2-Hydroxy-4-methoxybenzaldehyde, a chemical compound and an isomer of Vanillin, could be used to synthesis Urolithin M7[1]. 2-hydroxy-4-methoxybenzaldehyde is a potent tyrosinase inhibitor from three East African medicinal plants, Mondia whitei, Rhus vulgaris Meikle, and Sclerocarya caffra Sond[2].
OTS193320 (OTS-193320) is a potent inhibitor of protein methyltransferase SUV39H2 with IC50 of 22.2 nM; significantly reduces global H3K9 tri-methylation (H3K9me3) in breast cancer cells in vitro and induces apoptotic cell death, attenuates γ-H2AX levels in combination with doxorubicin compared with the DOX treatment alone, and causes a significant reduction in breast cancer cell viability when compared to the treatment with a single agent; causes growth suppressive effect of SUV39H2-positive A549 lung cancer cells with IC50 of 0.38 uM.
Spinosyn A, a polyketide-derived macrolide produced by Saccharopolyspora spinosa, is a potent insecticide[1].
LH secretion antagonist 1 is an antagonist of luteinising hormone secretion, and may be used as an analgesic.
JHU-083 selectively blocks glutaminase activity in brain CD11b+ cells[1]. Blocking the function of glutaminase by the glutamine antagonist JHU-083 in experimental cerebral malaria (ECM) can result in a net decrease of glutamate levels in the animals[2].
Cyprodinil-13C6 is the 13C6 labeled Cyprodinil. Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC50s=0.44, 4.8, and 0.03 µM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC50=1.91 µM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC50=15.1 µM).
NNC-0640 is a potent human G-protein-coupled glucagon receptor (GCGR) negative allosteric modulator (NAM) with an IC50 of 69.2 nM[1].
DB0614 (Example 21) is a bifunctional compound targeted protein degradation of kinases. DB0614 degrades AAK1, AURKA, BMP2K, CAMKK1, CDK16, CML, CDK6, EIF2AK2, FER, GAK, LCK, LIMK2, MAP3KH, MAPK8, MAPK9, NEK9, PLK4, PTK2B, SIK2, STK17A, STK17B, ULK1, ULK3, and WEE1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity[1].
5’-Deoxy-5’-N-methylaminothymidine 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].
SMS2-IN-3 is a potent and selective SMS2inhibitor (IC50=2.2 nM), significantly reduces the hepatic SM (22:0) levels[1].
Coenzyme A sodium, a ubiquitous essential cofactor, is an acyl group carrier and carbonyl-activating group for the citric acid cycle and fatty acid metabolism. Coenzyme A plays a central role in the metabolism of carboxylic acids, including short- and long-chain fatty acids[1].
Ethylene-d4-diamine is the deuterium labeled Ethylene-diamine[1].
Flosequinan is a balanced vasodilator. Flosequinan not only significantly reduces systemic vascular resistance, but also significantly reduces the beating component of left ventricular afterload, characteristic impedance and arterial wave reflection, which can be used in the research of acute heart failure[1].
2-Iodoaniline (2-Iodophenylamine) is an aniline derivative, and has potential hepatotoxic and nephrotoxic activity[1].
EF24 is a curcumin analogue with greater anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK[1][2].
Ansamitocin P-3 is a microtubule inhibitor. Ansamitocin P-3 is a macrocyclic antitumor antibiotic.
N4-Amino-2'-C-methylcytidine 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].
VU0360172 is a potent and selective mGlu5 receptor positive allosteric modulator with an EC50 value of 16 nM and a Ki of 195 nM, respectively. VU0360172 stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice[1].
Z-Gly-Gly-Arg-AFC is a biological active peptide. (Plasminogen Activator Acrosine Substrate, fluorescent Z-Gly-Gly-Arg-AFC)
1,4-Chrysenequinone, a polycyclic aromatic quinone, acts as an activator of aryl hydrocarbon receptor (AhR).
WS-383 (WS383) is a highly potent, selective, and cellular active inhibitor of DCN1-UBC12 interaction with IC50 of 11 nM; inhibits Cul3/1 neddylation selectively over other cullins and also induces accumulation of p21, p27 and NRF2; exhibits cellular target engagement to DCN1 in MGC-803 cells, enhances the thermal stability of cellular DCN1 protein even at 1 uM
KDS2010 (KDS-2010, KDS 2010) is a potent, highly selective, reversible Monoamine oxidase-B (MAO-B) inhibitor with IC50 of 7.6 nM; displays 12,500-fold selectivity over MAO-A; shows a marked enantiomer selectivity (eightfold selectivity) over the (R)-isomer; significantly ameliorates the impairments in spike probability, learning, and memory in APP/PS1 mice, but not by selegiline, also reverses spatial learning and memory impairments in the Morris water maze test.
Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl- competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC50 of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain[1][2].
Sulfamethoxypyridazine is a long-acting sulfonamide antibiotic, for treatment of Dermatitis herpetiformis.
Molidustat (BAY 85-3934) is a novel inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with mean IC50 values of 480 nM for PHD1, 280 nM for PHD2, and 450 nM for PHD3.
Oseltamivir acid methyl ester is a precursor form of the neuraminidase inhibitor and antiviral oseltamivir acid. Oseltamivir acid methyl ester is converted to oseltamivir acid by carboxylesterase 1 (CES1) [1].
DPA-714 is a high affinity translocator protein (TSPO) ligand (Ki=7 nM), which is designed with a fluorine atom in its structure, allowing labelling with fluorine -18 and in vivo imaging using positron emission tomography. [18F]DPA-714 successfully evaluates for the specific imaging of inflammation in various models of neuroinflammation and in a brain tumor model[1][2].
NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively[1]. NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models[2].
Autophagy inducer 4 is a Magnolol-based Mannich base derivatives, which can be used as an anticancer agent. Autophagy inducer 4 suppresses cancer cells via inducing autophagy. Autophagy inducer 4 has 76-fold improvement in cytotoxicity against T47D cells compared with Magnolol. Autophagy inducer 4 also possesses suppressive effects on migration of T47D and Hela cancer cells[1].
Ac-LEHD-AMC is a fluorogenic substrate for caspase-9 (Excitation: 341 nm; Emission: 441 nm). Caspase-9 can induce hydrolysis of Ac-LEHD-AMC, resulting in the release of AMC fluorophore and its fluorescence can be used to quantify caspase-9 activity[1].