whole-cell

VU0134992 hydrochloride is the first subtype-preferring, orally active and selective blocker of the Kir4.1 potassium channel pore (IC50: 0.97 μM).

VU0134992 is an Kir4.1 blocker with an IC50 value of 0.97 μM

SB-408124 Hydrochloride is a non-peptide OX1 receptor antagonist(Ki of 57 nM and 27 nM in both whole cell and membrane, respectively).

SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity over OX2 receptor.

Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Ethyl tosylcarbamate is an intermediate in the synthesis of Gliclazide (G409877).

Olinciguat (IW-1701) is an oral guanylate cyclase (sGC) stimulator. It also has concentration-dependent stimulation of sGC in purified rat and human enzyme assays and a whole-cell assay.

GSK-3α/β-IN-1 is a GSK-3α/β inhibitor with IC50 values of 0.265 μM for GSK-3α and 0.255 μM for GSK-3β. It also inhibits PKA with an IC50 of 0.188 μM. GSK-3α/β-IN-1 effectively reduces cell viability in three glioblastoma (GBM) cell lines (IC50: 3-6 μM over 72 hours) without being toxic to human astrocytes, and it exhibits good metabolic stability. Additionally, it shows potential central nervous system activity in a whole human blood-brain barrier (BBB) GBM model.

TCN 237 serves as an antagonist of NR2B subunit-containing NMDA receptors, with a Ki value of 0.85 nM. It specifically blocks glutamate and glycine-induced currents in whole-cell patch-clamp assays when using L-M(TK-) cells expressing NR2B subunit-containing NMDA receptors. This is in contrast to its effect on L-M(TK-) cells with NR2A- or NR2D subunit-containing receptors and HEK293 cells with NR2C subunit-containing receptors. Additionally, TCN 237 at 3 mg/kg dosage mitigates carrageenan-induced mechanical hyperalgesia in rats.

A 78773 is a potent, selective, direct, and reversible 5-lipoxygenase inhibitor. It has activity in a variety of purified cells and in more complex biological systems such as whole blood, lung fragments, and tracheal tissues. A 78773 acts against inflamma

BMS-933043 is a Selective α7 nAChR partial agonist. BMS-933043 showed potent binding affinity to native rat (Ki = 3.3 nM) and recombinant human alpha7 nicotinic acetylcholine receptors (Ki = 8.1 nM). BMS-933043 shows agonist activity in a calcium fluoresc

MitoEbselen-2 chloride is a mitochondria-targeted antioxidant combining TPP and Ebselen. It enriches in mitochondria to scavenge ROS/RNS, protecting mitochondrial function and mitigating oxidative stress-induced neurotoxicity.

Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5 μM) inhibits the proliferation of KG-1a leukemia cells.3 1.Garvin, L.K., Green, N., Hu, Y., et al.Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure-activity relationshipsBioor. Med. Chem. Lett.15(23)5288-5292(2005) 2.Wang, X., and Studzinski, G.P.Expression of MAP3 kinase COT1 is up-regulated by 1,25-dihydroxyvitamin D3 in parallel with activated c-jun during differentiation of human myeloid leukemia cellsJ. Steroid. Biochem. Mol. Biol.121(1-2)395-398(2010) 3.Wang, X., Gocek, E., Novik, V., et al.Inhibition of Cot1/Tlp2 oncogene in AML cells reduces ERK5 activation and up-regulates p27Kip1 concomitant with enhancement of differentiation and cell cycle arrest induced by silibinin and 1,25-dihydroxyvitamin D3Cell Cycle9(22)4542-4551(2010)

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.

Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) is an orally active, reversible, and non-competitive selective γ-secretase inhibitor with an IC50 value of 6.2 nM. It exerts its effects by inhibiting the Notch signaling pathway while minimizing gastrointestinal toxicity, making it suitable for the study of Notch receptor-dependent tumors.

Dihydroisopimaric acid activates BK channels alphabeta1, which are large conductance Ca 2+ activated K + channels. This compound directly measures the opening of BKalphabeta1 under a whole-cell voltage clamp.

1-Oleoyl-2-acetyl-sn-glycerol (1-oleoyl-2-acetyl-glycerol) is a cell-permeable calcium-dependent protein kinase C (PKC) activator that modulates whole-cell Ca2+ currents in a variety of excitable cells and induces the production of superoxide.

FTI 277 TFA is a prodrug form of FTI 276 that inhibits farnesyltransferase (FTase) (IC50 = 0.5 nM). Inhibits H-Ras and K-Ras processing in whole cells (IC50 values are 0.1 and 10μM respectively) and disrupts constitutive H-Ras-specific activation of MAPK. Causes significant antiproliferative effects in human malignant glioma cells and many other tumor cell lines.

Mycro 3 is potent and selective for c-Myc in whole cell assays.

BioA-IN-13 is a highly effective inhibitor of the Mycobacterium tuberculosis BioA enzyme, displaying potent cell permeability and whole-cell activity [1].

NAZ2329 is the first cell-permeable inhibitor of the R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), which is a variant and preferentially inhibits PTPRZ (IC50=7.5 μM for hPTPRZ1) and PTPRG (IC50=4.8 μM for hPTPRG) compared to other PTPs. NAZ2329 inhibited the tumor growth of glioblastoma cells and exhibited stem cell-like properties compared to the whole (D1 + D2) fragment of PTPRZ.

PD-85639 is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 μM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1.2 with simultaneous high- and low-affinity modes of binding (EC50 = 56 nM/40% & 20 μM/60% at pH 9.0, 5 nM/28% & 3 μM/72% at pH 7.4, against 2 nM [3H]-PD85,639 for binding rat brain synaptosomes; EC50 = 17 nM/39% & 10 μM/61% using at pH 9.0 using rat brain synaptosome membranes) and a fast kinetic (t1/2 = 1.2 at 4°C, <0.5 min at 25°C), competitive against the local anesthetic Na+ channel blockers tetracaine, bupivacaine, and mepivacaine, as well as Na+ channel activators veratridine and batrachotoxin (K1 = 0.26 μM against 5 nM [3H]-BTX for binding rat neocrotical membranes).

Narsoplimab (OMS 721) is a selective whole-human immunoglobulin gamma-4 (IgG4) monoclonal antibody and a mannan-binding lectin-associated serine protease-2 (MASP-2) inhibitor that binds MASP-2 to prevent lectin pathway activation and inhibit the agglutinin pathway. It is used to study diseases associated with hematopoietic stem cell transplantation in adults.

ω-Conotoxin CVIB is an antagonist of non-selective N- and P/Q-type voltage-gated calcium channels (VGCCs). It inhibits depolarization-activated whole-cell VGCC currents in dorsal root ganglion (DRG) neurons, exhibiting a pIC50 of 7.64 [1].

TRPV1-Tat, a peptide antagonist targeting transient receptor potential vanilloid 1 (TRPV1), is composed of amino acids 736-745 derived from TRPV1's A-kinase anchor protein (AKAP)-binding domain, combined with the HIV Tat-derived cell-penetrating peptide sequence. At a concentration of 200 µM, TRPV1-Tat effectively inhibits heat or phorbol 12-myristate 13-acetate (PMA014)-induced currents in primary mouse dorsal root ganglia via whole-cell patch-clamp assays. Additionally, when administered at dosages of 10 or 30 µM, it elevates the mechanical pain threshold in the hind paws of rats.