intact

Erlotinib (NSC-718781) is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.

GeA-69 (GeA69) is a selective and allosteric PARP14 macrodomain 2 (MD2) inhibitor (Kd: 0.86 μM in ITC assays).

Acemetacin (TVX 1322) is a carboxymethyl ester of indometacin and a potent non-steroidal anti-inflammatory drug derived from indol-3-acetic acid, with its activity primarily attributed to its active metabolite, indomethacin. In clinical trials, acemetacin shows better gastric tolerability compared to indomethacin.

Tepoxalin (RWJ 20485) is a 5-lipoxygenase inhibitor potentially for the treatment of asthma, osteoarthritis. Tepoxalin inhibits COX-1, COX-2, and 5-LOX. Tepoxalin is a potent inhibitor of sheep seminal vesicle cyclooxygenase (COX) (IC50 = 4.6 microM), rat basophilic leukemia cell (RBL-1) lysate COX (IC50 = 2.85 microM) and COX from intact RBL-1 cells (IC50 = 4.2 microM).

Siguazodan (SKF 94836) is an effective, selective, orally active phosphodiesterase III ((PDE-III)) inhibitor with an IC50 of 117 nM. Siguazodan inhibited phenylephrine induced 5-HT release with an IC50 value of 4.2 μM. Siguazodan can increase cAMP accumulation in intact platelets, with EC50 of 18.88 μM.

Losulazine is a peripheral sympathetic antihypertensive compound that can be taken orally. Losulazine causes relatively modest, transient depletion of dopamine and norepinephrine in brain regions protected by the blood-brain barrier.

TNIK-IN-5 is an potent TNIK inhibitor (IC50= 0.05 μM). TNIK-IN-5 potently inhibits Wnt signaling in intact cells. TNIK-IN-5 exhibits excellent in vitro anti-colorectal cancer activity.

PKC ζ pseudosubstrate acetate is an inhibitor of protein kinase C (PKC) ζ; attached to cell permeabilisation Antennapedia domain vector peptide. Consists of amino acids 113 - 129 of PKC ζ pseudosubstrate domain linked by a disulphide bridge to the Antenna

Lyn peptide inhibitor acetate is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders.

Quiflapon (MK-591) causes cell apoptosis. Quiflapon is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor (IC50: 1.6 nM in a FLAP binding assay) and is also an effective and orally active Leukotriene biosynthesis (LT) inhibitor (IC50: 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively).

ALKBH5-IN-3 (Compound 20m) is a selective ALKBH5 inhibitor (IC50=21 nM) that effectively stabilizes ALKBH5 in HepG2 cells and elevates m6A levels in intact cells.

2-Methyl-3-phenylquinoxaline (compound 38) serves as an effective inhibitor of the Platelet-Derived Growth Factor Receptor Tyrosine Kinase (PDGF-RTK), exhibiting significant inhibitory activity against the full-length PDGFR kinase in intact cells (IC50 greater than 100 μM).

11:0 PC (1,2-Diundecanoyl-sn-glycero-3-phosphocholine) is a type of phosphatidylcholine that plays a role in the folding of intact, functional integral membrane proteins.

AZD2389 is an effective and orally active FAP inhibitor that improves histological fibrosis and increases intact α2-AP, suitable for studying metabolic dysfunction-associated steatohepatitis.

2-Fluorodeoxyarbutin is a derivative of Deoxyarbutin and acts as an inhibitor of tyrosine hydroxylase and dopa oxidase. It suppresses melanin synthesis in intact melanocytes and can be utilized in the study of skin lightening or the treatment of pigmented lesions.

Trioxacarcin B (TXN-B) is a potent cytotoxic agent and DNA-targeting inhibitor. It disrupts DNA function and induces apoptosis in cancer cells. Trioxacarcin B effectively inhibits the growth of various Gram-positive and Gram-negative bacteria, as well as malignant plasmodium. It also prevents the formation of tumor stem cell colonies and significantly reduces tumor size and prolongs survival in preclinical in vivo models. Its activity is highly dependent on its intact spiroepoxide structure, which becomes ineffective upon hydrolysis. Trioxacarcin B shows no activity against fungi, microalgae, or small RNA viruses. It is applicable in research on bacterial infections, malaria, and various cancers, including colon cancer and melanoma.

BAY-297 is an inhibitor of PIP4K2A. It binds to PIP4K2A in both intact cells and cell lysates. BAY-297 serves as a chemical probe for studying the PIP4K2A signaling pathway and its role in physiological conditions such as cancer.

HZ52 is a potent, reversible 5-lipoxygenase (5-LO) inhibitor that blocks leukotriene (LTs) synthesis with an IC50 of 0.7 μM in intact human polymorphonuclear leukocytes [1].

Netzahualcoyone inhibited the respiration of intact cells of B. subtilis but had no effect on the respiration of E. coli.

5-Oxodecanoic acid is a biochemical. 5-Oxodecanoic acid can be reducced to 5-hydroxydecanoic acid by intact cells of baker's yeast.

Acetylethylcholine mustard can effect muscarinic receptor-coupled attenuation of cAMP formation for intact GH3 cells.

CDy9 is a highly selective fluorescent probe for the detection and isolation of mESC using fluorescence microscopy and flow cytometry. CDy9 allows the detection and isolation of intact stem cells with marginal impact on their function and capabilities. CD

PF-6808472 is a cell-permeable covalent kinase probe that reacts with conserved lysine residues within the ATP-binding site of kinases, thereby binding to and labelling multiple kinases such as CDK1/2/4.

Neuromedin U-23 (NMU-23) is a neuropeptide involved in diverse biological processes, including smooth muscle contraction, energy homeostasis, and nociception.1It is an agonist of neuromedin-U receptor 1 (NMUR1; EC50= 0.17 nM for the human receptor in a calcium mobilization assay using HEK293 cells) and NMUR2 (EC50= ~1.4-2 nM for arachidonic acid release in CHO cells expressing the human receptor).2,3NMU-23 (1 μM) induces contractions in isolated rat colon smooth muscle strips.4It decreases body weight and food intake and increases core body temperature in mice when administered at a dose of 36 μg/animal.5Intrathecal administration of NMU-23 decreases the mechanical pain threshold in the von Frey test in rats.6 1.Mitchell, J.D., Maguire, J.J., and Davenport, A.P.Emerging pharmacology and physiology of neuromedin U and the structurally related peptide neuromedin SBr. J. Pharmacol.158(1)87-103(2009) 2.Szekeres, P.G., Muir, A.I., Spinage, L.D., et al.Neuromedin U is a potent agonist at the orphan G protein-coupled receptor FM3J. Biol. Chem.275(27)20247-20250(2000) 3.Hosoya, M., Moriya, T., Kawamata, Y., et al.Identification and functional characterization of a novel subtype of neuromedin U receptorJ. Biol. Chem.275(38)29528-29532(2000) 4.Brighton, P.J., Wise, A., Dass, N.B., et al.Paradoxical behavior of neuromedin U in isolated smooth muscle cells and intact tissueJ. Pharmacol. Exp. Ther.325(1)154-164(2008) 5.Peier, A., Kosinski, J., Cox-York, K., et al.The antiobesity effects of centrally administered neuromedin U and neuromedin S are mediated predominantly by the neuromedin U receptor 2 (NMUR2)Endocrinology150(7)3101-3109(2009) 6.Yu, X.H., Cao, C.Q., Mennicken, F., et al.Pro-nociceptive effects of neuromedin U in ratNeuroscience120(2)467-474(2003)