product summary
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company name :
Tocris Bioscience
product type :
chemical
product name :
PDD 00017273
catalog :
5952/1
quantity :
1 mg (also 10 mg)
price :
160 USD
more info or order :
citations: 18
Reference
Est xe8 ve P, Sen S, Vishnu U, Ruse C, Chin H, Pradhan S. Poly ADP-ribosylation of SET8 leads to aberrant H4K20 methylation in mammalian nuclear genome. Commun Biol. 2022;5:1292 pubmed publisher
Giansanti C, Manzini V, Dickmanns A, Dickmanns A, Palumbieri M, Sanchi A, et al. MDM2 binds and ubiquitinates PARP1 to enhance DNA replication fork progression. Cell Rep. 2022;39:110879 pubmed publisher
Vaitsiankova A, Burdova K, Sobol M, Gautam A, Benada O, Hanzlikova H, et al. PARP inhibition impedes the maturation of nascent DNA strands during DNA replication. Nat Struct Mol Biol. 2022;29:329-338 pubmed publisher
Li J, M Saville K, Ibrahim M, Zeng X, McClellan S, Angajala A, et al. NAD+ bioavailability mediates PARG inhibition-induced replication arrest, intra S-phase checkpoint and apoptosis in glioma stem cells. NAR Cancer. 2021;3:zcab044 pubmed publisher
Matanes E, L xf3 pez Ozuna V, Octeau D, Baloch T, Racovitan F, Dhillon A, et al. Inhibition of Poly ADP-Ribose Glycohydrolase Sensitizes Ovarian Cancer Cells to Poly ADP-Ribose Polymerase Inhibitors and Platinum Agents. Front Oncol. 2021;11:745981 pubmed publisher
Khanam T, Mu xf1 oz I, Weiland F, Carroll T, Morgan M, Borsos B, et al. CDKL5 kinase controls transcription-coupled responses to DNA damage. EMBO J. 2021;40:e108271 pubmed publisher
Paes Dias M, Tripathi V, van der Heijden I, Cong K, Manolika E, Bhin J, et al. Loss of nuclear DNA ligase III reverts PARP inhibitor resistance in BRCA1/53BP1 double-deficient cells by exposing ssDNA gaps. Mol Cell. 2021;81:4692-4708.e9 pubmed publisher
Demin A, Hirota K, Tsuda M, Adamowicz M, Hailstone R, Brazina J, et al. XRCC1 prevents toxic PARP1 trapping during DNA base excision repair. Mol Cell. 2021;81:3018-3030.e5 pubmed publisher
Genois M, Gagné J, Yasuhara T, Jackson J, Saxena S, Langelier M, et al. CARM1 regulates replication fork speed and stress response by stimulating PARP1. Mol Cell. 2021;81:784-800.e8 pubmed publisher
Gatti M, Imhof R, Huang Q, Baudis M, Altmeyer M. The Ubiquitin Ligase TRIP12 Limits PARP1 Trapping and Constrains PARP Inhibitor Efficiency. Cell Rep. 2020;32:107985 pubmed publisher
Kalasová I, Hailstone R, Bublitz J, Bogantes J, Hofmann W, Leal A, et al. Pathological mutations in PNKP trigger defects in DNA single-strand break repair but not DNA double-strand break repair. Nucleic Acids Res. 2020;48:6672-6684 pubmed publisher
Zhou B, Yan J, Guo L, Zhang B, Liu S, Yu M, et al. Hepatoma cell-intrinsic TLR9 activation induces immune escape through PD-L1 upregulation in hepatocellular carcinoma. Theranostics. 2020;10:6530-6543 pubmed publisher
Dutta P, Paico K, Gomez G, Wu Y, Vadgama J. Transcriptional Regulation of CCL2 by PARP1 Is a Driver for Invasiveness in Breast Cancer. Cancers (Basel). 2020;12: pubmed publisher
Houl J, Ye Z, Brosey C, Balapiti Modarage L, Namjoshi S, Bacolla A, et al. Selective small molecule PARG inhibitor causes replication fork stalling and cancer cell death. Nat Commun. 2019;10:5654 pubmed publisher
Keuss M, Hjerpe R, Hsia O, Gourlay R, Burchmore R, Trost M, et al. Unanchored tri-NEDD8 inhibits PARP-1 to protect from oxidative stress-induced cell death. EMBO J. 2019;38: pubmed publisher
Ando Y, Elkayam E, McPherson R, Dasovich M, Cheng S, Voorneveld J, et al. ELTA: Enzymatic Labeling of Terminal ADP-Ribose. Mol Cell. 2019;73:845-856.e5 pubmed publisher
Moore S, Berger N, Luijsterburg M, Piett C, Stanley F, Schräder C, et al. The CHD6 chromatin remodeler is an oxidative DNA damage response factor. Nat Commun. 2019;10:241 pubmed publisher
Hanzlikova H, Kalasová I, Demin A, Pennicott L, Cihlarova Z, Caldecott K. The Importance of Poly(ADP-Ribose) Polymerase as a Sensor of Unligated Okazaki Fragments during DNA Replication. Mol Cell. 2018;71:319-331.e3 pubmed publisher
product information
brand :
Tocris
MasterCode :
5952
SKU :
5952/1
product name :
PDD 00017273
target :
PARG Inhibitors
category :
Small Molecules
unit size :
1 mg (also 10 mg)
purity :
98%
observed molecular weight :
514.62
url print :
?utm_source=biocompare&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
PDD 00017273 is a potent and selective poly (ADP ribose) glycohydrolase (PARG) inhibitor (IC50 = 26 nM). Exhibits 350-fold selectivity for PARG over a panel of ion channels, enzymes and receptors, including PARP1 and ARH3. Maintains PAR chains and induces DNA double-stranded breaks in cells following DNA damage. Decreases colony formation of ZR-75-1 BRCA1 WT cells and inhibits cancer cell survival. Cell permeable.
extended description :
Potent and selective PARG inhibitor; cell permeable
chemical name text :
1-[(1,3-Dimethyl-1H-pyrazol-5-yl)methyl]-1,2,3,4-tetrahydro-N-(1-methylcyclopropyl)-3-[(2-methyl-5-thiazolyl)methyl]-2,4-dioxo-6-quinazolinesulfonamide
formula :
C 23 H 26 N 6 O 4 S 2
formula text :
C23H26N6O4S2
cas num :
1945950-21-9
USD :
160 USD
product details :
Potent and selective PARG inhibitor; cell permeable
storage :
Store at -20°C
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK