-
PARP inhibitor
AG14361 is a potent PARP inhibitor, enhanced TMZ cytotoxicity in MMR(mismatch repair)-proficient / deficient cells.- Vimal Pandey, .et al. , Scientific Reports, 2019, 9, Article number: 5012 PMID: 30899038
- Alendronate is a nitrogen-containing bisphosphonate that is commonly used in the treatment of osteoporosis and other metabolic bone diseases.
-
DNA/RNA Synthesis inhibitor
Bleomycin sulfate is a mixture of the sulfate salts of basic glycopeptide antineoplastic antibiotics isolated from Streptomyces verticillus.- Mai Kanemaru, .et al. , J Dermatol Sci, 2018, Jan;93(1):41-49 PMID: 30655107
-
HDAC inhibitor
JNJ-26481585 (Quisinostat) is a pan-HDAC inhibitor with marked potency toward HDAC1 (IC(50), 0.16 nmol/L).- Minoru Ueda, .et al. , Plant Physiol, 2017, Dec; 175(4): 1760-1773 PMID: 29018096
-
HDAC Inhibitor
LAQ824 (NVP-LAQ824) is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma.- De-Run Chen, .et al. , Appl Mater Today, 2022, 26: 101363
-
HDAC Inhibitor
Trichostatin A (TSA) inhibits the HDACs 1, 3, 4, 6 and 10 with IC50 values around 20 nM.- Goudreault M, .et al. , Research Square, 2021, 22 Nov
- Hiroyuki Imuta, .et al. , Heart Vessels, 2020, Jul 16 PMID: 32676696
- Méndez-Blanco C, .et al. , Cancers (Basel), 2019, Dec 9;11(12). pii: E1984 PMID: 31835431
-
mTOR inhibitor
Torin 2 is a potent and selective mTOR inhibitor (IC50 = 2.1 nM). Displays 800-fold cellular selectivity for mTOR over PI3K (cellular EC50 values are 0.25 and 200 nM for mTOR and PI3K respectively).- Diane Yang, .et al. , Diabetes, 2021, Oct;70(10):2419-2429 PMID: 34344789
-
DNA-PK inhibitor
Compound 401 is a cell-permeable pyrimido-isoquinolinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 280 nM) with ~19-fold selectivity over mTOR (IC50 = 5.3 μM). -
HDAC inhibitor
Romidepsin strongly inhibits HDAC1 and HDAC2 with IC5N/A of 1.6 nM and 3.9 nM, respectively, but is relatively weak in inhibiting HDAC4 and HDAC6 with IC5N/A 25 nM and 79N/A nM, respectively.- Yu-Fang Liu, .et al. , J Biochem Mol Toxicol, 2022, Jun;36(6):e23044 PMID: 35499365
- David Diaz-Carballo, .et al. , Commun Biol, 2021, Mar 3;4(1):276 PMID: 33658617
- Eva Hesping, .et al. , Int J Parasitol Drugs Drug Resist, 2020, 14: 249-256
- Shariful Islam, .et al. , Blood Adv, 2020, 4(20): 5297-5310 PMID: 33108458
- Elena Netchiporouk, .et al. , Oncotarget, 2017, Nov 10; 8(56): 95981-95998 PMID: 29221181
- Ivan V. Litvinov, .et al. , Clin Cancer Res, 2014, 20(14): 3799-3808 PMID: 24850846
- Ivan V Litvinov, .et al. , Cell Cycle., 2014, 15; 13(18): 2975-2982 PMID: 25486484
-
HDAC inhibitor
Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of histone deacetylase enzymes (HDAC) which is under development for the treatment of cutaneous T-cell lymphoma. -
HDAC inhibitor
Resminostat, also known as RAS2410, is a potent inhibitor of histone deacetylase (HDAC) classes I and II. It binds to and inhibits HDACs leading to an accumulation of highly acetylated histones. -
HDAC4 inhibitor
Tasquinimod is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. - Palifosfamide is a synthetic mustard compound with potential antineoplastic activity.
-
HDAC6 inhibitor
ACY-241 is a new, selective and orally available inhibitor of HDAC6.- Bae J, .et al. , Leukemia, 2018, Sep;32(9):1932-1947 PMID: 29487385
-
Topoisomerase II inhibitor
Pixantrone is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity. -
modified nucleoside
6-O-Methyl Guanosine is a modified nucleoside. 6-O-Methyl Guanosine (6-methylguanosine) inhibit colony-forming ability in a malignant xeroderma pigmentosum cell line. -
topoisomerase 1 inhibitor
Genz-644282 is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity. -
DNA-PK inhibitor
KU0060648 is a potent and selective inhibitor of DNA-dependent protein kinase (DNA-PK), (IC50 = 8.6 nM); with 20-1000 fold selectivity for DNA-PK over other PIKKs and a panel of 60 kinases. KU-0060648 enhances HDR efficiency and attenuates NHEJ frequency. -
1,3-β-D-glucan synthase inhibitor
Micafungin (Mycamine; FK463) is an echinocandin antifungal drug which can inhibit 1,3-beta-D-glucan synthase.- Kate Chatfield-Reed, .et al. , Genetics, 2016, Apr; 202(4): 1365-1375 PMID: 26896331
-
biomarker
N6-Etheno 2'-deoxyadenosine is a reactive oxygen species (ROS)/reactive nitrogen species (RNS)-induced DNA oxidation product, used as a biomarker to evaluate chronic inflammation and lipid peroxidation in animal or human tissues. -
ATR inhibitor
ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.- Fu-Xing Gong, .et al. , Nucleic Acids Res, 2021, Sep 20;49(16):9342-9352 PMID: 34403458
- 3-Methylcytidine, a urinary nucleoside, can be used as a biomarker of four different types of cancer: lung cancer, gastric cancer, colon cancer, and breast cancer.
-
JAK2/HDAC dual inhibitor
JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. -
IMPDH inhibitor
AVN-944 (also known as VX-944) serves as an effective oral inhibitor, specifically targeting and inhibiting IMPDH (inosine monophosphate dehydrogenase). This enzyme plays a crucial role as a rate-limiting factor in the synthesis of guanine nucleotides from scratch. Additionally, AVN-944 acts against the synthesis of RNA in arenaviruses, effectively preventing arenavirus infections. Demonstrating a wide spectrum of anti-cancer properties, AVN-944 is utilized in research related to multiple myeloma (MM) and acute myeloid leukemia (AML).
- Kevin Chiem, .et al. , Microbiol Spectr, 2023, Aug 17;11(4):e0474522 PMID: PMC10434227
- Desarey Morales Vasquez, .et al. , Viruses, 2020, Sep; 12(9): 1041 PMID: 32961956
- Park JG, .et al. , J Virol, 2020, Mar 17;94(7) PMID: 31941776
- Dunham EC, .et al. , Antiviral Res, 2018, Sep;157:140-150 PMID: 30031760
- 3'-Azido-3'-deoxy-beta-L-uridine (Compound 25) is a nucleoside derivative.
-
DNA topoisomerase II inhibitor
Ellipticine is a DNA intercalating agent and a DNA topoisomerase II inhibitor.- Calhelha RC, .et al. , Analyst, 2017, Oct 23;142(21):4124-4141 PMID: 28991301
-
topoisomerase I/II inhibitor
TAS 103, also known as BMS-247615, is a quinoline derivative that displays antitumor activity in murine and human tumor models -
DNA/RNA Synthesis inhibitor
Chlorambucil is a nitrogen mustard alkylating agent. -
MTH1 (NUDT1) inhibitor
(S)-crizotinib, the (S)-enantiomer of crizotinib, is a potent MTH1 (NUDT1) inhibitor with IC50 of 72 nM. -
PERK inhibitor
ISRIB is a potent and selective PERK inhibitor with IC50 of 5 nM.- Zhou W, .et al. , Research Square, 2023, MAY 03
- Satoshi Watanabe, .et al. , Proc Natl Acad Sci U S A, 2021, May 18;118(20) PMID: 33972447
- Satoshi Watanabe, .et al. , bioRxiv, 2020, February 27
-
HDAC inhibitor
4SC-202 is an orally bioavailable benzamide and inhibitor of human class I histone deacetylases (HDACs) isoenzymes 1, 2 and 3, with potential antineoplastic activity. - Bleomycin is a glycopeptide antibiotic produced by the bacterium Streptomyces verticillus. It acts by induction of DNA strand breaks.
- Ou QX, .et al. , Bioelectrochemistry, 2017, Jun;115:47-55 PMID: 28063751