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PI3K/HDAC inhibitor
CUDC-907 (Fimepinostat) is a single small molecule inhibitor that targets both PI3K and HDAC. CUDC-907 is more efficacious than either a single PI3K or HDAC inhibitor reference compound or a combination of the two single agents at maximally tolerated doses.- Caner Gunaydın, .et al. , Immunopharmacol Immunotoxicol, 2022, Jun;44(3):447-455 PMID: 35291899
- Chie Ishikawa, .et al. , Eur J Haematol, 2020, Eur J Haematol PMID: 32780889
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PI3K inhibitor
Wortmannin is a potent, selective, cell-permeable and irreversible inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) (IC50 = 2 - 4 nM) which also potently inhibits polo-like kinase 1 (PLK1) (IC50 = 5.8 nM).
- Hirotake Ishida, .et al. , J Neurosci, 2021, Oct 13;41(41):8494-8507 PMID: 34452938
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MDMX Inhibitor
NSC207895 is a cell-permeable benzofuroxan compound that downregulates the p53 negative regulator MDMX protein level in MCF-7, LNCaP, and A549 cells (1 to 10 µM for 16 to 24 h) by suppressesing MDMX promoter transcription activity (IC50 = 2.5 µM in HT1080 cells), leading to enhanced p53 stabilization and activation.
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PARP inhibitor
BMN-673 is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential antineoplastic activity.- Subhajit Chatterjee, .et al. , J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
- Charles-André Philip, .et al. , BMC Cancer, 2017, 17: 638 PMID: 28886696
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DNA synthesis inhibitor
Gemcitabine (LY 188011) is a DNA synthesis inhibitor which inhibits the growth of BxPC-3, Mia Paca-2, PANC-1, PL-45 and AsPC-1 cells with IC50s of 37.6, 42.9, 92.7, 89.3 and 131.4 nM, respectively.- Yi-Ru Pan, .et al. , Int J Biol Sci, 2023, May 21;19(9):2772-2786 PMID: 37324940
- Khan Mohammad Imran, .et al. , Pharmaceutics, 2023, May 24;15(6):1585 PMID: 37376034
- Yi-Ru Pan, .et al. , Biomolecules, 2020, Nov 9;10(11):1529 PMID: 33182492
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DNA synthesis inhibitor
Mitomycin C is a DNA crosslinking agent that inhibits DNA synthesis and induces apoptosis in a variety of cells.- Gehlen-Breitbach S, .et al. , Int J Oral Sci, 2023, 15(1):16 PMID: 37024457
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DHFR inhibitor
Pralatrexate is an antifolate (a folate analogue metabolic inhibitor) designed to accumulate preferentially in cancer cells. -
eIF4A inhibitor
Silvestrol is a eukaryotic translation initiation factor 4A (eIF4A) inhibitor isolated from the fruits and twigs of Aglaia foveolata. Silvestrol induces autophagy and caspase-mediated apoptosis. - Silvestrol aglycone is a Silvestrol analogue, inhibits protein translation initiation in cancer cells, with EC50s of 10 and 200 nM for myc-LUC and tub-LUC luciferase reporter protein translation, respectively. Anti-cancer activity.
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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
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viral RNA polymerase inhibitor
T-705, a substituted pyrazine compound, has been found to exhibit potent anti-influenza virus activity in vitro and in vivo.
- Steven B Tillis, .et al. , Microorganisms, 2023, May 24;11(6):1371 PMID: 37374873
- Hyeon-Min Cha, .et al. , ACS Infect Dis, 2023, Apr 14;9(4):1033-1045 PMID: 36912867
- Satoko Yamaoka, .et al. , Antiviral Res, 2022, Apr;200:105291 PMID: 35296419
- Crystal A Mendoza, .et al. , Antiviral Res, 2021, Jan;185:104993 PMID: 33296695
- Liva Checkmahomed, .et al. , Viruses, 2020, Oct; 12(10): 1139 PMID: 33049959
- JE Comer, .et al. , Viruses, 2019, Feb 3;11(2). pii: E137 PMID: 30717492
- Ma J, .et al. , Antiviral Res, 2018, Feb;150:112-122 PMID: 29253498
- Ji-Ae Kim, .et al. , Viruses, 2018, Feb; 10(2): 72 PMID: 29425176
- Haejin Chun, .et al. , Polym Chem, 2018, 9: 2116-2123
- Baz M, .et al. , Viruses, 2018, Nov 3;10(11) PMID: 30400276
- Sehee Park, .et al. , PLoS One., 2014, 9(7): e101325 PMID: 24992479
- Triptolide is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii.
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ATM/ATR inhibitor
VE-821 is a potent and selective inhibitor of protein kinase ATR.- Atsushi Saito, .et al. , Cell Rep, 2023, May 30;42(5):112479 PMID: 37178686
- Mitsuru Sasaki-Honda, .et al. , Hum Mol Genet, 2018, Dec 1; 27(23): 4024-4035 PMID: 30107443
- Kim J, .et al. , Mol Cell, 2018, Jan 4;69(1):36-47.e7 PMID: 29249653
- Antonio Postigo, .et al. , Cell Rep, 2017, May 2; 19(5): 1022-1032 PMID: 28467896
- Nnennaya Kanu, .et al. , Genome Biol, 2016, 17: 185 PMID: 27634334
- Carolyn Botting, .et al. , Virol J, 2016, 13: 15 PMID: 26817608
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RHA inhibitor
YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding to the oncogenic transciption factor EWS-FLI1.- Christopher M Schafer, .et al. , Proc Natl Acad Sci U S A, 2020, Oct 20;117(42):26494-26502 PMID: 33020273
- Levoleucovorin calcium is the calcium salt of Levoleucovorin, which is the enantiomerically active form of folinic acid.
- Procarbazine Hydrochloride is an alkylating agent, with anticancer activity.
- Cyclophosphamide monohydrate is an alkylating, cytotoxic agent experimentally shown to crosslink DNA, causing strand breakage and inducing mutations.
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Topoisomerase inhibitor
Balofloxacin is a quinolone antibiotic. The bactericidal action of Balofloxacin results from interference with the enqyme DNA gyrase which is needed for the synthesis of bacterial DNA. Balofloxacin is efficacious against Gram-negative bacteria. It also has enhanced activity against Gram positive bacteria, including MRSA and Streptococcus pneumoniae. -
Topoisomerase inhibitor
Sarafloxacin hydrochloride is a fluoroquinolone antibacterial agent. Inhibits bacterial DNA gyrase (topoisomerase). -
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). - Azithromycin is an azalide antibiotic, which inhibits the growth of gram negative bacteria, such as Haemophilus influenza.
- Adenine sulfate is a sulfate salt form of adenine which is a purine derivative and a nucleobase with a variety of roles in biochemistry.
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Topoisomerase II inhibitor
Flumequine is a synthetic chemotherapeutic antibiotic which affecting mammalian chromosome and DNA unwinding at the level of gyrase/topoisomerases. - Pefloxacin mesylate is a synthetic chemotherapeutic agent and an antibacterial agent with IC5N/A of 6.7 nM.
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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
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HDAC6 inhibitor
ACY-1215 selectively targets and binds to HDAC6, thereby disrupting the Hsp90 protein chaperone system through hyperacetylation of Hsp90 and preventing the subsequent aggresomal protein degradation. -
HDAC Inhibitor
CI-994 is a histone deacetylase (HDAC) inhibitor and induces histone hyperacetylation in living cells. - Schisandrin B is the most abundant dibenzocyclooctadiene isolated from the fruit of Schisandra chinensis (Turcz) Baillon or Wu-Wei-Zi (transliterally meaning "the fruit of five tastes" in Chinese), which is a commonly used tonic herb in Chinese medicine, particularly for the treatment of liver ailments.
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Topoisomerase
(S)-10-Hydroxycamptothecin is a camptothecin derivative that inhibits DNA topoisomerase by enacting strand breaks in chromosomal DNA and inducing apoptosis. - Betulinic acid is a naturally occurring pentacyclic triterpenoid which has antiretroviral, antimalarial, and anti-inflammatory properties.
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DNA topoisomerase Inhibitor
SN 38 is the active metabolite of irinotecan (an analog of camptothecin - a topoisomerase I inhibitor).- Sarigama Rajesh, .et al. , Pharmaceutics, 2022, Oct 12;14(10):2175 PMID: 36297610
- Chen JC, .et al. , Biomolecules, 2019, Sep 9;9(9) PMID: 31505885
- Alibolandi M, .et al. , Artif Cells Nanomed Biotechnol, 2018, May 27:1-12 PMID: 29806500
- Bar-Zeev M, .et al. , Eur J Pharm Biopharm, 2018, Dec;133:240-249 PMID: 30367935
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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. -
p53 activator
Tenovin-6 is a analog of tenovin-1. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 in vitro with IC50 values of 21, 10, and 67 uM, respectively.- Igase M,, .et al. , Exp Cell Res, 2019, Dec 28:111810 PMID: 31891684
- Aldoxorubicin, also known as INNO-206, is the 6-maleimidocaproyl hydrazone derivative prodrug of the anthracycline antibiotic doxorubicin (DOXO-EMCH) with antineoplastic activity.
- Jingjing Ding, .et al. , Adv Mater, 2021, Feb;33(7):e2005562 PMID: 33432702
- Dos Santos Câmara AL, .et al. , Nanomedicine (Lond), 2017, Aug;12(15):1751-1765 PMID: 28703043