tnp

TNP (IP3K Inhibitor) is a cell-permeable inhibitor of IP6K1 and IP3K, with IC 50 values of 0.55 μM and 10.2 μM for IP6K1 and IP3K, respectively. TNP binds to the ATP-binding sites of both enzymes [1].

TNP-470 is a methionine aminopeptidase-2 inhibitor and an angiogenesis inhibitor.

TNP-ATP is an antagonist of purinergic P2Y1, P2X3, and P2X2/3 receptors, exhibiting IC50 values of 6, 0.9, and 7 nM, respectively, in HEK293 cells expressing human receptors. It reduces acetic acid-induced calcium flux in 1321N1 cells expressing P2X3 and P2X2/3 receptors with IC50 values of 100 and 62 nM, respectively. TNP-ATP also dose-dependently alleviates acetic acid-induced writhing responses in a visceral pain model in mice, with an ED50 of 6.35 µmol/kg.

TNP-β-L-GTP tetrasodium is a fluorescent GTP analog utilized in the study of binding kinetics and affinity of GTP-binding proteins, such as G proteins and GTPases. This compound, which carries a TNP fluorescent group, exhibits changes in fluorescence intensity upon protein binding, enabling quantitative analysis.

Tnp 351 is a novel antifolate drug being assessed for chemotherapy of lung cancer.

TNP-ATP, a derivative of ATP, acts as an antagonist to the purinergic P2Y1, P2X3, and P2X2/3 receptors, demonstrating selectivity by showing lower inhibitory concentrations (IC50 = 6, 0.9, 7 nM, respectively) compared to the P2X2, P2X4, and P2X7 receptors (IC50 = 2, 15.2, >30 µM, respectively) in HEK293 cells expressing these human receptors. It effectively diminishes acetic acid-induced calcium influx in 1321N1 cells targeting P2X3 and P2X2/3 receptors (IC50 = 100 and 62 nM, respectively) and alleviates pain in a mouse model of visceral pain (ED50 = 6.35 µmol/kg). Moreover, TNP-ATP exhibits a notable fluorescence characteristic, with an emission peak at 547 nm after excitation at 403 nm, which enhances four-fold and shifts to 538 nm when bound to the insulin-degrading enzyme (IDE).

TNP-GTP, a fluorescent derivative of guanosine 5'-triphosphate (GTP), essential for protein synthesis and gluconeogenesis, exhibits an emission peak at 552 nm when excited at 410 nm in water. Its fluorescence intensity increases and emission peaks shift to 544 nm and 532 nm in 40% and 80% N,N-dimethylformamide, respectively, due to the solvent's lower polarity compared to water. As a potent inhibitor of glutamate dehydrogenase (Ki = 2.7 μM), TNP-GTP enhances fluorescence and shifts its emission to 545 nm upon binding to this enzyme, a process reversible by GTP addition. Additionally, it serves as an antagonist to purinergic P2X2 and P2X2/3 receptors (IC50s = 0.4 and 1.2 nM, respectively) and selectively inhibits rat soluble guanylyl cyclase (sGC; Ki = 11 nM) over bovine liver glutamate dehydrogenase (GDH; Ki = 2.7 µM) and the calmodulin-dependent B. pertussis adenylyl cyclase (AC) toxin, with inhibition constants of 20 µM and 320 µM in the presence of manganese and magnesium, respectively.

TNP-GTP tetrasodium is a fluorescently labeled GTP derivative. It acts as an inhibitor of glutamate dehydrogenase (Ki = 2.7 μM) and serves as an antagonist for purinergic P2X2 and P2X2/3 receptors with IC50 values of 0.4 and 1.2 nM, respectively. Additionally, TNP-GTP tetrasodium inhibits rat soluble guanylyl cyclase (Ki = 1.1 nM).

P2X receptor antagonist

8-Bromo TNP-ITP (8-Bromo TNP-Inosine 5'-triphosphate) tetrasodium is an analog of Inosine-5'-triphosphate trisodium salt.

2-Chloro TNP-ITP (2-Chloro TNP-Inosine 5'-triphosphate) tetrasodium is an analog of Inosine-5'-triphosphate trisodium salt.

PALATINOSE (TNP-470) is a natural occurring disaccharide composed of alpha-1,6-linked glucose and fructose. PALATINOSE has a beneficial effect on liver metabolic functions and might therefore be a good substitute for sucrose as a sweetener.

CBR-2092 is a DNA-directed RNA polymerase and DNA topoisomerase inhibitor. CBR-2092 exhibited rifampin-like potency as an inhibitor of RNA polymerase, was an equipotent (balanced) inhibitor of DNA gyrase and DNA topoisomerase IV, and retained activity against a prevalent quinolone-resistant variant. Studies of mutant strains that exhibited reduced susceptibility to CBR-2092 further substantiated RNA polymerase as the primary cellular target of CBR-2092, with DNA gyrase and DNA topoisomerase IV being secondary and tertiary targets, respectively, in strains exhibiting preexisting rifampin resistance.

TTNPB (Ro 13-7410,AGN-191183), a potent RAR agonist, inhibits binding of [3H]tRA of human RARα (IC50: 5.1 nM), β (IC50: 4.5 nM), and γ (IC50: 9.3 nM), respectively.

BTNPO is a unimolecular two-photon fluorescent probe that is highly sensitive and selective for detecting peroxynitrite (ONOO^-). It exhibits excellent photostability and cell permeability, making it suitable for biological imaging applications. In the presence of peroxynitrite, BTNPO undergoes a significant fluorescence enhancement, which allows for real-time monitoring of cellular events.

TTNPB-CoA (TTNPB-coenzyme A) is a derivative of coenzyme A.

A-849519 is a reversible inhibitor of MetAP2 that has demonstrated anti-angiogenesis and anticancer activity in a number of in vitro and in vivo models. In this study, we evaluated the anticancer activity of A-849519 in a modified Dunning model of androgen-independent prostate cancer and compared its efficacy with TNP-470, an established MetAP2 inhibitor.

Rifasutenizol (TNP-2198) is an orally bioavailable, dual-targeted antibacterial agent with potent effectiveness against both microaerophilic and anaerobic bacterial pathogens [1].

8-Mercaptoguanosine acts as an immunoadjuvant influencing the in vivo antibody response to the T-cell-independent antigen TNP-Ficoll. It boosts IgG1, IgG2, and IgG3 antibody responses without affecting IgM responses. Additionally, it enhances responses to weak antigens like pneumococcal polysaccharide and restores reactions in immunodeficient xid mice unresponsive to TNP-Ficoll.

Fumagillol is a direct precursor of the potent angiogenesis inhibitors [TNP-470] and (fumagillin).