Propargyl-PEG3-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
PCSK9 modulator-4 (Compound 21) is a potent modulator of PCSK9 with an EC50 value of 0.15 nM. PCSK9 is a recently validated target for lowering low-density lipoprotein cholesterol (LDL-C). PCSK9 modulator-4 has the potential for the research of hyperlipidemia[1].
PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy[1][2][3].
6bK is a potent and selective insulin degrading enzyme (IDE) inhibitor with an IC50 value of 50 nM. 6bK increases circulating insulin in high-fat-fed mice. Acute administration of 6bK enhances glucose tolerance to oral glucose, notably to a greater extent in high-fat-fed mice[1].
N-(Azido-PEG2)-N-Boc-PEG3-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Sacrosidase is a yeast-derived enzyme that facilitates sucrose digestion. Sacrosidase has the potential for congenital sucrase-isomaltase (SI) deficiency research[1].
Lysophosphatidylcholines are a class of chemical compounds which are derived from phosphatidylcholines. Lysophosphatidylcholine is produced from phospholipids by the action of phospholipase A2 (PLA2). Lysophosphatidylcholine plays critical role in allergic airway disease manifestation[1].
Galanin (2-29) (rat) inhibits rat pancreatic protein and CCK-8-stimulated amylase secretion. Galanin (2-29) (rat) is an GAL2R agonist (Ki: 3.5 nM)[1][2].
SAP6 is a biological active peptide. (inhibited virus entry into the cells)
EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis[1].
Demethylcarolignan E is a phenylpropanoid ester that can be isolated from the stems of Hibiscus taiwanensi. Demethylcarolignan E has cytotoxicity against human cancer lines A549 and MCF-7 (IC50: <10 μg/mL)[1].
Mitiglinide(KAD-1229; S21403) is a drug for the treatment of type 2 diabetes; it is a highly selective KATP channel antagonist. IC50 value:Target: KATP channelMitiglinide is a hypoglycemic agent that closes adenosine triphosphate (ATP)-sensitive potassium channels (KATP channel s) in the pancreatic β-islet cells. Mitiglinide stimulates insulin secretion by stimulating Ca2+ influx.
L-Azidonorleucine hydrochloride, an unnatural amino acid, is A Methionine surrogate. L-Azidonorleucine hydrochloride can be used to label mammalian cell proteins and identify a diverse set of methionyl-tRNA synthetase (MetRS) mutants [1][2].
Alimemazine hemitartrate is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.
MeBIO is a potent AhR (aryl hydrocarbon receptor) agonist, with IC50 of 44 μM (GSK-3) and 55 μM (CDK1/cyclin B), respectively. MeBIO is inactive on GSK-3β[1].
2-Cyanomethylthioadenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
PSTi8 is a biological active peptide. (Pancreastatin inhibitor 8)
CC-3060 is a Cereblon modulator that promotes ZBTB16 degradation. CC-3060 degrades ZBTB16 with a DC50 of 0.47 nM in HT-1080 cells. CC-3060 targets ZBTB16 for degradation by primarily engaging distinct structural degrons on different zinc finger domains[1].
WX-081, an anti-tuberculosis agent, displays excellent anti-mycobacterial activity against M. tuberculosis H37Rv and low cytotoxicity. WX-081 exhibits potent activity with MIC50s of 0.083 and 0.11 μg/mL for drug susceptible tuberculosis (DS-TB) and multidrug resistant tuberculosis (MDR-TB) strains. WX-081 also inhibits hERG channel with the IC50 of 1.89 μM[1].
Psoromic acid is a potent and selective RabGGTase (Rab geranylgeranyl transferase) inhibitor with an IC50 value of 1.3 µM. Psoromic acid is an antioxidative agent. Psoromic acid exhibits a competitive type of HMGR inhibition and mixed type of ACE (angiotensin converting enzyme) inhibition[1][2].
Mizolastine dihydrochloride is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions. Target: Histamine H1-receptorMizolastine is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions. It does not prevent the actual release of histamine from mast cells, just prevents it binding to receptors. Side effects can include dry mouth and throat.Mizolastine has demonstrated antiallergic effects in animals and healthy volunteers and anti-inflammatory activity in animal models. Double-blind trials have shown mizolastine to be significantly more effective than placebo and as effective as other second generation antihistamine agents, such as loratadine or cetirizine, in the management of patients with perennial or seasonal allergic rhinitis and in patients with chronic idiopathic urticaria. Available data also suggest that prophylactic administration of mizolastine is significantly more effective than placebo and as effective as prophylactic terfenadine in delaying the onset of symptoms of seasonal allergic rhinitis.
GpTx-1 is a potent, selective, 34-residue peptide antagonist of Nav1.7 sodium channel with IC50 of 10 nM, displays 20- and 1000- fold selectivity over NaV1.4 and NaV1.5.
Mogroside III A2 is a cucurbitane glycoside. Mogroside III A2 can inhibit Epstein-Barr virus early antigen (EBV-EA) activation. Mogroside III A2 shows weak inhibitory effects on activation of NOR 1[1].
Trimebutine-d5 (fumarate) is deuterium labeled Trimebutine.
Carglumic acid, a functional analogue of N-acetylglutamate (NAG) and a carbamoyl phosphate synthetase 1 (CPS1) activator, is used to treat acute and chronic hyperammonemia associated with NAG synthase (NAGS) deficiency.
Quinfamide is an antiamebic agent. Quinfamide can be used to treat tropical parasitic infections such as Amoebiasis and Helminthiasis[1].
Anethole is a type of aromatic compound that occurs widely in nature, widely used as a flavoring substance.
Thymus factor X is a biologically active polypeptide which can be used as a natural stimulator of lymphocyte function.
FAK-IN-9 (Compound 8f) is a potent and orally active FAK inhibitor with an IC50 of 27.44 nM. FAK-IN-9 induces triple-negative breast cancer (TNBC) cell apoptosis[1].
[8]-Shogaol, one of the pungent phenolic compounds in ginger, exhibits anti-platelet activity (IC50=5 μM) and inhibits COX-2 (IC50=17.5 μM). [8]-Shogaol induces apoptosis in human leukemia cells[1][2][3][4].