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HIF-1α inhibitor
Minocycline hydrochloride is a broad-spectrum tetracycline antibiotic, acting by binding to the bacterial 30S ribosomal subunit and inhibiting protein synthesis.- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
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14-3-3 protein Inhibitor
Difopein, dimeric version of R18 peptide that binds to 14.3.3 proteins with high affinity.- William J Stone, .et al. , J Neurochem, 2025, Sep;169(9):e70228 PMID: 40931680
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Caspase-1/4 inhibitor
VX-765 is a novel Caspase-1 inhibitor,which is an enzyme that controls the generation of two cytokines, IL-1b and IL-18.- Xianyu Piao, .et al. , Cell Death Differ, 2026, Apr;33(4):717-731 PMID: 41125794
- Takemasa Takii, .et al. , mSphere, 2025, 10:e00110-25 PMID: 40387341
- Joseph Flores, .et al. , Cell Death Dis, 2022, Oct 11;13(10):864 PMID: 36220815
- Arjun Thapa, .et al. , Leukemia, 2021, 23 February PMID: 33623143
- Prenitha Mercy Ignatius Arokia Doss, .et al. , Cell Rep, 2021, Mar 9;34(10):108833 PMID: 33691111
- Joseph Flores, .et al. , Nat Commun, 2020, Sep 11;11(1):4571 PMID: 32917871
- Joseph Flores, .et al. , Nat Commun, 2018, 9: 3916 PMID: 30254377
- Mohamed F. Ali, .et al. , Front Immunol, 2017, 8: 1504 PMID: 29170665
- García-Fernández A, .et al. , J Control Release, 2017, Feb 28;248:60-70 PMID: 28069553
- Jiujiu Yu, .et al. , Proc Natl Acad Sci U S A, 2014, 111(43): 15514-15519 PMID: 25313054
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dual cIAP and XIAP inhibitor
BV-6 is a SMAC mimetic, dual cIAP and XIAP inhibitor.- Ximena Hildebrandt, .et al. , Sci Adv, 2025, Sep 17;11(38):eadw2539 PMID: 40961178
- Aneri Shah, .et al. , Cancers (Basel), 2020, Aug 5;12(8):E2188 PMID: 32764479
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LDH inhibitor
Sodium oxamate (SO, Aminooxoacetic acid, Oxamic acid) is an inhibitor of lactate dehydrogenase (LDH) that specificly inhibits LDH?A.- Yingying Chen, .et al. , Immunology, 2024, Jun;172(2):252-268 PMID: 38424694
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Apoptosis inducer
LY573636 is a potent anti-tumor agent, which causes growth arrest and apoptosis of a variety of human solid tumors in vitro and in vivo. LY573636-induced apoptosis occurs by a mitochondrial-targeted mechanism.- Yingzheng Xu, .et al. , JCI Insight, 2024, Jun 13:e174746 PMID: 38869957
- Ting TC, .et al. , Cell Rep, 2019, Nov 5;29(6):1499-1510.e6 PMID: 31693891
- Ting Han, .et al. , Science, 2017, Apr 28;356(6336). pii: eaal3755 PMID: 28302793
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Cdc42 GTPase inhibitor
CASIN is a novel and potent Cdc42 inhibitor.- Yongru Xu, .et al. , Int J Mol Sci, 2017, Mar; 18(3): 586 PMID: 28282856
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Caspase-3 inhibitor
Ivachtin is a potent, cell-permeable, reversible, non-competitive inhibitor of Caspase-3 (IC50 = 23 nM).- Yosefzon Y, .et al. , Mol Cell, 2018, May 17;70(4):573-587.e4 PMID: 29775577
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IAP inhibitor
AT-406 is an orally bioavailable inhibitor of IAP family of proteins with potential apoptotic inducing and antineoplastic activity. AT-406 selectively inhibits the biological activity of IAP proteins, including X chromosome-linked IAP (XIAP), the cellular IAPs 1 (c-IAP1) and 2 (c-IAP2) and melanoma inhibitor of apoptosis protein (ML-IAP).- Yoshikawa M, .et al. , J Med Chem, 2018, Mar 22;61(6):2384-2409 PMID: 29485864
- Tsuyoshi Ishii, .et al. , Sci Rep, 2017, 7: 13000 PMID: 29026104
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Mcl-1 inhibitor
MIM1 is a selective small molecule inhibitor of Mcl-1(IC50= 4.8 μM) that overcomes Mcl-1-dependent leukemia cell survival. - NKP-1339 (IT-139) is the first-in-class ruthenium-based anticancer drug in clinical development against solid cancer with limited side effects.
- Zin Zin Ei, .et al. , Sci Rep, 2021, Nov 17;11(1):22448 PMID: 34789798
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PKD inhibitor
CID 2011756 is a protein kinase D (PKD) inhibitor (IC50 values are 0.6, 0.7 and 3.2 μM for PKD2, PKD3 and PKD1 respectively). -
PKD inhibitor
kb NB 142-70 is a selective protein kinase D (PKD) inhibitor (IC50 values are 28.3, 58.7 and 53.2 nM for PKD1, 2 and 3 respectively). -
p53 inhibitor
inhibits p53 binding to mitochondria by reducing its affinity for antiapoptotic proteins Bcl-2 and Bcl-XL. -
p53 inhibitor
Pifithrin-α hydrobromide is a reversible inhibitor of p53-mediated apoptosis and p53-dependent gene transcription such as cyclin G, p21/waf1, and mdm2 expression.
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myeloperoxidase inhibitor
PF-06282999 is a potent and selective myeloperoxidase inhibitor which is potential useful for the treatment of cardiovascular diseases. -
Caspase-6 inhibitor
Z-VEID-FMK is the specific recognition sequence for caspase-6/Mch2. Z-VEID-FMK is a synthetic peptide that irreversibly inhibits activity of VEID-dependent caspases (e.g., caspase-6). The inhibitor is designed as a methyl ester to facilitate cell permeability. -
RIP1 inhibitor
GSK481 is a novel benzoxazepinone (BOAz) series of RIP1 inhibitors. Receptor Interacting Protein Kinase 1 (RIP1) has been implicated as a key contributor to inflammation through the regulation of programmed necrosis. Inhibition of this kinase has been shown to hinder cell necrotic death, thereby establishing RIP1 as a viable target for the potential treatment of multiple inflammatory diseases. -
Caspase-2 inhibitor
Z-VDVAD-FMK is a cell-permeable, irreversible inhibitor of caspase-2. Caspase inhibitors play an important role in investigating biological processes. - Trabectedin (Ecteinascidin-743 or ET-743) is a novel antitumour agent of marine origin with potent antitumour activity both in vitro and in vivo.
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p53R175 activator
NSC 319726 is a potent and selective activator of mutant p53R175 -
antitumor agent
2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound of Cinnamomum cassia, with antitumor activity. -
Apoptosis Inhibitor
Apoptosis Inhibitor is a cell-permeable inhibitor of apoptosis induction. -
nucleophosmin inhibitor
NSC348884 is a nucleolar phosphoprotein that displays several biological activities in ribosome biogenesis, cell proliferation, cytoplasmic/nuclear shuttle transportation, nucleic acid binding, ribonucleic cleavage, and centrosome duplication. NSC 348884 is a putative inhibitor of nucleophosmin (NPM). NSC 348884 inhibits NMP oligomer formation, up-regulates p53 and induces apoptosis. - Trifloxystrobin (CGA 279202) is a fungicide, with EC50s of 23.0 μg/L and 1.7 μg/L for Daphnia magna neonate and embryos, respectively, after treatment for 48 h.
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Bcl-xL inhibitor
WEHI-539 hydrochloride is a small-molecule inhibitor of BCL-xL with IC50 value of 1.1 nM. -
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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multi-kinase inhibitor
Lestaurtinib (CEP-701;KT-5555) is a multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively. -
VEGFR1/2/3/PDGFRβ/Kit/RET/Raf-1 inhibitor
Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively. -
anticancer and radioprotection agent
Geniposidic acid is an effective anticancer and radioprotection agent. -
Apoptosis Activator
Apoptosis Activator 2 strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation which leads to the destruction of cells (Apaf-1 dependent) with IC50 of ~4 μM, inactive to HMEC, PREC, or MCF-10A cells - TPEN is a heavy metal chelator. Reacts with both Zn-proteome and Zn-metallothionein (MT) in LLC-PK1 cells; acts as an intracellular chelator of proteomic Zn2+.
- Arctigenin is an antioxidant, anti-inflammatory, antiproliferative and antiviral agent. It inhibits LPS-induced iNOS expression via inhibition of IκBα phosphorylation and p65 nuclear translocation (IC50 = 10 nM)

