STh, an Escherichia coli heat-stable toxin, is a 19 amino acid polypeptide encompassing three disulfide bridges. STh is an antigen of interest in the search for a broad coverage enterotoxigenic Escherichia coli (ETEC) vaccine[1].
3’-O-Acetyl-2’-deoxyuridine 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].
Ethyl 4-isocyanatobenzoate-d4 is the deuterium labeled Ethyl 4-isocyanatobenzoate[1].
BA 1 is a potent bombesin receptor agonist (IC50 values are 0.26, 1.55 and 2.52 nM for BB1, BB2 and BB3 respectively). BA 1 enhances glucose transport in obese and diabetic primary myocytes. BA 1 also stimulates NCI-H1299 lung cancer cell proliferation in vitro.
TAT-DEF-Elk-1 (TDE) is a cell-penetrating peptide inhibitor of Elk-1, mimics and specifically interferes with the DEF domain of Elk-1. TAT-DEF-Elk-1 blocks Elk-1 phosphorylation and prevents Elk-1 nuclear translocation without interfering with ERK nor MSK1 activation. TAT-DEF-Elk-1 is a useful tool to analyze the role of Elk-1 in this process during the development of neuronal plasticity[1].
MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6[1]. MJ33 has a critical effect on inflammatory brain damage[2].
Cucurbitacin B belongs to a class of highly oxidized tetracyclic triterpenoids; could repress cancer cell progression.IC50 value:Target: anticancer natural compoundin vitro: Cucurbitacin-B inhibited growth and modulated expression of cell-cycle regulators in SHSY5Y cells. At the molecular level, we found that Cucurbitacin-B inhibited AKT signaling activation through up-regulation of PTEN [1]. CuB induced apoptosis of A549 cells in a -concentration-dependent manner, as determined by fluorescence microscopy, flow cytometry and transmission electron microscopy. CuB dose-dependently inhibited lung cancer cell proliferation, with cell cycle inhibition and cyclin B1 downregulation. Apoptosis induced by CuB was shown to be associated with cytochrome c release, B-cell lymphoma 2 downregulation and signal transducer and activator of transcription 3 pathway inhibition [2]. CuB inhibited ITGA6 and ITGB4 (integrin α6 and integrin β4), which are overexpressed in breast cancer. Furthermore, CuB also induced the expression of major ITGB1and ITGB3, which are known to cause integrin-mediated cell death [3]. Cuc B treatment caused DNA double-strand breaks (DSBs) without affecting the signal transducer and activator of transcription 3 (STAT3), the potential molecular target for Cuc B. Cuc B triggers ATM-activated Chk1-Cdc25C-Cdk1, which could be reversed by both ATM siRNA and Chk1 siRNA. Cuc B also triggers ATM-activated p53-14-3-3-σ pathways, which could be reversed by ATM siRNA [4].in vivo: Efficacy of CuB was tested in vivo using two different orthotopic models of breast cancer. MDA-MB-231 and 4T-1 cells were injected orthotopically in the mammary fat pad of female athymic nude mice or BALB/c mice respectively. Our results showed that CuB administration inhibited MDA-MB-231 orthotopic tumors by 55%, and 4T-1 tumors by 40%. The 4T-1 cells represent stage IV breast cancer and form very aggressive tumors [3].
Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin inhibits PKC beta II with an IC50 of 5.9 nM[1][2].
[DPro10] Dynorphin A (1-11), porcine, a N-Alkylated derivative, is a potent κ-opioid receptor agonist with a Ki value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine has analgesic property[1][2].
NSD3-IN-3 is a potent NSD3 inhibtor with an IC50 value of 1.86 μM. NSD3-IN-3 has anticancer activity and significantly inhibits the growth and proliferation of non-small cell lung cancer cell line H460[1].
Sinococuline is a potent anti-dengue agent that is effective against all four serotypes of dengue virus (DENV). Sinococuline is also an effective tumor cell growth inhibitor[1][2].
Betanin has potent antioxidant and anti-inflammatory effect, that could inhibit peroxynitrite (ONOO-), with an IC50 of 19.2 μM. Betanin is a red glycoside obtained from beets that can be used as colorant.
KRAS inhibitor-18 (compound 3-10) is a potent KRAS G12C inhibitor with an IC50 of 4.74 µM. KRAS inhibitor-18 shows p-ERK inhibition activities with IC50s of 66.4, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-18 has the potential for the research of pancreatic, colorectal, and lung cancers[1].
Grepafloxacin (OPC-17116) hydrochloride is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin hydrochloride has high tissue penetration and a promising pharmacodynamic profile[1][2][3][4].
Adenosine antagonist-1 is an adenosine A3 receptor (AA3R) antagonist.
ERAP2-IN-1 (compound 61) is an uncompetitive ERAP2 inhibitor. ERAP2-IN-1 specifically inhibits the ERAP2 peptide hydrolysis activity, inhibiting Arg-AMC hydrolysis with an IC50 of 27 μM and model peptide hydrolysis with an IC50 of 44 μM[1].
Antiproliferative against-5 (compound 4o) can significantly and irreversibly inhibit proliferation of gastric cancer cells. Antiproliferative against-5 causes the G2/M phase arrest, and induces ROS accumulation and activation of autophagy. Antiproliferative against-5 can be used for researching anticancer[1].
RX 801077 hydrochloride (2 BFI) is a selective imidazoline I2 receptor (I2R) agonist with a Ki value of 70.1 nM. RX 801077 hydrochlorideshows anti-inflammation and neuroprotection. RX 801077 hydrochloride has the potential for the research of traumatic brain injury (TBI)[1][2].
ML 297 (VU 0456810) is a potent and selective GIRK1/2 activator, with an EC50 of 0.16 μM. ML 297 is potential for the treatment of epilepsy[1][2].
Ginkgolide J is a main constituent of the non-flavone fraction of Ginkgo biloba with an IC50 range of 12-54 µM, has neuroprotective and anti neuronal apoptotic ability[1][2].
Licarin A ((+)-Licarin A), a neolignan isolated from various plants, significantly and dose-dependently reduces TNF-α production (IC50=12.6±0.3 μM) in dinitrophenyl-human serum albumin (DNP-HSA)-stimulated RBL-2H3 cells. Anti-allergic effects. Licarin A reduces TNF-α and PGD2 production, and COX-2 expression[1]。
LMI070 (Branaplam) is a highly potent, selective and orally active small molecule SMN2 splicing modulator.
OM-1700 is a potent tankyrase inhibitor with IC50s of 127 and 14 nM for tankyrase 1 and tankyrase 2, respectively. OM-1700 reduces cell growth in the colon cancer cell line COLO 320DM (GI50=650 nM)[1].
(+)-Osbeckic acid is a vasorelaxatant that can be isolated from Tartary Buckwheat. (+)-Osbeckic acid has a potent vasorelaxant effect in Sprague-Dawley rat thoracic aorta rings with an EC50 of 887 μM[1].
NIDA-41020 is a potent and selective cannabinoid receptor 1(CB1) antagonist with a Ki of 4.1 nM. NIDA-41020 was designed as a potential radioligand for use in positron emission tomography (PET)[1].
Budiodarone (ATI-2042) is an analogue of Amiodarone (HY-14187) with a half-life of 7 h. Budiodarone inhibits sodium, potassium, and calcium ion channels. Budiodarone is an antiarrhythmic agent and can be used for the research of atrial fibrillation[1].
DMAPP (Dimethylallyl pyrophosphate) triammonium is an isoprenoid precursor. DMAPP triammonium, as an isomer of isopentenyl pyrophosphate (IPP), exists in virtually all life forms[1].
N3-D-Dab(Boc)-OH is a click chemistry reagent containing an Azide[1].
Triptonodiol can be isolated from Trypterygium wilfordii. Triptonodiol has anti-inflammatory and anti-cancer activity. Triptonodiol inhibits the biological activity of GSK[1][2].
20(S),24(R)-Ocotillol is isolated from Panax ginseng[1].