BADAN (6-Bromoacetyl-2-dimethylaminonaphthalene) is a polarity-sensitive fluorescent probe[1].
LY-272015 hydrochloride is an orally active, specific 5-HT2B receptor antagonist. LY-272015 hydrochloride completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 hydrochloride is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats[1][2].
Amino-PEG13-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
(rel)-Tivantinib is a potent and highly selective inhibitor of the receptor tyrosine kinase c-MET. (rel)-Tivantinib has two novel targets, GSK3α and GSK3β, which play an important role in the cellular mechanism of non-small cell lung cancer (NSCLC)[1].
Rosamultic acid is an A-ring contracted triterpene, that can be isolated from the roots of Rosa rnultiflora. Rosamultic acid inhibits gastric cancer cells proliferation by inducing Apoptosis mediated through cell cycle arrest, downregulation of cell cycle related protein expressions, inhibition of cell migration, DNA damage, and activation of caspases[1][2].
Thiorphan-d7 is the deuterium labeled Thiorphan[1]. Thiorphan is a selective NEP (neprilysin) inhibitor with an IC50 of 6.9 nM[2].
1-Phenyl-2-pyrrolidinone (1-Phenylpyrrolidin-2-one) is a phenyl analogue of GABA with sedative effect, decreasing the exploratory behavior of rats at 50-100 mg/kg (i.v.). 1-Phenyl-2-pyrrolidinone also has been proved to inhibit emotional reactions in dogs and cats. 1-Phenyl-2-pyrrolidinone induces decreases in the pressor reaction to emotional stress without accompanied by normalization of the function of baroreceptor reflexes[1][2].
Shionone is the major triterpenoid isolated from Aster tataricus, has anti-tussive, anti-inflammatory activities[1][2]. Shionone possesses a unique six-membered tetracyclic skeleton and 3-oxo-4-monomethyl structure[1].
Novaluron is a chemical with pesticide properties, belonging to the class of insecticides called insect growth regulators.
Pyrvinium pamoate is an FDA-approved antihelmintic drug that inhibits WNT pathway signaling.
(S,S)-Z-FA-FMK is a cell-permeable, irreversible cathepsin B inhibitor. (S,S)-Z-FA-FMK blocks LPS-induced production of IL-1α and IL-1β. (S,S)-Z-FA-FMK can be used as a negative control for caspase-1 and caspase-2 inhibitors because it lacks an aspartic acid residue at the P1 position[1][2].
Primidone is an anticonvulsant of the pyrimidinedione class.Target: GABA ReceptorPrimidone is an anticonvulsant of the pyrimidinedione class, the active metabolites of which, phenobarbital (minor) and phenylethylmalonamide (PEMA) (major), are also anticonvulsants. It is believed to work via interactions with voltage-gated sodium channels which inhibit high-frequency repetitive firing of action potentials [1]. The effect of primidone in essential tremor is not mediated by PEMA.[76] The major metabolite, phenobarbital, is also a potent anticonvulsant in its own right and likely contributes to primidone's effects in many forms of epilepsy [2]. Primidone and the other enzyme-inducing anticonvulsants can cut the half-life of antipyrine roughly in half (6.2 ± 1.9 h vs. 11.2 ± 4.2 h), and increases the clearance rate by almost 70%. Phenobarbital reduces the half-life to 4.8 ± 1.3 and increases the clearance by almost 109% [3].
Thapsigargin is an inhibitor of microsomal Ca2+-ATPase.
Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (5-HT2C) receptor-selective agonist with an EC50 of 8 nM.
Thiol-C10-amide-PEG8 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35) agonist with an EC50 of 5.8 nM, displays good druggability[1].
Salinomycin is an anticoccidial drug with potent anti-bacterial activity and an novel anticancer agent targeting human cancer stem cells.
LC kinetic stabilizer-2 is a potent amyloidogenic immunoglobulin light chain (LC) kinetic stabilizer with an EC50 of 24 nM[1].
Bcl-2-IN-10 is an active Bcl-2 inhibitor that can release up to four nitric oxide (NO) molecules. Bcl-2-IN-10 has cytotoxic activities against cancer cells, such as human leukemia, breast cancer and lung cancer. Bcl-2-IN-10 induces cell apopotosis and arrest cell cycle of G2/M phase, and can be used in cancer-related research[1].
FAPI-34 is a fibroblast-activating protein (FAP) inhibitor with favorable pharmacokinetic and biochemical properties. (patent WO2019154886A1).
PR-104 (sodium) is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104 (sodium), as a nitrogen mustard pre-prodrug, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A[1].
Oxonic acid potassium salt is an inhibitor of uricase, oxonic inhibits the phosphorylation of 5-FU to 5-fluorouridine-5'-monophosphate catalyzed by pyrimidine phosphoribosyl-transferase in a different manner from allopurinol in cell-free extracts and intact cells in vitro.IC50 value: Target: On p.o. administration of 5-FU (2 mg/kg) and a potent inhibitor of 5-FU degradation to Yoshida sarcoma-bearing rats, oxonic acid (10 mg/kg) was found to inhibit the formation of 5-fluorouridine-5'-monophosphate from 5-FU and its subsequent incorporation into the RNA fractions of small and large intestine but not of tumor and bone marrow tissues [1]. Oxonic acid diet increased plasma uric acid by 80-90 micromol/l, while blood pressure was elevated only in hyperuricemic 5/6 nephrectomy rats (18 mmHg) [2].
JNJ-42041935 is a potent, competitive and selective inhibitor of prolyl hydroxylase PHD; inhibits PHD1, PHD2, and PHD3 with pKi values of 7.91±0.04, 7.29 ±0.05, and 7.65±0.09, respectively.
Phenylacetylglutamine-D5 (NSC 203800-D5;Phenylacetyl-L-glutamine-D5) is a deuterated form of Phenylacetylglutamine. Phenylacetylglutamine is a colonic microbial metabolite from amino acid fermentation[1].
Biotin-C1-PEG3-C3-amine (TFA) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Heptylbenzene-d5 is the deuterium labeled Heptylbenzene[1].
S-(+)-Arundic Acid ((S)ONO-2506) is the S-enantiomer of Arundic Acid. Arundic acid is an astrocyte-modulating agent, has the potential for stroke and Alzheimer’s disease research[1].
Fmoc-NH-PEG8-CH2CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Thalidomide-4-NH-PEG2-COO(t-Bu) is a t-Bu modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The t-Bu protecting group at the end of Thalidomide-4-NH-PEG2-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-4-NH-PEG2-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
3’,5’-Di-O-benzoyl-2’-deoxy-2’-fluoro-3-Deaza-arabinouridine 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].