hek293t

SR1664 is a potent and selective PPARγ inhibitor with potential antidiabetic activity. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50 = 80 nM; Ki = 28.67 nM) without exhibiting PPARγ agonist activity.

PTGR2-IN-1 is a potent inhibitor of PTGR2 (IC50: 0.7 μM) that enhances 15-keto-PGE2-dependent PPARγ transcriptional activity in PTGR2-transfected HEK293T cells.

N1-Methylpseudouridine (1-Methylpseudouridine) is a methylpseudouridine and enhances translation through eIF2α-dependent and independent mechanisms by increasing ribosome density in mRNA.

PTC-209 hydrobromide (PTC-209 HBr) is the hydrobromide salt of PTC-209, which is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM, and results in irreversible reduction of cancer-initiating cells (CICs).

Yoda 1 is an agonist of the Piezo1 channel that agonizes human- and mouse-derived Piezo1 (EC50=17.1 26.6 μM). Yoda 1 is also an inhibitor of glycine transporter protein 2 (GlyT2).

ML-209 is an antagonist of retinoic acid receptor-related orphan receptor γt (RORγt; IC50= 1.1 μM in a reporter assay).1It inhibits RORγt-induced transcription in HEK293T cells expressing the human receptor (IC50= 300 nM). ML-209 inhibits RORγt-dependent differentiation of isolated na?ve cord blood human CD4+T cells into Th17 T helper cells.

Niacinamide is an important compound functioning as a component of the coenzyme NAD. Its primary significance is in the prevention and or cure of blacktongue and PELLAGRA. Most animals cannot manufacture this compound in amounts sufficient to prevent nutr

WS-12 is a potent TRPM8 agonist that acts as a cooling agent (EC50 : 193 nM)

PTC-209 is a potent and selective BMI-1 inhibitor.

ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1), with IC50 values of 6.4 nM and 4.2 nM in HEK293T and MDA-MB-231 cells, respectively.

TD-165, a PROTAC-based cereblon (CRBN) degrader, consists of a cereblon (CRBN) ligand-binding group, a linker, and a von Hippel-Landau (VHL) binding group[1].

YSY01A is a proteasome inhibitor that suppresses cancer cell survival by inducing apoptosis (Apoptosis). It demonstrates IC50 values against various cell lines such as HEK293T, A549, MCF-7, MGC-803, and PC-3M with values of 51.01, 9.21, 5.21, 8.9, and 35.4 nM respectively. Additionally, YSY01A serves as a degrader of gp130 and JAK2, eliminating constitutive STAT3 signaling in human A549 lung cancer cells by downregulating gp130 and JAK2. YSY01A holds potential for research in cancer therapeutics.

HPG1860, an agonist of the farnesoid X receptor (FXR), induces luminescence in reporter gene assays utilizing HEK293T cells expressing human FXR, with an EC50 value of 18 nM. In vivo studies demonstrate that HPG1860 (administered at 1, 3, or 10 mg kg daily) reduces serum alanine aminotransferase (ALT) and total cholesterol levels in a mouse model of non-alcoholic steatohepatitis (NASH), which was induced by a high-fat diet and carbon tetrachloride (CCl4). Additionally, this compound decreases hepatic inflammation, fat levels, and fibrosis.

Cyano-myracrylamide is an inhibitor of zinc finger DHHC domain-containing palmitoyltransferase 20 (zDHHC20) with an IC50 value of 1.35 µM. It also inhibits the S-palmitoylation of EGFR and CD36. In HEK293T cells expressing recombinant E. coli GobX, recombinant human MyD88, or endogenous Ras, Cyano-myracrylamide inhibits the S-palmitoylation of E. coli E3 ligase GobX, MyD88, and Ras, which are substrates of zDHHC20, zDHHC9, and zDHHC6.

MYF-01-37 (1-[3-Methyl-3-[3-(trifluoromethyl)anilino]pyrrolidin-1-yl]prop-2-en-1-one) is a novel covalent TEAD inhibitor.

XY018 is an orally available, selective and highly effective ROR-γ antagonist with antitumor activity, inhibits ROR-γ activity, inhibits tumor cell growth, and can be used to study drug-resistant prostate cancer.

Lipoxygenin is an inhibitor of 5-lipoxygenase (5-LO) with an IC50value of 5 μM for inhibition of 5-LO product synthesis in isolated human granulocytes stimulated with the cation ionophore A23187 .1It inhibits hedgehog-dependent signaling in Shh-LIGHT2 cells and TGF-β-, activin A-, bone morphogenic protein (BMP)-, or Wnt-dependent signaling in HEK293T cells (IC50s = 9.3, 3.2, 8.2, 9.6, and 3.7 μM, respectively, in luciferase reporter assays). Lipoxygenin (5 and 10 μM) increases levels of troponin T (TnnT), a marker of cardiomyocyte differentiation, in human induced pluripotent stem cells (iPSCs) stimulated with BMP4 and the glycogen synthase kinase 3 (GSK3) inhibitor CHIR99021 .

Gliotoxin-13C13is intended for use as an internal standard for the quantification of gliotoxin by GC- or LC-MS. Gliotoxin is an immunosuppressive mycotoxin produced by pathogenic strains ofAspergillusand other fungi with diverse biological activities.1,2,3,4,5,6,7,8It inhibits 20S proteasomal chymotrypsin activity (IC50= 10 μM), blocking the degradation of IκBα and preventing the activation of NF-κB.2,3Gliotoxin induces apoptosis in monocytes and dendritic cells and reduces phagocytosis by neutrophils.4,5It suppresses viral infection by Nipah and Hendra virus in HEK293T cells (IC50s = 149 and 579 nM, respectively).6Under reducing conditions, gliotoxin inhibits leukotriene A4hydrolase epoxide hydrolase activity, but not aminopeptidase activity, and leukotriene B4synthesis in neutrophils and monocytes.7

Photoswitchable PAD inhibitor is a photoactivated protein arginine deiminase (PAD) inhibitor and a derivative of BB-Cl-amidine that contains an azobenzene photoswitch allowing optical control of PAD activity.1 Without photoactivation, it is a weak inhibitor of PAD2 (IC50 = >100 μM) and is less potent than BB-Cl-amidine in inhibiting citrulline production in vitro (kinact/KIs = 2,300, 600, 1,000, and 10,510 M-1min-1 for PAD1-4, respectively) and does not inhibit histone H3 citrullination in HEK293T cells overexpressing PAD2 when used at concentrations up to 100 μM. However, it can rapidly be photoactivated with UV-A radiation to the more active cis-isomer, which is an irreversible, competitive inhibitor of histone H3 citrullination with an IC50 value of 9.1 μM.References1. Mondal, S., Parelkar, S.S., Nagar, M., et al. Photochemical control of protein arginine deiminase (PAD) activity. ACS Chem. Biol. 13(4), 1057-1065 (2018). Photoswitchable PAD inhibitor is a photoactivated protein arginine deiminase (PAD) inhibitor and a derivative of BB-Cl-amidine that contains an azobenzene photoswitch allowing optical control of PAD activity.1 Without photoactivation, it is a weak inhibitor of PAD2 (IC50 = >100 μM) and is less potent than BB-Cl-amidine in inhibiting citrulline production in vitro (kinact/KIs = 2,300, 600, 1,000, and 10,510 M-1min-1 for PAD1-4, respectively) and does not inhibit histone H3 citrullination in HEK293T cells overexpressing PAD2 when used at concentrations up to 100 μM. However, it can rapidly be photoactivated with UV-A radiation to the more active cis-isomer, which is an irreversible, competitive inhibitor of histone H3 citrullination with an IC50 value of 9.1 μM. References1. Mondal, S., Parelkar, S.S., Nagar, M., et al. Photochemical control of protein arginine deiminase (PAD) activity. ACS Chem. Biol. 13(4), 1057-1065 (2018).

Selective peptide-based β-catenin Degrader. Comprises a β-catenin-targeted stapled peptide, xStAx, linked to a VHL-binding peptide. Reduces β-catenin levels in HEK293T cells and colorectal cancer cell lines. Selectively degrades β-catenin over other Wnt signaling pathway components. Inhibits tumor growth in APCmin/+ mice, with constitutively active Wnt signaling, and reduces survival of patient-derived colorectal cancer cell organoids.

Guanosine 5'-diphosphate (GDP) is a purine nucleotide and biosynthetic precursor of guanosine 5'-triphosphate .1It has been used to study the conformations of GTPases.2GDP (100 μM) activates sulfonylurea receptor 2B (SUR2B) linked to the inward-rectifier potassium channel 6.1 (Kir6.1) in HEK293T cells in a patch-clamp assay.3 1.Berg, J.M., Tymoczko, J.L., and Stryer, L.Biochemistry(2002) 2.Vetter, I.R., and Wittinghofer, A.The guanine nucleotide-binding switch in three dimensionsScience294(5545)1299-1304(2001) 3.Yamada, M., Isomoto, S., Matsumoto, S., et al.Sulphonylurea receptor 2B and Kir6.1 form a sulphonylurea-sensitive but ATP-insensitive K+ channelJ. Physiol.499(Pt 3)715-720(1997)

Biotinylated UNC 1999 (Cat.No. 4904, IC50 = 17 nM). Enriches lysine methyltransferase EZH2 from HEK293T cells. Negative control also avilable. 0

SSAA09E1 is an inhibitor of severe acute respiratory syndrome coronavirus (SARS-CoV) viral entry.1It reduces infection of HEK293T cells transiently transfected with angiotensin-converting enzyme 2 (ACE2) by an HIV-based virus system pseudotyped with SARS-CoV surface glycoprotein (EC50= 6.7 μM). SSAA09E1 also inhibits the proteolytic activity of cathepsin L (IC50= 5.33 μM) but not cathepsin B when used at a concentration of 20 μM. 1.()

PW0464 ((Rac)-Razpipadon) is a non-catechol D1R agonist and potent omplete G protein biased ligand with an EC50 (Gs-cAMP)=5.8 nM for the study of neurological disorders.