tc 1

σ1 receptor ligand

PTP1B TC-PTP IN-1 is a dual inhibitor of PTP1B and TC-PTP. It can be used as a target protein ligand for the synthesis of the PROTAC DU-14 (PTP1B TC-PTP PROTAC).

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.

nicotinic α7 receptor agonist

TC 14012, a peptidomimetic compound, acts as both an antagonist to the chemokine (C-X-C motif) receptor 4 (CXCR4; IC50 = 2.9 nM) and as an agonist for CXCR7, effectively recruiting β-arrestin in HEK293T cells that express CXCR7 (EC50 = 350 nM). Moreover, it demonstrates significant antiviral activity by reducing the cytopathic effects of HIV in MT-4 cells with an EC50 value of 0.4 nM and inhibiting HIV entry in vitro through a CXCR4-dependent pathway (IC50 = 19.3 nM). Additionally, TC 14012 suppresses chemokine (C-X-C motif) ligand 12 (CXCL12)-induced migration in MDA-MB-231 breast cancer and human umbilical vein endothelial cells (HUVECs) within the 10 to 1,000 nM concentration range. In a mouse model, administration of TC 14012 at 10 mg/kg significantly reduced infarct size following acute myocardial infarction induced by ligation of the left anterior descending (LAD) coronary artery.

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.

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

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

DSPE-PEG(2000)-mannose, a pegylated and mannosylated derivative of 1,2-DSPE, has been employed in both in vitro and in vivo studies for delivering peptides, oligodeoxynucleotides, and siRNA via liposomes and lipid nanoparticles (LNPs). Fluorescently labeled LNPs containing DSPE-PEG(2000)-mannose predominantly accumulate in the liver and spleen of mice, significantly more so than in the brain, lungs, heart, kidneys, and pancreas. In immunization studies, liposomes encapsulating Human Papillomavirus type 16 (HPV16) E7 peptides with CpG oligodeoxynucleotides as an adjuvant led to reduced tumor volume and decreased numbers of CD4+ or CD8+ T cells and angiogenesis within tumors in a mouse lung cancer model using TC-1 cells.

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].

Selective histone demethylase KDM2/7 subfamily inhibitor

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

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.

PTP1B AKR1B1-IN-1 is a dual inhibitor targeting protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), with IC50s of 0.06 μM for PTP1B and 4.3 μM for AKR1B1. It also inhibits T-cell protein tyrosine phosphatase (TC-PTP) with an IC50 of 9 μM. This compound acts as an insulin-mimetic in murine myoblasts, reduces AKR1B1-mediated sorbitol accumulation, and aids in managing blood glucose levels and inhibiting type 2 diabetes mellitus (T2DM) development [1].

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

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].

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.

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.

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.