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1,3-β-D-glucan synthase inhibitor
Caspofungin is an antifungal medicine. It is used to help the body overcome serious fungus infections, including Candida and Aspergillosis infections. It is also used to treat serious fungus infections when other medicines (e.g., amphotericin B, itraconazole) have failed. -
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
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NNRT inhibitor
Delavirdine is a potent inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). -
ATR inhibitor
Berzosertib (VE-822) is an potent ATR inhibitor.
- Joshua J Deppas, .et al. , Toxicol Appl Pharmacol, 2025, Jul:500:117375
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human topoisomerase I (Top1) inhibitor
Top1 inhibitor 1 (compound 28) is a potent human topoisomerase I (Top1) inhibitor with an IC50 value of 29 nM. -
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
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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. -
IRE-1α inhibitor
6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) is an IRE-1α inhibitor with an IC50 of 0.08 μM, extracted from patent WO 2008154484 A1, IRE-lα inhibitor compound 3-5. -
HCV NS5B polymerase inhibitor
Deleobuvir (BI207127) was a non-nucleoside hepatitis C virus NS5B polymerase inhibitor for the treatment of hepatitis C
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glucan synthase inhibitor
Anidulafungin is a semi-synthetic cyclic lipopeptide belonging to the echinocandin class that was reported in 1995 and commercially developed by Eli Lilly. Anidulafungin inhibits the synthesis of ??-(1,3)-D-glucan, an essential component of the cell wall of susceptible fungi and is extensively referenced in the literature with over 400 citations.- Noel Vera-González, .et al. , Adv Healthc Mater, 2024, Aug 29:e2401157 PMID: 39210641
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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
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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.- Cheng Cao, .et al. , ACS Appl Mater Interfaces, 2024, 16, 21, 27177-27186
- Calhelha RC, .et al. , Analyst, 2017, Oct 23;142(21):4124-4141 PMID: 28991301
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IRE1 Rnase inhibitor
4μ8C is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM.- Gideon Ong, .et al. , Cell Death Dis, 2024, Apr 18;15(4):276 PMID: 38637497
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PERK inhibitor
ISRIB (mix-isomer) is a potent and selective small molecule inhibitor of PERK signaling (IC50 ~5 nM) that can potently reverse the effects of eIF2α phosphorylation.
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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
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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
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eIF4E/eIF4G inhibitor
4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with KD of 25 uM.- Amnon Wittenstein, .et al. , PLoS Biol, 2023, Nov 9;21(11):e3002355 PMID: 37943958
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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.- Le Xu, .et al. , Cell Stem Cell, 2024, Aug 16:S1934-5909(24)00287-X PMID: 39181129
- SeungHye Han, .et al. , Nature, 2023, Aug;620(7975):890-897 PMID: 37558881
- 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
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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.- Jun Kumai, .et al. , Exp Cell Res, 2025, Jul 15;450(2):114629 PMID: 40466802
- Masahiko Okuda, .et al. , Nucleic Acids Res, 2021, Jul 16 PMID: 34268577
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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.
DNA Damage
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