Pyridoxal phosphate is the active form of vitamin B6, acts as an inhibitor of reverse transcriptases, and is used for the treatment of tardive dyskinesia.
Uperolein is a physalaemin-like endecapeptide, produced in the skin of Uperoleia rugosa and Uperoleia marmorata. Uperolein has a spasmodic effect on both the gastrointestinal tract and longitudinal muscles[1][2][3].
Iferanserin (S-MPEC) is a selective 5-HT receptor (serotonin receptor) antagonist with an affinity for 5-HT2A receptor. Iferanserin has the potential for internal hemorrhoid disease treatment[1].
PHA-543613 is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki of 8.8 nM. PHA-543613 displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors[1]. PHA-543613 can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research[2].
Pteryxin, a coumarin in Peucedanum japonicum Thunb leaves, exerts antiobesity activity[1]. Pteryxin is a potent butyrylcholinesterase (BChE) inhibitor, with an IC50 of 12.96 μg/ml[2].
EZH2-IN-5 is a potent EZH2 inhibitor with IC50 values of 1.52 nM and 4.07 nM for wild-type and mutant Tyr641 EZH2, respectively[1].
(R)-2,3-Dihydroxypropanal-3-13C is the 13C labeled (R)-2,3-Dihydroxypropanal[1].
Rapanone is a natural benzoquinone. Rapanone exhibits a broad spectrum of biological actions, including anti-tumor, antioxidant, anti-inflammatory, antibacterial and antiparasitic. Rapanone also is a potent and selective human synovial PLA2 inhibitor, with an IC50 of 2.6 μM[1][2][3][4].
PF-06273340 is a potent, selective, orally bioavailable and peripherally restricted pan Trk inhibitor[1].
N-(3-Methoxybenzyl)Palmitamide is a promising inhibitor of FAAH for the treatment of pain, inflammation and CNS degenerative disorders[1].
Benzyl-PEG2-CH2-Boc is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
Bexmarilimab (FP-1305) is a potent humanized anti-CLEVER-1 IgG4-antibody with an IC50 value of 4.51 nM. Bexmarilimab is capable of inducing a phenotypic M2 to M1 immune switch of tumor-associated macrophages. Bexmarilimab can be used in research of cancer[1].
2-Cyanopyrimidine is a potent and non-selective cysteine protease cathepsin K inhibitor with an IC50 of 170 nM. 2-Cyanopyrimidine is used for osteoporos[1].
(Cys47)-HIV-1 tat Protein (47-57) has membrane translocation function and can be used to derivatize the surface of magnetic pharmaceuticals and substantially facilitated their uptake into target cells[1][2].
Gypenoside XLIX, a dammarane-type glycoside, is a prominent component of G. pentaphyllum. Gypenoside XLIX is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator and inhibits cytokine-induced vascular cell adhesion molecule-1 (VCAM-1) overexpression and hyperactivity in human endothelial cells[1].
Enpp-1-IN-19 (compound 29f) is an orally active ENPP1 inhibitor that inhibits cGAMP hydrolysis by ENPP1 (IC50=68 nM). Enpp-1-IN-19 increases anti-PD-L1 responses and inhibits tumor growth in CT26 syngeneic models. Enpp-1-IN-19 also enhances STING-mediated type I interferon responses, induces immune memory, and prevents tumor recurrence[1].
Midaglizole ((±)-DG5128 free base, DG5128 free base) is a potent α2-adrenoceptor antagonist. Midaglizole is a hypoglycemic agent. Midaglizole increases blood pressure and reduces blood glucose levels in vivo[1][2][3].
m-PEG7-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Brevicornin is a flavonol from Epimedium brevicornum[1].
NSC 10281-d4 is the deuterium labeled NSC 10281[1].
VO-OHPic is a reversible, noncompetitive and selective PTEN inhibitor with an IC50 of 46 nM. VO-OHPic attenuates apoptosis, adverse cardiac remodeling, and pro-inflammatory M1 macrophages in doxorubicin-induced cardiomyopathy. VO-OHPic inhibits autophagy[1][2][3].
UCD38B hydrochloride is a cell permeant, competitive enzymatic uPA inhibitor with an IC50 value of 7 μM. UCD38B hydrochloride targets intracellular uPA causing mistrafficking of uPA into perinuclear mitochondria, reducing the mitochondrial membrane potential, and followed by the release of apoptotic inducible factor (AIF). UCD38B hydrochloride induces apoptosis[1][2].
Gondoic acid (cis-11-Eicosenoic acid), a monounsaturated long-chain fatty acid, is contained in a variety of plant oils and nuts[1].
4'-Methoxyflavonol is a synthesized flavone/flavonol with 1, 2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) bilayers[1].
2'-F-Bz-dC Phosphoramidite can be used in the synthesis of oligoribonucleotides[1].
Quinate is an antiarrhythmic agent. Quinate is a potent, orally active, selective cytochrome P450db inhibitor. Quinate is also a K+ channel blocker with an IC50 of 19.9 μM. Quinate can be used for malaria research[1][2][3].
AZD-1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of < 0.4 nM, selectively against JAK3 and Tyk2, and to a smaller extent against JAK1.
Trequinsin hydrochloride (HL 725) is an extremely potent inhibitor of platelet CAMP phosphodiesterase (PDE), with an IC50 of 0.25 nM. Trequinsin hydrochloride (HL 725) is an extremely potent inhibitor of the aggregation of human platelets induced in vitro by ADP, collagen, thrombin and epinephrine[1][2][3].
3-(2-Pyridyldithio)propanoic Acid is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
F16 is a small molecule that selectively inhibits proliferation of mammary epithelial, neu-overexpressing cells, as well as a variety of mouse mammary tumor and human breast cancer cell lines. 1, F16 induced cell cycle arrest in sensitive mouse tumor and human cancer cell lines.2, Prolonged incubation with 3 uM F16 resulted in increased cell death of F16-sensitive cells but not of F16-resistant ones.3, F16 caused apoptosis in A6 cells.4, F16 caused a dramatic decrease in the number of cells in S phase and an increase in the percentage of cells in G1 phase.5, F16 is capable of inhibiting oxidative phosphorylation and inducing mitochondrial transmembrane depolarization.