tr-1

TR antagonist 1 is a highly potent thyroid hormone receptor (TR) antagonist (IC50 of 36 and 22 nM for TRα and TRβ, respectively) that can be used to study diseases caused by endocrine abnormalities.

GNE-049 is a highly potent and selective inhibitor of CBP (IC50: 1.1 nM in TR-FRET assay). GNE-049 also inhibits BRET and BRD4(1) (IC50s: 12 nM and 4200 nM, respectively).

NKG2D-IN-2 (compound 47) is an inhibitor of the natural killer group 2D receptor (NKG2D), demonstrating half-maximal inhibitory concentrations (IC50s) of 0.1 µM for NKG2D/MICA and 0.2 µM for ULBP6 in time-resolved fluorescence resonance energy transfer (TR-FRET) assays [1].

NKG2D-IN-1, also known as compound 21, is an inhibitor of the natural killer group 2D receptor (NKG2D) exhibiting inhibitory concentration 50 (IC50) values of 0.3 µM in NKG2D/MICA TR-FRET assays and 0.7 µM in ULBP6 TR-FRET assays [1].

(R)-Butaprost (free acid) is a prostaglandin E2 (PGE2) analog exhibiting high EP2 receptor subtype selectivity, commonly used to delineate EP receptor expression in human and animal tissues and cells. In 1986, Gardiner induced significant confusion regarding its structure by incorrectly identifying the selective C-16 epimer as (R)-butaprost (refer to the British Journal of Pharmacology, page 46, as TR 4979, and notes). By removing the methyl ester and restoring the native carboxylic acid at C-1, the binding affinity for prostaglandin receptors was enhanced, given such free acids typically display 10 to 100 times greater affinity than their ester counterparts. Although not extensively studied pharmacologically, (R)-butaprost is generally viewed as the less active C-16 epimer, with careful studies conducted later in the United States and Japan ultimately establishing the correct active structure as the 16(S) epimer.

MProinhibitor 11b is an inhibitor of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (MPro; IC50= 0.04 μM in a TR-FRET assay).1It reduces viral yield in the culture supernatant of SARS-CoV-2-infected Vero E6 cells (EC50= 0.72 μM). MProinhibitor 11b also reduces viral RNA copy numbers in the same model when used at concentrations ranging from 1.85 to 50 μM. 1.Dai, W., Zhang, B., Jiang, X.-M., et al.Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main proteaseScience368(6497)1331-1335(2020)

GNE-781 is a highly potent and selective inhibitor of CBP (IC50: 0.94 nM in TR-FRET assay). GNE-781 also inhibits BRET and BRD4(1) (IC50s: 6.2 nM and 5100 nM, respectively).

Antileishmanial agent-23 (compound G1/9), a potent and selective trypanothione reductase (TR) inhibitor, exhibits an IC50 of 2.24 ± 0.52 μM. It effectively inhibits the growth of Leishmania, Trypanosoma cruzi, and Trypanosoma brucei [1].

CELT-133 is a selective fluorescent antagonist for the hα1A adrenergic receptor, demonstrating complete selectivity towards α1A over α2A receptors, with a Ki of 5 nM and 15% displacement at 1 μM in radioligand binding assays, respectively. It displays equivalent affinity across all α1 adrenergic receptor subtypes. Notably, CELT-133 features excitation and emission maxima (λ) at 560 and 571 nm, respectively, making it suitable for use as an acceptor dye in time-resolved Förster resonance energy transfer (TR-FRET) assays when paired with the CoraFluor 1 TR-FRET donor.

Tr-PEG2-OH is a PEG-based PROTAC linker utilized in PROTAC synthesis[1]. It also serves as a non-cleavable 2-unit PEG ADC linker for the synthesis of antibody-drug conjugates (ADCs)[2].

Antitrypanosomal agent 1 is a potent and selective trypanothione reductase (TR) inhibitor (IC50: 3.3 μM). Antitrypanosomal agent 1 inhibits glutathione reductase (IC50: 64.8 μM) and T. brucei (EC50: 1 μM).

Aristolochic acid A (TR 1736) is a compound of mutagenic, carcinogenic, and nephrotoxic compounds commonly found in the Birthwort (Aristolochiaceae) family of plants.

(1α,1'S,4β)-Lanabecestat is a Beta site APP Cleaving Enzymel (BACE1) inhibitor, and has IC50s of 2.2 nM (TR-FRET assay) and 0.28 nM (sAPPp release assay), respectively.

Keap1-Nrf2-IN-15 (Compound 24a) is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction, displaying IC50 values of 77 nM in a fluorescence polarization (FP) assay and 2.5 nM in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay [1].