3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) is an improved dopamine analog cytotoxic and inhibits DNA polymerase activity in melanoma cells[2]. 3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) displays growth inhibitory activity in melanoma cell lines with varying degrees of tyrosinase activity[2].
TH287 is a potent inhibitor of MTH1 (NUDT1) with an IC50 value of 0.8 nM, less potent for MTH2, NUDT5, NUDT12, NUDT14, and NUDT16.IC50 value: 0.8 nM [1]Target: MTH1 inhibitorTH287 is considered a new target for cancer therapy. TH287 is highly selective towards MTH1, with no relevant inhibition of other members of the nudix protein family. TH287 has been shown to selectively kill a variety of cancer cell lines, but is rapidly metablized, so not as useful for in vivo studies.
SCR130 is a SCR7-based DNA nonhomologous end-joining (NHEJ) inhibitor. SCR130 inhibits the end-joining of DNA in a Ligase IV-dependent manner. SCR130 is specific to Ligase IV, and shows minimal or no effect on Ligase III and Ligase I mediated joining. SCR130 induces cell apoptosis and has anticancer activity[1].
Deoxycytidine triphosphate-d14 (dCTP-d14 dilithium; 2′-Deoxycytidine-5′-triphosphate-d14) dilithium is deuterium labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
5'-O-DMT-rU is a modified nucleoside and can be used to synthesize RNA.
Erythromycin stearate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin stearate binds to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid[1][2]. Erythromycin stearate also exhibits antitumor and neuroprotective effect in different fields of research[3][4].
Triciribine is a DNA synthesis inhibitor, also inhibits Akt and HIV-1/2 with IC50 of 130 nM, and 0.02-0.46 μM, respectively.
Tirandamycin A, an antibiotic, is a bacterial RNA polymerase inhibitor. Tirandamycin A has antiamoebic and antibacterial properties[1][2].
5'-Cholesteryl-TEG phosphoramidite is a phosphoramidite that can be used in the synthesis of oligonucleotides.
L82-G17 is an uncompetitive DNA ligase I (Lig I)-selective inhibitor. L82-G17 inhibits the third step of the ligation reaction, phosphodiester bond formation. L82-G17can be used as a probe of the catalytic activity[1].
IMP-1088 is a potent, selective human N-myristoyltransferase with IC50 of less than 1 nM for both HsNMT1 and HsNMT2, inhibits Rhinoviruses (RVs) capsid myristoylation in cells; pharmacological and rapidly inhibits host-cell N-myristoylation, potently and efficiently block RV replication (IC50=17 nM) without cytotoxicity; potently blocks a key step in viral capsid assembly, to deliver a low nanomolar antiviral activity against multiple RV strains, poliovirus and foot and-mouth disease virus, and protection of cells against virus-induced killing.
5'-O-TBDMS-dU can be used in the synthesis of oligoribonucleotides[1].
BMH-22, a benzonaphthyridin, is a RNA polymerase I (Pol I) transcription inhibitor independent of p53 function. BMH-22 causes reorganization of nucleolar marker proteins consistent with segregation of the nucleolus. BMH-22 destabilizes RPA194 in a proteasome-dependent manner and inhibits nascent rRNA synthesis and expression of the 45S rRNA precursor. BMH-22 shows potent anticancer activity across many tumor types[1].
CTP Synthetase-IN-1 is a potent, orally active cytidine 5'-triphosphate synthetase (CTPS) inhibitor with IC50s of 32 nM and 18 nM for human CTPS1 and human CTPS2, respectively. CTP Synthetase-IN-1 has anti-inflammatory effects[1].
ddCTP is one of 2',3'-dideoxyribonucleoside 5'-triphosphates (ddNTPs) that acts as chain-elongating inhibitor of DNA polymerase for DNA sequencing[1].
RG7800 a small molecule SMN2 splicing modifier to enter human clinical trials to treat spinal muscular atrophy.
DHODH-IN-15 (Compound 7b) is a hydroxyfurazan analog of A771726. DHODH-IN-15 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 11 μM for rat liver DHODH. DHODH-IN-15 can be used for rheumatoid arthritis[1].
Synucleozid (NSC 377363) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein (IC50=1.5 μM). Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease[1].
5-Propargylamino-ddCTP, a nucleoside molecule that can be used to synthesis of cyanine dye-nucleotide conjugate which is used in nucleic acid labeling or sequence analysis[1].
Nimustine hydrochloride (ACNU) is a DNA cross-linking and DNA alkylating agent, which induces DNA replication blocking lesions and DNA double-strand breaks and inhibits DNA synthesis, commonly used in chemotherapy for glioblastomas[1][2][3].
Rifaquizinone (CBR-2092) is a Rifamycin-Quinolone Hybrid Antibiotic. Rifaquizinone inhibits wild-type S. aureus RNA polymerase with an IC50 of 34 nM. Rifaquizinone is effective against S. aureus infections, with MICs ranged from 0.008 to 0.5 μg/mL for 300 clinical isolates of staphylococci and streptococci[1][2].
BMH-21 is a small molecule DNA intercalator that binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription; does not cause phosphorylation of H2AX.IC50 value: 10-90 nM(RPA195 IC50) [1]Target: RNA Pol I inhibitorin vitro: BMH-21 effects on the nucleolar stress response were independent of major DNA damage associated PI3-kinase pathways, ATM, ATR and DNA-PKcs. BMH-21 is a chemically unique DNA intercalator that has high bioactivity towards Pol I inhibition without activation or dependence of DNA damage stress [1].
5'-O-DMT-Bz-Rc is a modified nucleoside and can be used to synthesize DNA or RNA.
Foscarnet trisodium hexahydrate (Trisodium phosphonatoformate hexahydrate) is a viral DNA polymerase activity inhibitor, leading to reversible suppression of viral replication. Foscarnet trisodium hexahydrate is an antiherpesvirus agent used in cytomegalovirus retinitis[1][2][3].
AV-153, a 1,4-dihydropyridine (1,4-DHP) derivative, is an antimutagenic. AV-153 intercalates to DNA in a single strand break and reduces DNA damage, stimulates DNA repair in human cells in vitro. AV-153 interacts with thymine and cytosine and has an influence on poly(ADP)ribosylation. AV-153 has anti-cancer activity[1][2][3].
Aphidicolin is an inhibitor of DNA polymerase α and δ, prevents mitotic cell division by interfering with the activity of DNA polymerase[1].Aphidicolin is an antibiotic produced by the mold Cephalosporium aphidicola. Aphidicolin is a potent inhibitor of cellular deoxyribonucleic acid synthesis and inhibits the growth of herpes simplex virus[2].Aphidicolin potentiates apoptosis induced by arabinosyl nucleosides in a human promyelocytic leukemia cell line[3].
Temozolomide acid is a carboxylic acid derivative of Temozolomide. Temozolomide is a DNA alkylating agent, methylating the guanine and adenine bases of DNA, causing breaks in DNA double strand, cell cycle arrest, and eventually cell death. Temozolomide acid has an activity similar to the parent compound Temozolomide with the same anticancer activity[1].
Orotidine 5'-monophosphate trisodium is a pyrimidine nucleotide. Orotidine 5'-monophosphate trisodium is synthesized via the de novo synthesis pathway for DNA synthesis in a large number of microorganisms including M. tuberculosis, S. cerevisiae, S. typhimurium and P. falciparum to name a few. The synthesis of orotidine 5'-monophosphate trisodium uses phosphoribosyl pyrophosphate (PRPP) and orotic acid (OA) as the substrates catalyzed by orotate phosphoribosyltransferase (OPRT)[1].
Erythromycin lactobionate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin lactobionate binds to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid[1][2]. Erythromycin lactobionate also exhibits antitumor and neuroprotective effect in different fields of research[3][4].
Antipain dihydrochloride is a protease inhibitor isolated from Actinomycetes. Antipain dihydrochloride inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations. Antipain dihydrochloride restricts uterine DNA synthesis and function in mice[1][2][3][4].