5'-O-DMT-PAC-dA can be used in the synthesis of oligoribonucleotides[1].
Nervogenic acid is an aromatic compound that can be isolated from Piper elongatum VAHL. Nervogenic acid has antibacterial activities and antioxidative effects[1].
m-PEG5-Tos is a derivative of silybin ethers, extracted from patent CN105037337A (compound III-c). m-PEG5-Tos is a PEG-based PROTAC linker can be used in the synthesis of Silymarin (HY-W043277)[1].
Dieckol, is a naturally occurring phlorotannin found in some brown algal species. Dieckol has anti-bacterial, anti-cancer, anti-oxidant, anti-aging, anti-diabetic, neuroprotective actions[1].
RO1138452 is a potent and selective IP (prostacyclin) receptor antagonist. RO1138452 displays high affinity for IP receptors. In human platelets, pKi is 9.3±0.1; in a recombinant IP receptor system, pKi is 8.7±0.06.
Bumadizone is a non-steroidal anti-inflammatory drug (NSAID) and can relieve pain[1].
SEN 12333 (WAY-317538) is a potent, selective and orally active α7 nAChR agonist. SEN12333 displays high affinity for the rat α7 nAChRs expressed in GH4C1 cells (K>i=260 nM) and acts as full agonist in functional Ca2+ flux studies (EC50=1.6 μM). SEN 12333 is used for AD and schizophrenia research[1].
VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively.
Hydroxylamine-d3 (hydrochloride) is the deuterium labeled Hydroxyamine hydrochloride[1]. Hydroxyamine hydrochloride is a selective monoamine oxidase (MAO) inhibitor used for inhibiting of platelet aggregation. Hydroxyamine hydrochloride is an intermediate of organic synthesis[2].
Thalidomide-O-C4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide (HY-14658) based cereblon ligand and a linker used in PROTAC technology.
AT-121 is a bifunctional nociception and mu opioid receptor agonist, with Kis of 3.67 and 16.49 nM, respectively. AT-121 is a safe, non-addictive analgesic, and shows antinociceptive and antiallodynic effects[1].
ML358 is a first in class, selective small molecule inhibitor of the SKN-1 pathway with IC50 of 0.24 uM; shows inactivity against Nrf2, the homologous mammalian detoxification pathway, and is not toxic to C. elegans (LC50 > 64 uM) and Fa2N-4 immortalized human hepatocytes (LC50 > 5.0 uM); sensitizes the model nematode C. elegans to oxidants and anthelmintics; exhibits good solubility, permeability, and chemical and metabolic stability in human and mouse liver microsomes; a valuable chemical probe to study regulation and function of SKN-1 in vivo.
DM1-SMe is an unconjugated form of the Maytansinoid in IMGN901. DM1-SMe is about 3-10-fold more potent than the parent drug Maytansine, with IC50s ranging from 0.003 to 0.01 nM for DM1-SMe in a panel of human tumor cell lines[1].
Halo-DBCO is a click chemistry reagent containing dibenzocyclooctyne (DBCO). Halo-DBCO can be used as a ligand to react with HaloTag to form covalent HaloTag ligand couples.
2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one is a natural product found in the leaves and stem bark of M. glabra. 2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one displays binding affinities with dipeptidyl peptidase-4 (DPP-4) and α-Amylase. 2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one has potential antidiabetic activities[1].
Gp100 (619-627) is amino acids 619 to 627 fragment of human melanoma antigen glycoprotein 100 (gp100). Gp100 has been a widely studied target for melanoma immunotherapy[1].
Guanidinosuccinic acid is a nitrogenous metabolite isolated in excess from serum and urine.
Ibuproxam (G 277) is a non-steroidal anti-inflammatory agent[1].
Methionine (MRX-1024) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
PBT 1033 (PBT 2) is an orally active copper/zinc ionophore. PBT 1033 restores cognition in mouse models of Alzheimer's disease (AD). PB 1033 also has antibacterial activity against Gram-positive bacteria[1][2].
m-PEG6-C6-phosphonic acid ethyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).IC50 value: 58 pM (Ki)Target: PDE1in vitro: ITI-214 exhibits picomolar inhibitory potency for PDE1, demonstrates excellent selectivity against all other PDE families. ITI214 exhibits excellent selectivity over other PDE familymembers. For instance, the Ki values of ITI214 against recombinant full-length human PDE1A, PDE1B, and PDE1C are 33 pM, 380 pM, and 35 pM, respectively. ITI214 is profiled in a panel of enzymes, receptors, transporters, and ion channels from Caliper at 10 μM, which is over 170000 times higher than its Ki for PDE1, and demonstrates good selectivity. [1]in vivo: ITI214 possesses a good overall profile with balanced physicochemical properties, excellent potency and selectivity, and good pharmacokinetics. ITI214 is found to significantly enhance memory performance in the test with a minimum effective dose of 3 mg/kg. [1]
CDK4/6-IN-2 is a potent CDK4 and CDK6 inhibitor extracted from patent US20180000819A1, Compound 1, has IC50s of 2.7 and 16 nM for CDK4 and CDK6, respectively[1].
Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities[1][2].
2-Chloro-N6-methyladenosine 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].
[Leu31,Pro34]-Neuropeptide Y(human,rat) is a specific neuropeptide Y Y1 receptor agonist. [Leu31,Pro34]-Neuropeptide Y(human,rat) slao inhibits Y4, Y5. [Leu31,Pro34]-Neuropeptide Y(human,rat) can increase blood pressure in anesthetized rats and increases food intake[1][2].
(-)-(S)-Cibenzoline (Escibenzoline), a S(+)-enantiomer of Cibenzoline, is an antiarrhythmic agent[1].
Thiodicarb is a carbamate insecticide used to control flies in animal and poultry houses and dairies. Thiodicarb is metabolized into methomyl in animals and plants, and subsequently degraded into carbon dioxide and acetonitrile[1].
Mulnitorsen is an antisense non-coding mitochondrial RNA (ASncmtRNA) synthesis reducer. Mulnitorsen is an antitumor agent[1].
TNH is a dimer that can enter living cells and recruit proteins into cellular structures[1].