Non-peptide neurotensin receptor 1 (NTS1) partial agonist (EC50 <15.6 nM and Emax = 63% of neurotensin response in Ca2+ mobilization assay). Exhibits over 50-fold selectivity for NTS1 over NTS2 and GPR35. Hershberger et al (2014) Imidazole-derived agonists for the neurotensin 1 receptor. Bioorg.Med.Chem.Lett. 24 262 PMID:24332089

TC-AQP1-1 is a blocker of the aquaporin 1 channel identified by virtual screening and inhibits water flux through hAQP1 in Xenopus laevis oocyte swelling assays at low micromolar concentrations.

ROCK-IN-2 (Azaindole 1) is a selective and ATP-competitive ROCK inhibitor with IC50 of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2.

TC-T 6000 (hENT4-IN-1) is a selective and potent inhibitor of human equilibrium nucleoside transporter protein 4 (ENT4) (IC50: 74.4 nM) with vasodilator activity, inhibits hENT1 and hENT2, and can be used for the study of cancer and cardiovascular injury.

σ1 receptor ligand

AAL Toxin TC1 is a useful organic compound for research related to life sciences and the catalog number is T125567.

TC-N 22A is a strong, selective, oral active mGlu4 forward allosteric regulator (PAM) that can cross the blood-brain barrier. EC50 expression of TC-N 22A in BHK cells expressing human mGlu4 was 9 nM. TC-N 22A showed very low activity against mGlu 1, 2, 3, 5, and 7 receptors in excitation and forward allosteric models (EC50 >10 μM). TC-N 22A can be used in the study of central nervous system diseases.

TC ASK 10 is a potent, selective and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1)(IC50 of 14 nM).

Polydatin (Piceid), the glycoside of Resveratrol, is originally isolated from the Chinese herb Polygonum cuspidatum. The compound can inhibit platelet aggregation and elevate the ratios of LDL-C/HDL-C and TC/HDL-C. In the myocardial cell, white blood cell, vascular smooth muscle cell, and endothelial cell, Polydatin can inhibit ICAM-1 expression, elevate Ca2+, weaken white blood cell-endothelial cell adhesion, and activate KATP channels.

Angulatin E serves as an active component in the synthesis of celangulin TC [1].

TC11 (1H-Isoindole-1,3(2H)-dione, 5-amino-2-[2,6-bis(1-methylethyl)phenyl]-TC11) is a potent inhibitor of tumor cell proliferation and an inducer of apoptosis via activation of caspase-3, 8 and 9.

TC-E 5008 is a selective inhibitor of mutant isocitrate dehydrogenase 1 (mIDH1).

H-Tyr-Phe-OH (L-Tyrosyl-L-phenylalanine) can be used as the biomarker to distinguish benign thyroid nodules (BTN) from thyroid cancer (TC). H-Tyr-Phe-OH is an orally active Angiotensin-converting enzyme inhibitor with the 48% inhibiton rate at 50 μM. H-Tyr-Phe-OH shows xanthine oxidase inhibitory activity(uric acid lowering) that acts as regulator of IL-8 production in neutrophil-like cells [1] [2] [3] [4].

TC-G 1005 is a potent and selective GPBA agonist (EC50 :0.72 nM; hTGR5). Selective for TGR5 over FXR (farnesoid X receptor). Increases plasma GLP-1 levels and reduces blood glucose in mice. Orally available.

PTP1B/AKR1B1-IN-1 is a dual inhibitor targeting protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), exhibiting inhibitory potency with IC50s of 0.06 μM for PTP1B and 4.3 μM for AKR1B1. Additionally, it inhibits T-cell protein tyrosine phosphatase (TC-PTP) with an IC50 of 9 μM. This compound acts as an insulin-mimetic in murine myoblasts and diminishes AKR1B1-mediated sorbitol accumulation, contributing to the management of blood glucose levels and the inhibition of type 2 diabetes mellitus (T2DM) development [1].

Vandetanib Fumarate is an orally available tyrosine kinase inhibitor. Vandetanib Fumarate works by blocking RET (REarranged during Transfection), vascular endothelial growth factor receptor (VEGFR-2, VEGFR-3), and epidermal growth factor receptor and to a

PBD dimer-2 (compound 2c), a C8-linked pyrrolobenzodiazepine dimer, has the capability to span an extra base pair and cross-link the 5′-Pu-GA(T/A)TC-Py sequence. It serves as a potential payload for antibody–agent conjugates (ADCs) and is under research for cancer treatments [1] [2].

Selective histone demethylase KDM2/7 subfamily inhibitor

TC-SP 14, also known as compound 14, is a highly active and potent S1P1 agonist with oral bioavailability. It exhibits an EC50 value of 0.042 μM, indicating its strong binding affinity to the S1P1 receptor. Notably, its interaction with the S1P3 receptor is minimal, as evidenced by an EC50 value of 3.47 μM. TC-SP 14 demonstrates significant pharmacological effects, including a marked reduction in blood lymphocyte counts and the attenuation of delayed type hypersensitivity response to antigen challenge [1].

TC-Mps1-12 is an effective and selective inhibitor of monopolar spindle 1 (IC50: 6.4 nM) .