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PARP inhibitor
PJ34 is a novel potent specific inhibitor of PARP-l/2 with EC50 of 20 nM.- Tim J Wigle, .et al. , Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
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HDAC inhibitor
Resminostat hydrochloride is a potent inhibitor of HDAC1/3/6(IC50=43-72 nM); less potent to HDAC8 with IC50 of 877 nM. -
SIRT1 Activator
SRT 1720 is a selective activator of human SIRT1 (EC1.5 = 0.16 μM) versus the closest sirtuin homologues, SIRT2 and SIRT3 (SIRT2: EC1.5 = 37 uM; SIRT3: EC1.5 > 300 uM).- Lanlan Yin, .et al. , Placenta, 2024, May:150:52-61 PMID: 38593636
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DNA polymerase Inhibitor
Valacyclovir is an antiviral drug used in the management of herpes simplex, herpes zoster, and herpes B. -
Topoisomerase inhibitor
Voreloxin Hcl is a small molecule and a naphthyridine analogue with antineoplastic activity; inhibitor of Topo II. -
RNA polymerase II inhibitor
Oncrasin 1 is a proapoptotic substance. Induces abnormal nuclear aggregation of PKCι and suppressing RNA transcription. -
HDAC Inhibitor
NCH 51 is a cell-permeable prodrug that is intracellularly converted to a potent HDAC inhibitor, with an IC50 of 48 nM. -
PARP-1 inhibitor
BYK204165 is a cell-permeable isoquinolinedione compound that potently and selectively inhibits poly (ADP-ribose) polymerase 1 (PARP1). -
PARP1 Inhibitor
EB 47 is a potent inhibitor of PARP1 with IC50 of 45 nM. -
DNA/RNA polymerase Inhibitor
Mithramycin A is an antibiotic DNA/RNA polymerase and DNA binding transcriptional inhibitor observed to facilitate TNF-?? and Fas-ligand induced apoptosis. -
HDAC6 inhibitor
TCS HDAC6 20b, selective inhibitor of histone deacetylase 6 (HDAC6). Inhibits HCT116 growth in combination with taxol. Also inhibits growth of MCF-7 cells stimulated by estrogen. -
HDAC inhibitor
R306465 is a novel hydroxamate-based histone deacetylase (HDAC) inhibitor with broad-spectrum antitumour activity against solid and haematological malignancies in preclinical models.- Mari Ishigami-Yuasa, .et al. , Biol Pharm Bull, 2019, 42, 448-452 PMID: 30828077
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GL1 synthase Inhibitor
Genz-123346 free base is an inhibitor of GL1 synthase that blocks the conversion of ceramide to GL1; IC50 for GM1 inhibition is 14 nM. -
HCV Polymerase Inhibitor
VCH-759 is a non-nucleoside inhibitor of HCV RNA-dependent polymerase with sub-micromolar IC50 values versus genotype 1a/1b replicons.- Hassan GS, .et al. , Eur J Med Chem, 2019, Oct 1;184:111747 PMID: 31604164
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TNKS inhibitor
G007-LK displays high selectivity toward tankyrases 1 and 2 with biochemical IC50 values of 46 nM and 25 nM, respectively, and a cellular IC50 value of 50 nM combined with an excellent pharmacokinetic profile in mice,- Dominic B. Bernkopf, .et al. , Nat Commun, 2019, 10:4251 PMID: 31534175
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Trifluridine-tipiracil hydrochloride mixture
TAS-102 is an orally bioavailable combination agent composed of the cytotoxic pyrimidine analog Trifluridine (5-trifluoro-2'-deoxythymidine or TFT) and a thymidine phosphorylase inhibitor (TPI) tipiracil hydrochloride, in a molar ratio of 1.0:0.5 (TFT:TPI), with potential antineoplastic activity,
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anti-inflammatory agent
Neobavaisoflavone, a flavonoid, is isolated from the seeds of Psoralea corylifolia. Neobavaisoflavone exhibits anti-inflammatory, anti-cancer and anti-oxidation activities. Neobavaisoflavone inhibits DNA polymerase at moderate to high concentrations. Neobavaisoflavone also inhibits platelet aggregation. -
HDAC/ACE inhibitor
Sinapinic acid (Sinapic acid) is a phenolic compound isolated from Hydnophytum formicarum Jack. Rhizome, acts as an inhibitor of HDAC, with an IC50 of 2.27 mM, and also inhibits ACE-I activity. Sinapinic acid posssess potent anti-tumor activity, induces apoptosis of tumor cells. -
TNKS2 inhibitor
NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM; > 300 fold selectivity against PARP1 and PARP2. -
ATR inhibitor
AZD6738 is a potent inhibitor of ATR kinase activity with an IC50 of 1 nM against the isolated enzyme and 74 nM against ATR kinase-dependent CHK1 phosphorylation in cells.- Joshua J Deppas, .et al. , Toxicol Appl Pharmacol, 2025, Jul:500:117375
- Erika Nakatsuka, .et al. , Transl Oncol, 2024, Sep 12:50:102119 PMID: 39270525
- Zhiyan Silvia Liu, .et al. , Cancer Res, 2024, Feb 15;84(4):577-597 PMID: 37967363
- Yang Lim, .et al. , Science, 2023, Sep 22;381(6664) PMID: 37590370
- Brian F Kiesel, .et al. , Cancer Chemother Pharmacol, 2022, Feb;89(2):231-242 PMID: 35066692
- Albert Job, .et al. , Sci Rep, 2020, Nov 3;10(1):18924 PMID: 33144657
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de novo purine synthesis inhibitor
6-Mercaptopurine Monohydrate is a widely used antileukemic agent and immunosuppressive drug that inhibits de novo purine synthesis through incorporation of thiopurine methyltransferase metabolites into DNA and RNA. -
Selective SIRT2 inhibitor
SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM.- Yang Li, .et al. , Neoplasia, 2018, Jul; 20(7): 745-756 PMID: 29925042
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HDAC6 inhibitor
ACY-738 is a potent and selective HDAC6 inhibitor with improved brain bioavailability. ACY-738 inhibits HDAC6 with low nanomolar potency and a selectivity of 60- to 1500-fold over class I HDACs.- Dao Xu, .et al. , Immunohorizons, 2024, Sep 1;8(9):668-678 PMID: 39259207
- Guang Bai, .et al. , Epigenetics of Chronic Pain, 2019, Pages 1-48
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DNA and RNA synthesis activator
Saccharin 1-methylimidazole is considered a general-purpose activator for DNA and RNA synthesis.

