assay

PTZ-343 is a potent enhancer of Luminol, acting as an electron transfer mediator. It reacts with HRP-II to release HRP and a PTZ-343 radical, which then oxidizes luminol anions to induce light emission.

Remibrutinib inhibits BTK activity with an IC50 value of 0.023 μM in blood. Remibrutinib is an effective and orally active Bruton tyrosine kinase inhibitor (IC50: 1 nM). Remibrutinib has the potential for Chronic urticaria (CU) treatment.

Semaglutide is a glucagon-like peptide 1 receptor (GLP-1R) agonist(EC50 of 6.2 pM in a reporter assay using BHK cells expressing the human receptor).

PF-573228 is an ATP-competitive FAK inhibitor. In a cell-free assay, the IC50 of FAK is 4 nM.

GW9662 (TIMTEC-BB SBB006523) is a PPARγ antagonist (IC50=3.3 nM) with selectivity. GW9662 can be used to study the pathogenesis of metabolic diseases, such as obesity and diabetes, by inhibiting the activity of PPARγ. GW9662 can be used to study the pathogenesis of inflammatory diseases, such as atherosclerosis and rheumatoid arthritis. GW9662 has anti-tumor effect.

LY-411575, a potent γ-secretase inhibitor, is with IC50 of 0.078 nM in the membrane and 0.082 nM in cell-based. It also suppresses Notch clevage with IC50 of 0.39 nM.

AZD-7648 is an inhibitor of DNA-dependent protein kinase (DNA-PK) with the IC50 of 0.63 nM in an enzyme assay,has anti-tumor activity.

Urotensin I acetate, a CRF-like neuropeptide, acts as an agonist of CRF receptor with pEC50s of 11.46, 9.36 and 9.85 for human CRF1, human CRF2 and rat CRF2α receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF2α and mCRF2β receptors, respectively[1][2].

Galidesivir (BCX4430) is a broad-spectrum antiviral compound, an adenosine analog that inhibits viral RNA-dependent RNA polymerase (RdRp) activity.Galidesivir inhibits a wide range of RNA viral pathogens in vitro, and reduces lung infections in infected animals.

Celgosivir (6 O-butanoyl castanospermine) is an inhibitor of α-glucosidase I. In vitro assay, it inhibits bovine viral diarrhoea virus (BVDV) ( IC50: 1.27 μM ).

Cysteine protease inhibitor 2 is a cysteine protease inhibitor. Cysteine protease inhibitor 2 inhibited DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.

GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells). GCN2-IN-6  is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9

Mutant IDH1-IN-2 is an inhibitor of mutant Isocitrate dehydrogenase (IDH) proteins, with an IC50 of 16.6 nM in fluorescence biochemical assay and an IC50 of <22 nM in LS-MS biochemical assay.

PI3Kα/mTOR-IN-1 is a potent dual inhibitor of PI3Kα/mTOR, with an IC50 of 7 nM for PI3Kα in a cell assay and Kis of 12.5 nM and 10.6 nM for mTOR and PI3Kα [in a cell-free assay], respectively.

(1R,2R)-2-PCCA hydrochloride is a potent, selective, and blood-brain-barrier-crossing GPR88 receptor agonist with an EC50 value of 1140 n in striatal membranes of WT mice; it can be used to study the central nervous system.

3CAI is a potent and specific AKT1 and AKT2 inhibitor, demonstrating significant inhibition of AKT in an in vitro kinase assay. It suppressed the expression of AKT direct downstream targets (such as mTOR and GSK3β) and induced growth inhibition and apoptosis in colon cancer cells.

MAK683 is an inhibitor of embryonic ectoderm development (EED) (IC50s: 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay).

FMK 9a is an irreversible inhibitor of ATG4B with IC50 values of 80 and 73 nM in the TR-FRET and cellular-based LRA assays.

GNE-049 is a highly selective and potent inhibitor designed to target the CREB-binding protein (CBP) with high affinity, exhibiting an IC50 of 1.1 nM for the suppression of BRET and BRD4 activity, which consequently blocks prostate cancer cell proliferation in both in vitro and in vivo models.

Naluzotan(PRX 00023) is a novel and potent 5-HT1A agonist with IC50 and Ki values of approximately 20 nM and 5.1 nM, respectively.Naluzotan is a potent hERG K+ channel blocker with an IC50 value of 3800 nM.Naluzotan exhibits anxiolytic activity and can be used to study depression.

Tazemetostat hydrobromide (E-7438 hydrobromide) is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 (Ki: 2.5 nM). Tazemetostat hydrobromide also inhibits EZH1 (IC50: 392 nM).

Calpain Inhibitor XII (Z-L-Nva-CONH-CH2-2-Py) is a selective and potent inhibitor of calpain I, inhibits calpain II and cathepsin B. Calpain Inhibitor XII shows antiviral activity against coronavirus in cell culture.

GPR35 agonist 2 (TC-G 1001) is a potent GPR35 agonist.The EC50 values of GPR35 agonist 2 in the β-arrestin and Ca2+ release assays were 26 and 3.2 nM, respectively.

Antifolate C2 (AGF 154) has antitumor activity with an IC of 0.14 nM measured in a growth inhibition assay of human tumor cells.Antifolate C2 can be used for the study of cancer and autoimmune diseases.