Tripterin (Celastrol) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
MCPG is a carboxylic phenyl glycine. MCPG can block metabotropic glutamate receptor (mGluR)(HY-15129) and has antagonistic activity of mGluR subtype. MCPG can be used to study the induction and maintenance of long-term potentiation (LTP) [1].
Loracarbef hydrate, a cephalosporin antibiotic, is an orally active second-generation synthetic beta-lactam antibiotic of the carbacephem class[1][2].
Rennin, also known as Chymosin, is a pepsin-related proteolytic enzyme synthesized by cells in the stomach of certain animals that efficiently converts liquid milk into a semi-solid, allowing it to remain in the stomach for longer. The natural substrate of Rennin is K-casein, which is specifically cleaved at the peptide bond between amino acid residues 105 and 106, phenylalanine and methionine, and is widely used in cheese production[1].
N2,N6-Bis(((9H-fluoren-9-yl)methoxy)carbonyl)-D-lysine is a lysine derivative[1].
QN523 is a novel scaffold with drug-like properties, showing potent in vitro cytotoxicity in a panel of 12 cancer cell lines. QN523 induces apoptosis and autophagy. QN523 can be used in research of cancer[1].
Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol), an analog of Bakuchiol (HY-N0235) isolated from Psoralea corylifolia (L.), is a potent monoamine transporter inhibitor. 13-Hydroxyisobakuchiol is more selective for the dopamine transporter (DAT) (IC50=0.58 μM) and norepinephrine transporter (NET) (IC50=0.69 μM) than for the serotonin transporter (SERT) (IC50=312.02 μM). 13-Hydroxyisobakuchiol has the potential for the research of disorders such as Parkinson's disease, depression, and cocaine addiction[1].
Omeprazole D3 is deuterium labeled Omeprazole, which is a proton pump inhibitor used in the treatment of dyspepsia.
4,5-Dioxodehydroasimilobine is an alkaloid, which can be isolated from the genus Houttuynia[1].
Saxagliptin(BMS477118) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM and Ki of 1.3 nM.IC50 value: 26 nM [1]Target: DPP4in vitro: Saxagliptin has an inhibition constant Ki of 1.3 nM for DPP4 inhibition, which is 10-fold more potent than either vildagliptin or sitagliptin (another two DPP4 inhibitors) with Ki of 13 and 18 nM. In addition, Saxagliptin demonstrates greater specificity for DPP4 than for either the DPP8 or DPP9 enzymes (400- and 75- fold, respectively). The active metablite of saxagliptin is two-fold less potent than the parent. Both Saxagliptin and its metabolite are highly selective (>4000-fold) for the prevention of DPP4 compared with a range of other proteases (selectivity of sitagliptin and vildagliptin for DPP4 is >2600 and <250-fold, respectively, compared with DPP8 and DPP9) [2]. Saxagliptin reduces the degradation of the incretin hormone glucagon-like peptide-1, thereby enhancing its actions, and is associated with improved β-cell function and suppression of glucagon secretion.in vivo: Saxagliptin is highly effective at eliciting marked dose-dependent enhancements in glucose clearance in the dose range 0.13-1.3 mg/kg in ob/ob mice relative to controls. Saxagliptin dose-dependently elevate plasma insulin significantly at 15 min post-oGTT, with concomitant improvement in the glucose clearance curves at 60 min post-oGTT [4].
L-372662 is a potent and orally active non-peptide oxytocin antagonist with a Ki value of 4.8. The Kd value of L-372662 for wild-type hOTR and [A318G]OTR is 5.8 nM and 73 nM. L-372662 shows selectivity to OTR:V1aR[1][2].
BMP-2 Epitope (73-92) is a biological active peptide. (This is amino acids 73 to 92 fragment of bone morphogenetic protein (BMP) knuckle epitope. It is a member of transforming growth factor beta (TGF-b). This peptide fragment is able to raise alkaline phosphate activity in murine multipotent mesenchymal cells.)
Anticancer agent 9, a glycine derivative, is an anticancer agent. Anticancer agent 9 can inhibit tumor cells viability of myelogenous leukemia and human prostate cancer[1].
SB-435495 hydrochloride is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM[1][3].
5-Nitro-1-(3-azido-3-deoxy-β-D-ribofuranosyl)-2(1H)-pyridinone 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].
1-Palmitoyl-sn-glycerol 3-phosphate (1-P-GPA) is an endogenous metabolite. 1-Palmitoyl-sn-glycerol 3-phosphate can be used for the research of non‐alcoholic fatty liver disease[1].
Tafluprost acid (AFP-172), an active metabolic form of Tafluprost, is a selective prostanoid FP receptor agonist. Tafluprost acid shows a high affinity for human prostanoid FP receptor with Ki and EC50 values of 0.4 nM and 0.53 nM, respectively. Tafluprost acid has 126 times weaker binding affinity for prostanoid EP3 receptor (IC50=67 nM) than for the prostanoid FP receptor. Tafluprost acid can be used in the research of glaucoma[1][2][3].
INT(Iodonitrotetrazolium chloride) is used in various dehydrogenase colorimetric analysis of the electron acceptor.
Rosthornin A is a ent-kaurene diterpenoid compound, isolated from the ether extract of the dried leaves of Rabdosia rosthornii[1].
Chlorpropham-d7 is the deuterium labeled Chlorpropham[1]. Chlorpropham is a carbamate herbicide and plant growth regulator. Chlorpropham inhibits mitosis and cell division by interfering with the organisation of the spindle microtubules[2][3].
ICMT-IN-2 (compound 45) is an inhibitor of ICMT (IC50=0.168 μM)[1].
Terrestrosin K, a steroidal saponin from Tribulus terrestris L., has potential to treat cardiovascular and cerebrovascular diseases[1].
HFI-419 is an insulin-regulated aminopeptidase (IRAP) inhibitor. HFI-419 has inhibitory potency for IRAP with Ki value of 0.48 μM. HFI-419 can be used for the research of cognitive and memory impairments such as Alzheimer's disease, brain trauma, and stroke[1].
Bufrolin is a Cromoglycate (histamine release inhibitor) analog and a high potency agonist of GPR35. Bufrolin promotes interactions between β-arrestin-2 and either human GPR35a or rat GPR35. Bufrolin also serves as antiallergic mast cell stabilizer and inhibit an anti-inflammatory response inducible by the internalization peptide. Bufrolin acts as an anti-inflammatory agent to be used in research of delivering pharmacol linked with internalization peptide[1][2][3].
(R)-CE3F4 is a potent and selective inhibitor of exchange protein directly activated by cAMP isoform 1 (Epac1), with an IC50 of 4.2 μM, with 10-fold selectivity for Epac1 over Epac2 (IC50, 44 μM). (R)-CE3F4 is more potent than racemic CE3F4 and (S)-CE3F4[1].
(E)-2,3-Dibromo-2-butenedioic acid is one of brominated haloacids, which are the drinking water disinfection byproducts (DBPs)[1].
(Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH (Surfagon, Mwt 1167.34 Da) is an agonist of gonadotropin-releasing hormone (GnRH). (Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH can be used as an internal standard for the LC-MS analysis of leuprorelide acetate. (Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH has potential applications in biochemical analysis and fertility[1][2][3].
MYC-IN-2 is a MYC protein-protein inhibitor. MYC-IN-2 can be used for the research of cancer[1].
Dehydroleucodine is a sesquiterpene lactone isolated from Gynoxys verrucosa. Dehydroleucodine is a mast cell stabilizer that inhibits tmast cell degranulation induced by compound 48/80. Dehydroleucodine inudces cells apoptosis, and has gastric ulcer inhibition and antileukemic effects[1][2][3].
PM050489 is an effective polyketone inhibitor of Microtubule/Tubulin that can be isolated from Madagascan sponge Lithoplocamia lithistoides. PM050489 inhibits mitosis with an IC50 value of 26.4 nM. PM050489 has antitumor activity and can be used in cancer research[1][2].