intact cell

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

Platycodin D may stimulate TNF-α synthesis or inhibit degradation of TNF-α mRNA. Platycodin D (10 30 μM) suppresses prostaglandin E2 production in rat peritoneal macrophages stimulated by the protein kinase C activator 12-O-tetradecanoyl phorbol 13-acetate (TPA). Platycodin D and D3 are useful as expectorant agents in the treatment of various airway diseases, they can increase mucin release from rat and hamster tracheal surface epithelial cell culture and also from intact rat trachea upon nebulization.

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

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.

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.

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).

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 probe suitable for click chemistry designated to measure kinase selectivity in intact cells. PF-6808472 contains sulfonyl fluoride group, which react with conserved lysine residue within kinase ATP binding site.

Erlotinib-13C6 (CP-358774-13C6) is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR[1]. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer[1].Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process[2]. [1]. Moyer JD, et al. Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res. 1997, 57(21), 4838-4848.[2]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

Ru360, an oxygen-bridged dinuclear ruthenium amine complex, is a selective mitochondrial calcium uptake inhibitor. Ru360 potently inhibits Ca2+ uptake into mitochondria with an IC50 of 0.184 nM. Ru360 binds to mitochondria with high affinity (Kd of 0.34 nM). Ru360 has antiarrhythmic and cardioprotective effects[1][2]. Ru360 permeates slowly into the cell, and specifically inhibits mitochondrial calcium uptake in intact cardiomyocytes and in isolated heart. 1 μm Ru360 is taken up by myocardial cells and accumulated in the cytosol in a biphasic manner[1]. During pelleting hypoxia, Ru360 (10 µM) significantly improves cell viability in wild type cardiomyocytes[3]. Ru360 (15-50 nmol/kg) treatment abolishes the incidence of arrhythmias and haemodynamic dysfunction elicited by reperfusion in a whole rat model. Ru360 administration partially inhibits calcium uptake, preventing mitochondria from depolarization by the opening of the mitochondrial permeability transition pore (mPTP)[1]. [1]. G de J García-Rivas, et al. Ru360, a Specific Mitochondrial Calcium Uptake Inhibitor, Improves Cardiac Post-Ischaemic Functional Recovery in Rats in Vivo. Br J Pharmacol. 2006 Dec;149(7):829-37. [2]. M A Matlib, et al. Oxygen-bridged Dinuclear Ruthenium Amine Complex Specifically Inhibits Ca2+ Uptake Into Mitochondria in Vitro and in Situ in Single Cardiac Myocytes. J Biol Chem. 1998 Apr 24;273(17):10223-31. [3]. Lukas J Motloch, et al. UCP2 Modulates Cardioprotective Effects of Ru360 in Isolated Cardiomyocytes During Ischemia. Pharmaceuticals (Basel). 2015 Aug 4;8(3):474-82.

JJH260 is an N-hydroxy hydantoin carbamate that inhibits androgen-induced gene 1 (AIG1), an enzyme that hydrolyzes fatty acid esters of hydroxy fatty acids (FAHFAs). It blocks the hydrolysis of 9-PAHSA with an IC50 value of 0.57 μM. JJH260 also inhibits the novel FAHFA hydrolase androgen-dependent TFPI-regulating protein (ADTRP; IC50 = 8.5 μM), as well as the serine hydrolase ABHD6 and the lysophospholipases LYPLA1 and LYPLA2. JJH260 inhibits the FAHFA hydrolase activity of LNCaP and T cell lysates and intact cells.

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).

AMB639752 is a potent inhibitor of diacylglycerol kinase alpha (DGKα) that reinstates restimulation-induced cell death (RICD) in SAP-deficient lymphocytes through DGKα inhibition within intact cells. This compound is applicable in the research of X-linked lymphoproliferative disease 1 (XLP-1) [1].

1CAY10649, a thiazolinone compound, directly inhibits 5-lipoxygenase (5-LO) product formation in intact polymorphonuclear leukocytes (PMNL) with an IC50 value of 0.28 μM and in a soluble fraction of an S100 PMNL cell lysate with an IC50 value of 0.09 μM, following stimulation by calcium and arachidonic acid. This activity highlights its potential in mitigating inflammatory responses by targeting the biosynthesis of leukotrienes, substances implicated in various inflammatory processes such as neutrophil chemotaxis, increased vascular permeability, and smooth muscle contraction.

TAT peptide corresponds to the polycationic aa49-57 region of TAT protein. TAT peptide is a cell-penetrating peptide (CPP) used to cargo larger molecules through the lipophilic barrier of the cellular membranes to deliver them inside the cells with intact

Selective cell-permeable peptide inhibitor of protein kinase C (IC50 ~ 0.5 μM). Consists of amino acids 19 - 31 of PKC pseudosubstrate domain linked by a disulphide bridge to a cell permeabilisation Antennapedia domain vector peptide. The Antennapedia pep

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 Antennapedia domain vector peptide. The Antennapedia peptide is actively taken up by intact cells, at 4 or 37°C, ensuring rapid and effective uptake of the inhibitor peptide. Once inside the cell, the disulphide bonds are subjected to reduction in the cytoplasm leading to release of the inhibitor peptide. Induces mast cell degranulation by a PKC ζ-independent pathway.

Activator of protein kinase C; attached to cell permeabilization Antennapedia domain vector peptide. Consists of peptide derived from the C2 domain of PKC β linked by a disulfide bridge to the Antennapedia domain vector peptide. The Antennapedia peptide i