L82 is a selective and uncompetitive DNA ligase 1 (DNA Lig1) inhibitor (hLig1 IC50=12 μM). L82 shows anti-proliferative activity to breast cancer cells[1][2].
Saccharin 1-methylimidazole is an activator for DNA/RNA Synthesis.
3,7,4'-Trihydroxyflavone, isolated from Rhus javanica var. roxburghiana, is a flavonoid with DNA strand-scission activity[1].
2'-OMe-G(ibu) Phosphoramidite is a modified phosphoramidite monomer, which can be used for the oligonucleotide synthesis.
DMT-dC(bz) Phosphoramidite-13C9,15N3 is the 13C and 15N labeled DMT-dC(bz) Phosphoramidite[1]. DMT-dC(bz) Phosphoramidite is typically used in the synthesis of DNA[2].
6-Hydroxy-DOPA is a selective and effective allosteric inhibitor of the RAD52 ssDNA binding domain. 6-Hydroxy-DOPA can be used for the research of cancer[1].
S-(N-PhenethylthiocarbaMoyl)-L-cysteine, a anticarcinogenic agent, has antileukaemic activity with a GC50 value of 336 nM. S-(N-PhenethylthiocarbaMoyl)-L-cysteine inhibits DNA synthesis in HL60 cells [1].
Xanthopterin hydrate, an unconjugated pteridine compound, is the main component of the yellow granule in the Oriental hornet bear wings, produces a characteristic excitation/emission maximum at 386/456 nm[2]. Xanthopterin hydrate(XPT) causes renal growth and hypertrophy in rat[1].Xanthopterin hydrate inhibits RNA synthesis[4].
DMT-2'O-MOE-rG(ib) Phosphoramidite (1g), belonging to the amide family of trivalent phosphate H3PO3, is a derivative of nucleotides and guanosine and can be used in the stereochemical synthesis of phosphorothioate oligonucleotides[1].
Dideoxy-amanitin (compound 2), an α-Amanitin (HY-19610) derivative, is a potent and selective RNA polymerase II allosteric inhibitor with an IC50 value of 74.2 nM[1].
DMT-2'-OMe-dA(bz) phosphoramidite is a phosphoramidite that can be used in the synthesis of oligonucleotides.
Rifalazil (KRM-1648; ABI-1648), a rifamycin derivative, inhibits the bacterial DNA-dependent RNA polymerase and kills bacterial cells by blocking off the β-subunit in RNA polymerase[1]. Rifalazil (KRM-1648; ABI-1648) is an antibiotic, exhibits high potency against mycobacteria, gram-positive bacteria, Helicobacter pylori, C. pneumoniae and C. trachomatis with MIC values from 0.00025 to 0.0025 μg/ml[3]. Rifalazil (KRM-1648; ABI-1648) has the potential for the treatment of Chlamydia infection, Clostridium difficile associated diarrhea (CDAD), and tuberculosis (TB)[2].
Datelliptium chloride hydrochloride is a DNA-intercalating agent derived from Ellipticine (HY-15753). Datelliptium chloride hydrochloride is effective in vivo against a variety of murine solid tumors[1][2].
Werner syndrome RecQ helicase-IN-4 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC50 value of 0.06 µM. Werner syndrome RecQ helicase-IN-4 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-4 shows anticancer activity[1].
DNA Gyrase-IN-4 (compound 8p) is a potent DNA gyrase inhibitor, with an IC50 of 0.13 μM. DNA Gyrase-IN-4 shows excellent antibacterial activity against Staphylococcus aureus, Listeria monocytogenes, Salmonella and Escherichia coli, with MIC values of 0.05, 0.05, 0.05, and 8 μg/mL, respectively[1].
DMT-dA(bz) Phosphoramidite is typically used in the synthesis of DNA[1].
Nedaplatin is a derivative of cisplatin and DNA damage agent.Target: OthersNedaplatin(NDP) is a derivative of cisplatin which produced less nausea & vomiting and nephrotoxicity. the effect of NDP on the 7-ethyl-1-hydroxy-CPT (the active form of CPT-11)-induced inhibitory effect on DNA topoisomerase I was examined. The topoisomerase I-inhibitory effect of 7-ethyl-1-hydroxy-CPT was enhanced 10-fold in the presence of NDP at microgram/milliliter concentrations [1]. NDP was developed as a second generation platinum complex. Because it has greater antitumour activity and lower nephrotoxicity than cisplatin (CDDP). At the high-dose of NDP in FN therapy, a reduction of tumour size and long-term tumour-free survival were frequently observed. The survival effect of the combinations of NDP with 5-FU was superior to those of the combination of CDDP with 5-FU. In conclusion, the sequence-dependent antitumour efficacy and toxicity of the combination of NDP or CDDP with 5-FU was demonstrated in this study, and FN therapy appeared to be the most efficient regimen as a clinical therapy [2].
Deoxythymidine-5'-triphosphate (dTTP) trisodium salt is one of the four natural deoxynucleotides. Deoxythymidine-5'-triphosphate trisodium salt is used for the biosynthesis of deoxyribonucleic acid by DNA polymerase and reverse transcriptase[1].
Simeprevir (TMC435; TMC435350) sodium is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir sodium inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir sodium also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir sodium inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses[1][4].
TH588 hydrochloride is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1(IC50= 5 nM) in cells.IC50 value: 5 nM [1]Target: MTH1 inhibitorTH588 is highly selective towards MTH1, with no relevant inhibition of other members of the nudix protein family or a panel of 87 enzymes, GPCRs, kinases, ion channels and transporter. TH588 has been shown to selectively kill a variety of cancer cell lines and with in vivo activity shown for TH588 in SW480 colorectal and MCF7 breast tumour xenografts.
NVS-SM2 is a potent, orally active and brain-penetrant SMN2 splicing enhancer with an EC50 of 2 nM for SMN. NVS-SM2 enhances U1-pre-mRNA association. NVS-SM2 promotes exon 7 inclusion and restores normal survival motor neuron (SMN) protein expression. NVS-SM2 can be used for spinal muscular atrophy (SMA) research[1][2].
5'-O-DMT-N6-ibu-dA can be used in the synthesis of oligodeoxyribonucleotides[1].
5'-O-TBDMS-dT is a nucleoside with protective and modification effects.
DMT-dA(bz) Phosphoramidite-13C10,15N5 is the 13C and 15N labeled DMT-dA(bz) Phosphoramidite[1]. DMT-dA(bz) Phosphoramidite is typically used in the synthesis of DNA[2].
hDHODH-IN-14 (compound 14) is a human dihydroorotate dehydrogenase (hDHODH) inhibitor with an IC50 of 0.469 μM[1].
3'-F-3'-dA(Bz)-2'-Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
GS-443902 trisodium (GS-441524 triphosphate trisodium) is a potent viral RNA-dependent RNA-polymerases (RdRp) inhibitor with IC50s of 1.1 µM, 5 µM for RSV RdRp and HCV RdRp, respectively. GS-443902 trisodium is the active triphosphate metabolite of Remdesivir (GS-5734)[1][2].
ddGTP (2′,3′-Dideoxyguanosine 5′-triphosphate) is one of 2',3'-dideoxyribonucleoside 5'-triphosphates (ddNTPs) that acts as chain-elongating inhibitor of DNA polymerase for DNA sequencing[1].
CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC50 of 0.9 μM for TAF1, and a Kd of 1.8 μM for TAF1 (2).
2,4-D-d5 is the deuterium labeled 2,4-D[1]. 2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development[2].