tr

Ganoderic acid TR is a broad-spectrum inhibitor of influenza neuraminidases (NAs), particularly H1N1 and H5N1 neuraminidases, with IC50 values of 4.6 and 10.9 μM, respectively.

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.

Tr-PEG2-OH is a PEG-based PROTAC linker used in PROTAC synthesis[1] and a non-cleavable 2-unit PEG ADC linker for antibody-drug conjugate (ADC) synthesis[2].

Tr-PEG3-OH, a non-cleavable three-unit PEG ADC linker, is used in the synthesis of antibody-drug conjugates (ADCs).

Tr-PEG4-OH is a non-cleavable tetraethylene glycol ADC linker used in ADC synthesis for the conjugation of antibodies and drugs.

Tr-PEG5-OH is a non-cleavable 5-unit PEG ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs).

Tr-PEG6-OH is a 6-unit polyethylene glycol (PEG) linker, which is non-cleavable and extensively employed in the synthesis of antibody-drug conjugates (ADCs).

Tr-PEG8-OH, a non-cleavable 8-unit PEG ADC linker, is utilized in the synthesis of antibody-drug conjugates (ADCs).

Methoxy-Tr-NH-PEG7 is a PEG-based linker for PROTACs, joining two essential ligands crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.

TR4161 is a prostaglandin bronchodilator of low tracheobronchial irritancy.

TR-14035 (MDK-1191) is a dual antagonist of α4β7/α4β1 integrins (IC50s: 7/87nM).

NASTRp, an inhibitor of CREB-CBP complex, possesses anti-cancer effects along with cell cycle regulation, autophagy suppression, and endoplasmic reticulum stress.

Tedizolid (DA-7157)is a novel oxazolidinone-class antibiotic that inhibits bacterial protein synthesis by binding to the 23S ribosomal RNA of the 50S subunit of the ribosome.

Tedizolid Phosphate (TR-701FA) is an oxazolidinone-class antibiotic. Tedizolid phosphate is a phosphate ester prodrug of the active compound tedizolid.

(S)-Tedizolid is the S-enantiomer of Tedizolid, a novel oxazolidinone with activity against Gram-positive pathogens.

Ropitoin is a novel drug of antiarrhythmics.

Butaprost is a selective agonist of the prostaglandin E receptor EP2 that exhibits an EC50 of 33 nM and a Ki of 2.4 μM toward the murine EP2 receptor, while showing markedly lower activity against murine EP1, EP3, and EP4 receptors. Butaprost effectively attenuates fibrotic responses by inhibiting the TGF-β/Smad2 signaling pathway, supporting its utility in fibrosis, inflammation, and prostaglandin receptor signaling research.

Aristolochic acid A is the main component of the plant extract aristolochic acids, primarily found in the herbaceous plants Aristolochia and Asarum. It significantly inhibits the activity of activator protein 1 (AP-1) and NF-κB, and downregulates the expression of the bladder cancer-associated BLCAP gene in human cells. It is commonly used to induce nephrotoxicity models.

Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable, and comparable potency inhibitor of CDK4 and CKD6 with IC50s of 12.4 nM and 9.9 nM, respectively. Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest.

Sodium aristolate 1, also known as aristolochic acid sodium salt, is found in certain Chinese herbal medicines and causes nephrotoxicity. This proagent becomes active when its nitro groups are reduced to amines, which subsequently leads to the production of cytotoxic DNA adducts.

ONO-TR-772 (VU6018042) is a selective TREK inhibitor with an IC50 of 15 nM. It improves recognition memory in the NOR mouse model induced by MK-801. ONO-TR-772 is useful in research on diseases associated with cognitive impairment.

TR-100 is a small molecule inhibitor targeting tumor-associated tropomyosin (Tpm). It binds to the C-terminus of Tpm3.1, affecting its interaction with actin filaments and thus influencing their stability and function. This mechanism allows TR-100 to specifically affect actin filament bundles in cancer cells without impairing cardiac muscle function. TR-100 is useful for studying the role of Tpm3.1 in cancer cell proliferation and survival, as well as its impact on insulin-stimulated glucose uptake and insulin secretion.

TR antagonist 2 (Compound 10a) is a competitive inhibitor of thyroid hormone receptors (TRα/β) with an IC50 of 47 nM. It works by competitively binding to the ligand-binding domain of the receptor with triiodothyronine (T3), thereby blocking the formation of the receptor-coactivator complex, inhibiting target gene transcription, and reducing thyroid hormone-mediated metabolic effects. TR antagonist 2 holds potential for research into hyperthyroidism (such as Graves' disease) and thyrotoxicosis.

TR-107 (Anticancer agent 230) is a selective and potent activator of the mitochondrial protease ClpP that inhibits tumor growth in the MDA-MB-231 xenograft model.