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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.
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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. -
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. -
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. - Uramustine is a chemotherapy drug which belongs to the class of alkylating agents.
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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
- 3'-Azido-3'-deoxy-beta-L-uridine (Compound 25) is a nucleoside derivative.
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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.- Calhelha RC, .et al. , Analyst, 2017, Oct 23;142(21):4124-4141 PMID: 28991301
- N6,N6-Dimethyladenosine is a modified ribonucleoside previously found in rRNA, and also exhibits in mycobacterium bovis Bacille Calmette-Gu??rin tRNA.
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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
- Triacsin C, originally isolated from Streptomyces sp., is an inhibitor of long fatty acid acyl-CoA synthetase (IC50 = 6.3 uM in Raji cells).
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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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SIRT1 activator
SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2.- Eleni Pitsillou, .et al. , Comput Biol Chem, 2020, 89: 107408 PMID: 33137690
- Liu X, .et al. , Life Sci, 2019, Nov 9:117041 PMID: 31715188
- Blasticidin S HCl is a nucleoside antibiotic isolated from Stretomyces girseochromogenes, and acts as a DNA and protein synthesis inhibitor.
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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.- 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.- 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.