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.

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.

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

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

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

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.

UZH1 is a racemate of UZH1a and UZH1b. UZH1a is a potent and selective METTL3 inhibitor with an IC50 of 280 nM, while UZH1b (IC50=28 μM) is essentially inactive. UZH1 can be used for epitranscriptomic modulation of cellular processes, has antitumor activity, and serves as a chemical probe for studying METTL3[1].

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).

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.

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.

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

Tianeptine metabolite MC5, an active derivative of the atypical antidepressant tianeptine produced through β-oxidation, exhibits selective G protein activation in bioluminescence resonance energy transfer (BRET) assays. Utilizing HEK293T cells expressing the human μ-opioid receptor (MOR) over the human δ-opioid receptor (DOR; EC50s = 0.454 and >100 µM, respectively), it demonstrates specificity. Moreover, this metabolite reduces immobility in wild-type mice during the forced swim test at a dose of 30 mg/kg, an effect not observed in MOR knockout mice, suggesting its antidepressant-like activity is MOR-dependent.

Chloroguanabenz is an antiprion agent and a derivative of the α2-adrenergic receptor agonist guanabenz . It inhibits prion formation in yeast and mammalian cell-based assays. Chloroguanabenz reduces the levels of both soluble and aggregated forms of the truncated Huntingtin derivative Htt48 in an HEK293T cellular model of Huntington's disease.

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.

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.

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

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).

STAT3-IN-32 (compound 4c) is an orally active, potent dual phosphorylation inhibitor of STAT3. It demonstrates significant inhibition of STAT3 luciferase activity in HEK293T cells, with an IC50 of 5.3 nM, and inhibits ATP production in BxPC-3 cells with an IC50 of 4.2 nM. By targeting the STAT3 SH2 domain (KD=21.3 nM), STAT3-IN-32 effectively blocks p-Tyr705 and p-Ser727, leading to the attenuation of STAT3 nuclear transcription and mitochondrial oxidative phosphorylation. Furthermore, this compound displays notable suppressive effects in a pancreatic cancer xenograft model.

M04 acts as a stimulator of interferon genes (STING) agonist, effectively inducing IFN reporter gene expression in HEK293T cells equipped with wild-type human STING. Its activity is specific, not affecting HEK293T cells with the R71H-G230A-R293Q (HAQ) human STING variant or mouse RAW 264.7 cells, showcasing allelic- and species-dependent effects at a concentration of 75 µM. This compound also stimulates the production of TNF-α, IL-10, IL-1β, and IL-12p70 in human peripheral blood mononuclear cells (PBMCs). At 50 µM, M04 enhances human monocyte-derived dendritic cells' expression of HLA-DR (MHC class II receptor) and co-stimulatory molecules CD40, CD80, and CD86, improving T cell cross-priming in an ex vivo assay.

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

HIF-1α-IN-5 is an inhibitor of HIF-1α with an IC 50 value of 24 nM in HEK293T cells that also inhibits the activity of MAO-A. HIF-1α-IN-5 downregulates the mRNA expressions of VEGF and PDK1 under hypoxia. HIF-1α-IN-5 has the potential to be used in the cancer research[1].

C-178 is a covalent inhibitor of STING, binds to Cys91 on STING to block its palmitoylation and prevents recruitment and phosphorylation of TBK1 in HEK293T cells.