JH-RE-06, a potent REV1-REV7 interface inhibitor (IC50=0.78 μM; Kd=0.42 μM), targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ. JH-RE-06 sensitizes mouse and human cell lines to Cisplatin, and suppresses tumor progression in mice and prolongs animal survival[1].
YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding to the oncogenic transciption factor EWS-FLI1. YK-4-279 inhibits Ewing's sarcoma family tumor (ESFT) cell growth; YK-4-279 induces apoptosis. IC50 value:Target: RNA Helicase AES-FLI1 is an oncogenic fusion protein found in Ewing’s sarcoma, a family of undifferentiated tumors that occur throughout the body. The binding of RNA helicase A (RHA) to ES-FLI1 promotes its oncogenic function. YK-4-279 is an inhibitor of protein-protein interactions between ES-FLI1 and RHA. At 10 μM, YK-4-279 blocks RHA binding to ES-FLI1 and induces apoptosis of a panel of Ewing’s sarcoma tumor cell lines with IC50 values ranging from 0.5-2 μM. At 1.5 mg per dose, YK-4-279 reduces the growth of Ewing’s sarcoma orthotopic xenografts in mice after treatment with the inhibitor for two weeks.
Sarecycline is an orally effective narrow-spectrum tetracycline derivative antibiotic. Sarecycline has anti-inflammatory activity. Sarecycline inhibits the activity of Gram-positive bacteria and several types of keratobacterium acnes. Sarecycline interferes with tRNA accommodation and tethers mRNA to the 70S ribosome. Sarecycline can be used to study moderate to severe acne[1][2][3][4][5][6].
Guanine-13C is the 13C labeled Guanine[1]. Guanine (2-Aminohypoxanthine) is one of the fundamental components of nucleic acids (DNA and RNA). Guanine is a purine derivative, consisting of a fused pyrimidine-imidazole ring system with conjugated double bonds.
Isopimpinellin, an orally active compound isolated from the roots of Pimpinella saxifrage. Isopimpinellin blocks DNA adduct formation and skin tumor initiation by 7,12-dimethylbenz[a]anthracene. Isopimpinellin possesses anti-leishmania effect[1].
5'-DMTr-dA(Bz)-Methyl phosphonamidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
AV-153 free base, a 1,4-dihydropyridine (1,4-DHP) derivative, is an antimutagenic. AV-153 free base intercalates to DNA in a single strand break and reduces DNA damage, stimulates DNA repair in human cells in vitro. AV-153 free base interacts with thymine and cytosine and has an influence on poly(ADP)ribosylation. AV-153 free base has anti-cancer activity[1][2][3].
Werner syndrome RecQ helicase-IN-3 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-3 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-3 shows anticancer activity[1].
GNE-371 is a potent and selective chemical probe for the second bromodomains of human transcription-initiation-factor TFIID subunit 1 and transcription-initiation-factor TFIID subunit 1-like, with an IC50 of 10 nM for TAF1(2).
Trimidox (VF-233) is a ribonucleotide reductase inhibitor with antileukemic activities. Trimidox inhibits the growth of human promyelocytic leukemia HL-60 cells with an IC50 of 35 μM[1].
Dasabuvir (ABT-333) sodium is a nonnucleoside hepatitis C virus (HCV) polymerase inhibitor. Dasabuvir sodium inhibits RNA-dependent RNA polymerase encoded by the HCV NS5B gene. Dasabuvir sodium inhibits genotype 1a (strain H77) and 1b (strain Con1) replicons, with EC50 values of 7.7 and 1.8 nM, respectively[1].
DNA Gyrase-IN-3 (Compound 28) is a bacterial DNA gyrase B inhibitor with IC50s of 5.41-15.64 µM for E. coli DNA gyrase. Anti-tubercular and antibacterial activity[1].
Crisnatol (BWA770U) is an orally active and anticancer agent, and a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol shows in vitro cytotoxicity against MCF-7 human breast cancer cells, breast cancer cell line (MDA-MB-231), but not normal human skin fibroblasts[1][2][3].
Ac-dA Phosphoramidite is a phosphinamide monomer that can be used in the preparation of oligonucleotides.
ε-Amanitin, a cyclic peptide isolated from a variety of mushroom species, potently binds to and inhibits the activity of RNA polymerase II[1][2].
CeMMEC13 is a potent inhibitor of TAF1 (2) bromodomain, with an IC50 of 2.1 μM.
Albomycin is an inhibitor of aminoacyl-tRNA synthetases with Trojan-horse effect. Albomycin is delivered by iron-chelator portion into bacterial through ferrichrome-specific transporter system. Albomycin combats against a wide range of Gram-positive and Gram-negative bacteria. Albomycin also serves as an efficient iron-scavenger of producer[1].
L-I-OddU, a L-5'-halo- dioxolane nucleoside analogue, is a potent and selective anti-Epstein-Barr virus (EBV) agent with an EC50 value of 0.03μM. L-I-OddU has low cytotoxicity with a CC50 value of 1000 nM. L-I-OddU has antiviral activity by suppressing replicative EBV DNA and viral protein synthesis[1][2].
Crisnatol (BWA770U) mesylate is an orally active and anticancer agent, and a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol mesylate shows in vitro cytotoxicity against human breast cancer cells, but not normal human skin fibroblasts[1][2][3].
3'-DMTr-dA can be used for the synthesis of nucleotides[1].
3'Ome-m7GpppAmpG is a cap analogue for mRNA synthesis in vitro[1].
5-Methylcytosine-d4 is the deuterium labeled 5-Methylcytosine[1]. 5-Methylcytosine is a well-characterized DNA modification, and is also predominantly in abundant non-coding RNAs in both prokaryotes and eukaryotes. 5-Methylcytosine in mRNA is a new epitranscriptome marker inArabidopsis, and that regulation of this modification is an integral part of gene regulatory networks underlying plant development[2].
5'-O-DMT-N4-Ac-2'-F-dC is a modified nucleoside and can be used to synthesize DNA or RNA.
Thymidine-d2 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1
DTP3 TFA is a potent and selective GADD45β/MKK7 inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway[1].
DHODH-IN-12 (Compound 12b) is a Leflunomide derivative and a weak dihydroorotate dehydrogenase (DHODH) inhibitor with a pKa of 5.07[1].
6-Azathymine, a 6-nitrogen analog of thymine, is a potent D-3-aminoisobutyrate-pyruvate aminotransferase inhibitor. 6-Azathymine inhibits the biosynthesis of DNA, and has antibacterial and antiviral activities[1][2][3][4].
5'-DMTr-T-Methyl phosphonamidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
NITD008 is a potent and selective flaviviruse inhibitor which can inhibit Dengue Virus Type 2 (DENV-2) with an EC50 of 0.64 μM.
2'-Azido-2'-deoxyuridine (N3dUrd) is a ribonucleotide reductase inhibitor. 2'-Azido-2'-deoxyuridine has anti-cancer activity[1].