Tegobuvir is a specific, covalent inhibitor of the HCV NS5B polymerase.
1-Naphthyl acetate is an attractive chromogenic substrate for the detection of erythrocyte acetylcholinesterase (AChE) activity. 1-Naphthyl acetate has the potential to detect organophosphorus pesticide (OP) poisoning[1].
(S)-2-Amino-3-(2-hydroxyphenyl)propanoic acid hydrochloride is a phenylalanine derivative[1].
Herbacetin 3,8-O-diglucoside (Herbacetin di-glucoside) is a flavonol compound that can be found in flax seeds[1].
BAY-252 is a potent branched-chain amino acid transaminases 1 (BCAT1) and BCAT2 inhibitor with IC50s of 2 μM and 2 μM, respectively. BAY-069 also can be used as a chemical probe. BAY-069 can be used for the research of cancer[1].
GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy, with an IC50 of 4.9 nM[1].
JTV-519 free base (K201 free base) is a Ca2+-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Cardioprotective agent[1].
FLT3-IN-3 is a potent FLT3 inhibitor with IC50s of 13 and 8 nM for FLT3 WT and FLT3 D835Y, respectively.
DL-Aspartic acid dimethyl ester hydrochloride is an aspartic acid derivative[1].
Casticin is a methyoxylated flavonol isolated from Viticis Fructus, with antimitotic and anti-inflammatory effect. Casticin inhibits the activation of STAT3.
STING agonist-27 (CF509) is a non-nucleotide small-molecule STING agonist. STING agonist-23 activates STING, exhibits activity against SARS-CoV series strains[1].
CGP 25454A is a novel and selective presynaptic dopamine autoreceptor antagonist. In vitro: CGP 25454A increase the field-stimulated [3H]- and [14C]-overflow from rat striatal slices preloaded with [3H]dopamine and [14C]choline, indicating that CGP 25454A is able to enhance the release of both dopamine (DA) and acetylcholine (ACh). However, CGP 25454A is 12.9 times more potent in increasing, by 1/6 of the apparent maximal increase, the release of [3H]DA than that of [14C]ACh.In vivo: CGP 25454A increase [3H]spiperone binding to receptors of the D2 family in rat striatum by 90-110% (ED50: 13 mg/kg i.p.). As a similar increase in [3H]spiperone binding is found with a variety of agents which increase the synaptic concentration of endogenous DA, the effect of CGP 25454A most probably reflects an enhanced release of DA under in vivo conditions. At 30-100 mg/kg, CGP 25454A inhibit [3H]spiperone binding in the pituitary of the same animals as a result of a blockade of postsynaptic DA receptors.
Calpurbatug is an immunoglobulin G1 antibody. Calpurbatug has activity with anti-bacterial DNA-binding protein DNABII family and anti-human monoclonal TRL1068 γ1-chain[1].
Ibuprofen-13C,d3 is the 13C- and deuterium labeled. Ibuprofen is an anti-inflammatory agent targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
Nisevokitug (NIS-793) is a human, IgG2λ antibody targeting TGF-β (TGFB1/TGFB2). Nisevokitug is expressed by CHO-K1 cells[1].
3'-Deoxy-3'-amino-ATP, an ATP analogue, is a potent and competitive inhibitor of ATP, with a Ki of 2.3 μM. 3'-Deoxy-3'-amino-ATP can be used to synthesis of 3′-Amino-3′-deoxy transfer RNA by incorporation into the 3' terminus of tRNA-C-C[1][2].
ONO-8711 is a potent and selective competitive antagonist of EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1 respectively). ONO-8711 effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer[1].
E3 ligase Ligand 9 is a Ligand of BETd-260 for E3 Ligase used in PROTAC. BETd-260 is a potent BET degrader based on PROTAC technology, with an IC50 of 51 pM against BRD4 protein in RS4;11 leukemia cell line[1].
Octadeca-9,12-dienamide is an endogenous lipid[1].
Cocoa butter can be used as an excipient, such as lubricants, suppository bases. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs[1].
SIRT5 inhibitor 4 (compound 11) is a potent, selective SIRT5 inhibitor with IC50 values of 26.4 and >400μM for SIRT5 and other SIRT subtype, respectively[1].
L-Aspartic acid is is an amino acid, shown to be a suitable prodrug for colon-specific drug deliverly.
Protodioscin, a major steroidal saponin in dioscoreae rhizome, has been shown to exhibit multiple biological actions, such as anti-hyperlipidemia, anti-cancer, sexual effects and cardiovascular properties.
MMSET-IN-1 is a multiple myeloma SET domain (MMSET, aka NSD2/WHSC1) inhibitor against SETD2 and MMSET with IC50s of 0.49 and 3.3 μM, respectively. MMSET-IN-1 has a Kd of 1.6 μM for MMSET[1].
Palmitic acid-d2-1 is the deuterium labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
Sperm motility agonist-1 (compound 745) is a Sperm motility agonist. Sperm motility agonist-1 can be used in studies of infertility and enhancement of fertility[1].
HDAC-IN-38 (compound 13) is a potent HDAC inhibitor. HDAC-IN-38 shows similar micro-molar inhibitory activity toward HDAC1, 2, 3, 5, 6, and 8. HDAC-IN-38 increases cerebral blood flow (CBF), attenuates cognitive impairment, and improves hippocampal atrophy. HDAC-IN-38 also increases the level of histone acetylation (H3K14 or H4K5)[1].
Cipargamin (NITD609) is an potent antimalarial compound, with IC50 of appr 1 nM against P. falciparum.
[Deglycinamide9, Arginine8]-Vasopressin is a Vasopressin (HY-B1811) analog. [Deglycinamide9, Arginine8]-Vasopressin induces platelet aggregation. [Deglycinamide9, Arginine8]-Vasopressin has hemostatic effect[1].
Ponatinib (AP24534) hydrochloride is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively[1].