3-Hydroxy-3-(4-hydroxyphenyl)-lactic acid is a key metabolite in the P. roqueforti fermentation approach, with quantitative data of 10.2 ± 1.1 µM in Tyr1 (presence of L-tyrosine) of [1].
Glecaprevir is a novel HCV NS3/4A protease inhibitor, with IC50 values ranging from 3.5 to 11.3 nM.
Trx-red (NBL-SS perchlorate) is a red-emitting fluorescent probe derivatized from the nile blue fluorophore. Trx-red is used for selectively imaging thioredoxin (Trx) in live cells and in vivo (λex=615 nm, λem=661 nm)[1].
MPG peptides, Pβ is a primary amphiphilic peptide consisting of three domains[1].
Boc-(S)-α-benzyl-Pro-OH is a proline derivative[1].
Gatralimab (GZ-402668) is an IgG1 anti-CD52 monoclonal antibody[1].
Vibozilimod (example 33) is a S1p1 receptor agonist (extracted from patent WO2012140020A1)[1].
Tubulin inhibitor 26 (compound 3c) is a potent inhibitor of tubulin. Tubulin inhibitor 26 is an indazole derivative compound. Tubulin inhibitor 26 shows noteworthy low nanomolar potency against HepG2, HCT116, SW620, HT29 and A549 cancer cell lines. Tubulin inhibitor 26 arrests tumor cell in G2/M phase and induced cell apoptosis. Tubulin inhibitor 26 suppresses tumor growth in vivo without affecting the mice body weight[1].
E7449 is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ∼50 and ∼50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate.
Ivachtin (Caspase-3 Inhibitor VII; compound 7a) is a nonpeptide, noncompetitive and reversibl caspase-3 inhibitor with an IC50 of 23 nM. Ivachtin has modest selectivity for the remaining caspases[1].
Valecobulin hydrochloride (CKD-516 hydrochloride) is a valine prodrug of S516 (HY-130233) and a vascular disrupting agent (VDA). Valecobulin hydrochloride is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors[1][2].
Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis treatment[1].
Boc-Glu-OtBu is a glutamic acid derivative[1].
Pirfenidone D5 (AMR69 D5) is a deuterium labeled Pirfenidone. Pirfenidone is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities[1][2][3].
Nidanilimab (CAN04) is a fully humanized monoclonal anti-IL1RAP antibody with a Kd value of 1.10 pM. Nidanilimab blocks IL1α and IL1β signaling and stimulates the immune system to destroy tumour cells. Nidanilimab can be used in research of non-small lung cancer (NSCLC) and pancreatic ductal adenocarcinoma (PDAC) [1][2].
MESG is a chromophoric substrate which can be used for the quantitation of inorganic phosphate.
Pirinixil is a hypolipidemic agent of low toxicity.
Aplodan is an antiischemic and antiarrhythmic agent. Aplodan has a protective action on cell membrane. Aplodan has the potential for the research of ischemic heart or ischemic heart disease with persistent ventricular premature beats (VPB) [1][2].
Thymohydroquinone is a monoterpene molecule. Thymohydroquinone has antioxidant and anti-inflammatory properties. Thymohydroquinone can be used for pharmacokinetic studies and regulatory toxicity studies [1].
H-Trp-Met-OH is a biologically active peptide.
Phenytoin is an inactive voltage-gated sodium channel stabilizer.Target: Sodium ChannelPhenytoin is an antiepileptic drug. It is useful to treat partial seizures and generalized tonic-clonic seizures but not primary generalized seizures such as absence seizures or myoclonic seizures. Phenytoin is believed to protect against seizures by causing voltage-dependent block of voltage-gated sodium channels [1]. Phenytoin has low affinity for resting sodium channels at hyperpolarized membrane potentials [2]. When neurons are depolarized and the channels transition into the open and inactivated states, greater binding and block occur. The inhibitory potency is strongly use dependent, so that block accumulates with prolonged or repetitive activation, such as occurs during a seizure discharge. The blocking of sodium channels by phenytoin is of slow onset. The time course of fast sodium currents is therefore not altered in the presence of the drug and action potentials evoked by synaptic depolarizations of ordinary duration are not blocked. Thus phenytoin is able to selectively inhibit pathological hyperexcitability in epilepsy without unduly impairing ongoing activity. Phenytoin also blocks persistent sodium current and this may be of particular importance in seizure control. Phenytoin is a class 1b antiarrhythmic [3].
1,2,3,7-Tetramethoxyxanthone is a xanthone isolated from Polygala tenuifolia[1].
Urolithin D is competitive and reversible antagonist of EphA receptors. Urolithin D exhibits intra-classes selectivity[1].
5-hydroxy-1-tetralone can be used as a fluorescent labeling reagent for the determination of glycosphingolipid from biological samples[1].
Boc-D-Thr(Bzl)-OH is a threonine derivative[1].
Benzenepentacarboxylic acid (BA), a novel fluorescent probeas to detect and scavenge HO-.A specific and reproducible fluorescent probe of HO- developed is utilized to prove and detect the generation of HO- in H2O2/TAED and H2O2/TBCC alkali systems.
ABT-072 (potassium trihydrate) is an orally active and potent non-nucleoside HCV NS5B polymerase inhibitor (HCV GT1a EC50=1 nM; HCV GT1b EC50=0.3 nM)[1][2][3].
4-Aminosalicylic acid hemicalcium is an orally active antibiotic and has the potential for tuberculosis research[1].
GSK4028 is the enantiomeric negative control of GSK4027, which is a PCAF/GCN5 bromodomain chemical probe, the pIC50 of GSK4028 is 4.9 in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) (Free Fatty Acid Receptor) agonist with a pEC50 of 7.39. TUG-499 exhibits >100-fold selectivity over the related receptors FFA2, FFA3, and the nuclear receptor PPARγ and other diverse receptors, ion channels, and transporters. TUG-499 can be used for the research of type 2 diabetes[1].