-
HDACs/mTOR Inhibitor 1
HDACs/mTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs) and mammalian target of Rapamycin (mTOR) target inhibitor for treating hematologic malignancies. -
cell cycle inhibitor
Briciclib disodium salt is a benzyl styryl sulfone analog, and a disodium phosphate ester prodrug of ON 013100, with potential antineoplastic activity. -
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
-
Topoisomerase I inhibitor
CKD-602 is a topoisomerase I inhibitor. -
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
-
PERK inhibitor
ISRIB (trans-isomer) is a potent and selective small molecule inhibitor of PERK signaling (IC50 ~5 nM) that can potently reverse the effects of eIF2α phosphorylation. -
Topoisomerase II inhibitor
NK314 is a novel synthetic benzo[c]phenanthridine alkaloid that shows strong antitumor activity. It inhibited topoisomerase II activity and stabilized topoisomerase II-DNA cleavable complexes.- Kopa P, .et al. , Mol Biol Rep, 2019, Oct 3 PMID: 31583565
- Macieja A, .et al. , Mol Biol Rep, 2019, Apr 24 PMID: 31020489
-
HDAC6 inhibitor
Nexturastat A is an aryl urea derivative that acts as a potent and highly selective inhibitor of histone deacetylase 6 (HDAC6) (IC50= 5.02 +/- 0.60 nM). -
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 -
PARP-1 inhibitor
Rucaparib is a potent inhibitor of purified full-length human PARP-1 and shows higher inhibition of cellular PARP in LoVo and SW620 cells.- Jianwei Dou, .et al. , J Sep Sci, 2020, Dec 4 PMID: 33275824
-
NAD(+)-dependent histone deacetylase Sir2p inhibitor
Splitomicin is a selective NAD(+)-dependent histone deacetylase Sir2p inhibitor with IC50 of 60 uM, showing a higher activity in a cell-based assay. -
HDAC inhibitor
Santacruzamate A (CAY10683) is a potent and selective HDAC inhibitor with IC50 of 119 pM for HDAC2, >3600-fold selectivity over other HDACs. -
DNA/RNA Synthesis inhibitor
Chlorambucil is a nitrogen mustard alkylating agent. -
protein synthesis inhibitor
Puromycin 2HCl is an aminonucleoside antibiotic, which acts as a protein synthesis inhibitor. -
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
-
APE1 inhibitor
CRT0044876 is a potent and selective APE1 inhibitor with IC50 of ~3 μM. -
RNA polymerase inhibitor
BMH-21 is a potent small molecule DNA intercalator. BMH-21 binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription.- Masahiko Okuda, .et al. , Nucleic Acids Res, 2021, Jul 16 PMID: 34268577
-
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. -
Topoisomerase II inhibitor
Nemorubicin is an anticancer drug with IC50 value of 0.08 uM. It is active on tumors resistant to alkylating agents, topoisomerase II inhibitors and platinum derivatives. It works primarily through topoisomerase I inhibition. -
Topoisomerase II inhibitor
Doxorubicin is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis.- Laura Wiggins, .et al. , Nat Commun, 2023, 14: 1854
- Stefania Scialla, .et al. , Int J Pharm, 2023, Feb 5;632:122575 PMID: 36603672
- Fernando Espinola-Portilla, .et al. , Mol. Pharmaceutics, 2023, 20(3): 1490-1499
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- R Mahalakshmi, .et al. , Mol Biol Rep, 2022, Jan;49(1):463-476 PMID: 34739690
- J Priyanga, .et al. , Chem Biol Interact, 2020, Nov 1;331:109250 PMID: 32956706
- Abdelrehim A, .et al. , PLoS One, 2019, Feb 22;14(2):e0212701 PMID: 30794671
- J Wei, .et al. , bioRxiv, 2018, 2018
-
PARP Inhibitor
BMN-673 (8R,9S) is the (8R,9S) enantiomer of BMN-673. BMN 673 is a novel PARP inhibitor with IC50 of 0.58 nM. -
DHFR inhibitor
Pemetrexed is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively. -
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
-
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. -
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.