5'-GTP trisodium salt hydrate, an activator of the signal-transducing G proteins, serves as a precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA.
Galidesivir triphosphate is a substrate for viral RNA-dependent RNA polymerase (RDRP), resulting in termination of viral RNA replication and thus serves as an antiviral. Galidesivir triphosphate inhibits HCV NS5B RNA polymerase activity and protects mice against Ebola. Galidesivir triphosphate (Immucillin-A triphosphate) is converted by the prodrug Galidesivir.
NHC-triphosphate is a weak alternative substrate for the viral polymerase and changes the mobility of the product in polyacrylamide electrophoresis gels.
(+)-Carbovir triphosphate is an active metabolite of Abacavir. It was used to study the molecular mechanism of inhibition and drug resistance for HIV-1 reverse transcriptase.
4'-Azidothymidine 5'-triphosphate exerts selectively action on both reverse transcriptase of human immunodeficiency virus type 1 and human DNA polymerases alpha and beta.
3'-Deoxyuridine-5'-triphosphate (3'-dUTP) is a nucleotide analogue that inhibits DNA-dependent RNA polymerases I and II. 3'-Deoxyuridine-5'-triphosphate strongly and competitively inhibits the incorporations of UTP into RNA with a Ki value of 2.0 μM[1]. 3'-Deoxyuridine-5'-triphosphate (3'-dUTP) is synthesized starting from cordycepin in good yield. 3'-Deoxyuridine-5'-triphosphate strongly and competitively inhibits the incorporations of UTP into RNA by the RNA polymerases. 3'-Deoxyuridine-5'-triphosphate will be useful in studies at the molecular level on the relationship of template and substrate in RNA synthesis with chromatin, isolated nuclei or permeable cells, because it does not have any effect on poly (rA) synthesis[1]. [1]. M Saneyoshi, et al. Inhibitory Effects of 3'deoxycytidine 5'-triphosphate and 3'-deoxyuridine 5'-triphosphate on DNA-dependent RNA Polymerases I and II Purified From Dictyostelium Discoideum Cells. Nucleic Acids Res. 1981 Jul 10;9(13):3129-38.
D-myo-Inositol-1,4,6-phosphate (Ins(1,4,6)-P3) is a member of the inositol phosphate (InsP) family that play critical roles as small, soluble second messengers in the transmission of cellular signals. The most studied InsP, Ins(1,4,5)-P3, is a second messenger produced in cells by phospholipase C (PLC)-mediated hydrolysis of phosphatidylinositol-4,5-biphosphate. Binding of Ins(1,4,5)-P3 to its receptor on the endoplasmic reticulum results in opening of the calcium channels and an increase in intracellular calcium. Ins(1,4,6)-P3 (tested as the meso compound) is 9-fold less potent than Ins(1,4,5)-P3 at initiating Ca2+ release when injected into Xenopus oocytes.
The inositol phosphates are a family of mono- to poly-phosphorylated compounds that act as messengers, regulating cellular functions including cell cycling, apoptosis, differentiation, andmotility. D-myo-Inositol-1,5,6-triphosphate is an intermediate compound, produced by the dephosphorylation of various inositol-tetrakisphosphate forms. The triphosphate can be further metabolized to produce inositol-biphosphate mediators. The biological roles of D-myo-inositol-1,5,6-triphosphate remain to be determined.
Ins(1,4,5)P3 is an isomer of the biologically important D-myo-inositol-1,4,5-triphosphate. Unlike its isomer, Ins(1,4,5)P3 does not evoke a rise in intracellular calcium when added to cells. It is not known if Ins(1,4,5)P3 can act as a competitive inhibitor of biologically-active inositol phosphates.
AZT triphosphate TFA (3'-Azido-3'-deoxythymidine-5'-triphosphate TFA) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TFA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TFA also inhibits the DNA polymerase of HBV. AZT triphosphate TFA activates the mitochondria-mediated apoptosis pathway[1][2][3]. Treatment with 100 μM Zidovudine (AZT) for 48h disrupts the mitochondrial tubular network via accumulation of AZT triphosphate (AZT-TP) in H9c2 cells. AZT triphosphate accumulation causes downregulation of Opa1 and upregulation of Drp1. AZT triphosphate causes mitochondrial dysfunction, increases the production of cytotoxic reactive oxygen species (ROS), and impairs the balance of the mitochondrial quality control system in H9c2 cell model established from rat embryonic myoblasts[1]. [1]. Ryosuke Nomura, et al. Azidothymidine-triphosphate Impairs Mitochondrial Dynamics by Disrupting the Quality Control System. Redox Biol. 2017 Oct;13:407-417. [2]. Takeya Sato, et al. Engineered Human tmpk/AZT as a Novel Enzyme/Prodrug Axis for Suicide Gene Therapy. Mol Ther. 2007 May;15(5):962-70. [3]. K Y Hostetler, et al. Enhanced Oral Absorption and Antiviral Activity of 1-O-octadecyl-sn-glycero-3-phospho-acyclovir and Related Compounds in Hepatitis B Virus Infection, in Vitro. Biochem Pharmacol. 1997 Jun 15;53(12):1815-22.
2'-Deoxyadenosine-5'-triphosphate (dATP) is a purine nucleotide and derivative of the nucleic acid adenosine 5'-triphosphate .1dATP is a substrate for DNA polymerase in the synthesis of DNA.2It is a noncompetitive inhibitor of ribonucleotide reductases, which provides feedback inhibition during DNA synthesis.1dATP has commonly been used in DNA synthesis, sequencing, and labeling in research applications.3,4dATP accumulates in adenosine deaminase deficiency, a disorder characterized by mutations in the gene for adenosine deaminase, the enzyme that catalyzes the deamination of adenosine and deoxyadenosine.5 1.Berg, J.M., Tymoczko, J.L., and Stryer, L.Key steps in nucleotide biosynthesis are regulated by feedback inhibitionBiochemistry(2002) 2.Berg, J.M., Tymoczko, J.L., and Stryer, L.DNA is replicated by polymerases that take instructions from templatesBiochemistry(2002) 3.Cadwell, R.C., and Joyce, G.F.Randomization of genes by PCR mutagenesisPCR Methods Appl.2(1)28-33(1992) 4.Steffens, D.L., Jang, G.Y., Sutter, S.L., et al.An infrared fluorescent dATP for labeling DNAGenome Res.5(4)393-399(1995) 5.Flinn, A.M., and Gennery, A.R.Adenosine deaminase deficiency: A reviewOrphanet J. Rare Dis.13(1)65(2018)