin (10, 20, 40, 80, and 100 μmol/L) for 24 hr and 48 hr. Arctigenin treatment clearly arrested tumor cells in the G1 phase of the cell cycle. At the molecular level, arctigenin treatment decreased cyclin D1 expression, whereas CDK4 and CDK6 expression levels were unaffected. Moreover, arctigenin selectively altered the phosphorylation of members of the MAPK superfamily, decreasing phosphorylation of ERK1/2 and activated phosphorylation of p38 significantly in a dose-dependent manner [2]. The use of arctigenin has been shown to be effective in a mouse model of Japanese encephalitis [3].
WAY-181187 (SAX-187) oxalate is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY-181187 oxalate mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist[1][2].