Poly(A) polymerase

Poly(A) polymerase enzymatically adds a polyadenosine tail of 20-200 adenine bases to the 3' end of RNA, a process that involves integrating ATP as AMP. This modification enhances RNA stability and augments mRNA translation efficiency in eukaryotic cells, evidencing the enzyme's high tailing efficiency [1] [2].

Niraparib metabolite M1 (Niraparib carboxylic acid metabolite M1) is the carboxylic acid metabolite of Niraparib. Niraparib is a novel poly (ADP-ribose) polymerase (PARP) inhibitor used in cancer research.

PARPYnD is a potent photoaffinity probe for poly(ADP-ribose) polymerase (PARP) (IC50 values for PARP2, PARP1 and PARP6 are 6, 38 and 230 nM, respectively). PARPYnD labels PARP1 and PARP2 in the cell when an N3 functionalized fluorescent probe is attached and can inhibit isolated PARP6.

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

Benzamide (Amid kyseliny benzoove), an inhibitor of poly(ADP-ribose) polymerase, is a derivative of benzoic acid.

Niraparib metabolite M1 HCl is the active metabolite of Niraparib, as a novel targeted ADP ribose polymerase (PARP) inhibitor, it can competitively inhibit PARP1 and PARP2 to block the DNA repair mechanism of tumor cells and thus effectively inhibit the growth and proliferation, which is commonly used in the study of ovarian cancer, fallopian tube cancer and primary peritoneal cancer, and is commonly used in the study of ovarian, fallopian tube and primary peritoneal cancers.

PARP/PI3K-IN-1 is a novel dual poly (ADP-ribose) polymerase (PARP) and phosphatidylinositol 3-kinase (PI3K) dual inhibitor with anticancer, antitumour and antiproliferative activities for the study of breast, pancreatic and lung cancers.

WD2000-012547 is a selective inhibitor of poly(ADP-ribose)-polymerase (PARP-1) (pKi: 8.221).

Ara-ATP, a structural analogue of ATP, inhibits the activity of poly(A) polymerase by competing with ATP.

MD6a is a melatonin derivative with inhibitory activity against poly(ADP-ribose) polymerase (PARP-1). It maintains protein homeostasis and improves mitochondrial function via the TOR/HSF-1 signaling pathway, providing neuroprotective effects.

DR2313 is a competitive inhibitor of poly(ADP-ribose) polymerase (IC50: 0.20 and 0.24 μM for PARP-1 and PARP-2 respectively). It also has neuroprotective.

CAY10753 is an inhibitor of tankyrase 2 (TNKS2; IC50= 0.3 nM).1It is selective for TNKS2 over TNKS1 (IC50= 6.1 nM), as well as poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 89.6 and 37.8 nM, respectively). CAY10753 inhibits proliferation of DLD-1 colorectal cancer cells when used at a concentration of 1 μM. 1.Tomassi, S., Pfahler, J., Mautone, N., et al.From PARP1 to TNKS2 inhibition: A structure-based approachMed. Chem. Lett.(2020)

CAY10760 is an inhibitor of the protein-protein interaction between RAD51 recombinase and BRCA2 (EC50= 19 μM in a cell-free competitive ELISA).1It decreases homologous recombination by 54% in wild-typeBRCA2-expressing BxPC-3 pancreatic cancer cells when used at a concentration of 20 μM. CAY10760 (20 μM) decreases proliferation of BxPC-3, as well as mutantBRCA2-expressing Capan-1, cancer cells when used alone or in combination with the poly(ADP-ribose) polymerase (PARP) inhibitor olaparib . 1.Bagnolini, G., Milano, D., Manerba, M., et al.Synthetic lethality in pancreatic cancer: Discovery of a new RAD51-BRCA2 small molecule disruptor that inhibits homologous recombination and synergizes with olaparibJ. Med. Chem.63(5)2588-2619(2020)

Benzamide-15N (NSC-3114-15N) is a 15N-labeled Benzamide. Benzamide inhibits poly(ADP-ribose) polymerase (PARP).

pNP-ADPr is a colorimetric substrate used in continuous activity assays for Poly(ADP-ribose) glycohydrolase (PARG) and ADP-ribosyl hydrolase 3 (ARH3), aiding research on poly(ADP-ribose) polymerase (PARP) enzymes.

TIQ-A is a PARP1 inhibitor which involved in DNA single-strand break repair via the base excision repair pathway. PARP1 is triggered by DNA damage and its excessive activation has been proposed as a causative factor in many pathological conditions includi

INO-1001 is a potent, selective poly(ADP-ribose) polymerase (PARP) inhibitor with antitumor activity.INO-1001 is a potent radiosensitization enhancer that uses interference with DNA repair mechanisms to enhance radiation-induced cell killing and necrotic cell death.

A-96649 is a new-type and effective inhibitor. The Ki of A-966492 for PARP1 and PARP2 is 1 nM and 1.5 nM, respectively.

WP-1034 is a novel Jak-Stat inhibitor, which is active against AML blasts. WP-1034 effectively inhibited proliferation of OCIM2 cells and fresh AML samples. WP-1034 caused cell cycle arrest of OCIM2 cells in sub-Go phase. WP-1034 induced apoptosis of OCIM2 cells and that induction of apoptosis involved cleavage of caspase 3 and the DNA repair enzyme poly (adenosine diphosphate [ADP]-ribose) polymerase (PARP).

KU-0058948 is a poly (ADP-ribose) polymerase (PARP) inhibitor that induces cell cycle arrest and apoptosis of primary myeloid leukemic cells and myeloid leukemic cell lines in vitro.

NU1064 is a potent poly(ADP-ribose) polymerase (PARP) inhibitor, which can potentiate the cytotoxicity of a panel of mechanistically diverse anti-cancer agents in L1210 cells. NU1064 potentiated a sublethal concentration of a DNA methylating agent in a concentration-dependent manner.

BIM-46174 is a 5,6,7,8-tetrahydroimidazole [1,2-a] pyrazine derivative that inhibits the heterotrimeric Galpha/Gbetagamma protein complex and has anticancer activity, inhibiting the growth of a large number of human cancer cell lines, inducing caspase-3-dependent cancer cell apoptosis, and inducing poly (ADP-ribose) polymerase cleavage.

NU1085 is a potent poly(ADP-ribose) polymerase (PARP) inhibitors have been developed that potentiate the cytotoxicity of ionizing radiation and anticancer drugs. The biological effects of NU1085 [Ki = 6 nM], in combination with temozolomide (TM) or topotecan (TP) have been studied in 12 human tumor cell lines (lung, colon, ovary, and breast cancer). Cells were treated with increasing concentrations of TM or TP +/- NU1085 (10 microM) for 72 h.

PD-128763 is a poly(ADP-ribose) polymerase inhibitor exhibiting radiosensitising effects, enhancing radiation-induced cell killing in X-ray-irradiated Chinese hamster V79 cells.