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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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Apoptosis Inducer
Andrographolide is an interesting pharmacophore with anticancer and immunomodulatory activities and hence has the potential for being developed as a cancer therapeutic agent. - Flunisolide is a corticosteroid often used to treat allergic rhinitis.The principal mechanism of action of Flunisolide is to activate glucocorticoid receptors, meaning it has an anti-inflammatory action.
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nonsteroidal anti-inflammatory agent
Flurbiprofen is a nonsteroidal anti-inflammatory agent (NSAIA) with antipyretic and analgesic activity. -
nitroimidazole antibiotic medication
Metronidazole is a nitroimidazole antibiotic medication used particularly for anaerobic bacteria and protozoa. -
TNF-alpha inhibitor
Pomalidomide is a derivative of thalidomide and acts as an immunomodulator. -
E3 ubiquitin ligase inhibitor
Thalidomide can directly inhibit angiogenesis induced by bFGF or VEGF in vivo. - Edratide (TV 4710) is a synthetic peptide of 19 amino acid based on the complementarity-determining region 1 (CDR1) of a human anti-DNA antibody that expresses a major idiotype denoted 16/6 Id. Edratide reduces the rates of apoptosis (Apoptosis) and down-regulates of caspase-8 and caspase-3, up-regulates Bcl-xL. Edratide has the potential for the research of systemic lupus erythematosus (SLE).
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Caspase-1 substrate
Ac-YVAD-pNA is a specific Caspase-1 substrate. Ac-YVAD-pNA can be used to detect Caspase-1 activity. Caspase-1 is a key mediator of inflammatory processes. -
mGluR II agonist
Xanthurenic acid is a putative endogenous Group II metabotropic glutamate receptor agonist, on sensory transmission in the thalamus. -
analgesic agent
Tetrahydropalmatine, an active component isolated from corydalis, possesses analgesic effects. Tetrahydropalmatine acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats. -
Anticancer agent
Flavokawain A is found in Piper methysticum (kava plant). It suppresses expression of iNOS and COX-2 in macrophages, decreases expression of Ki67, XIAP and survivin in urothelial cell carcinoma cells, and inhibits degradation of NF-kB.
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HMGB1 release inhibitor
Ethyl pyruvate is a simple derivative of the endogenous metabolite, pyruvic acid. Ethyl pyruvate is an anti-inflammatory agent. -
inhibitor of tubulin polymerization
4-Oxo-4-HPR is an inhibitor of tubulin polymerization, inducing marked G2-M cell cycle arrest and apoptosis in fenretinide-sensitive and fenretinide-resistant cell lines. It is also a fenretinide metabolite. -
GPX4 PROTAC Degrader
PROTAC GPX4 degrader-1 functions as a targeted protein degradation agent specifically for GPX4. It exhibits a DC50 of 0.03 μM in HT1080 cells, demonstrating potent activity in promoting the degradation of GPX4. This compound is applicable in research exploring the role of GPX4 in various cellular processes and the therapeutic potentials of targeting antioxidant defenses in disease models. -
PROTAC MDM2 Degrader
MD-222 is a first-in-class PROTAC degrader targeting MDM2. This compound contains ligands for both Cereblon and MDM2, facilitating the rapid degradation of MDM2 protein and subsequent activation of wild-type p53 in cellular contexts. Due to its mechanism of action, MD-222 exhibits notable anticancer properties, making it a valuable tool for research in cancer biology and therapeutic development. -
p53 Activator
C16-Ceramide is a natural small molecule that acts as a p53 activator by directly and selectively binding to the protein. This compound is known to induce apoptosis in various cancer cell lines, making it a valuable tool for research in cancer biology and therapeutic development. Its ability to modulate p53 activity facilitates investigations into cellular stress responses and the mechanisms underlying tumor suppression. -
Alkaloid
Conophylline is a vinca alkaloid derived from the leaves of the tropical plant Ervatamia microphylla. This compound functions as a differentiation inducer for pancreatic cells and demonstrates potent biological activity by suppressing hepatic stellate cells (HSC) while inducing apoptosis. It is of particular interest in research focused on pancreatic differentiation and the modulation of liver fibrosis. -
Rac1/Cdc42 Inhibitor
AZA1 is a potent dual inhibitor of Rac1 and Cdc42, key regulators of cell signaling pathways. This compound has been shown to induce apoptosis in prostate cancer cells while simultaneously inhibiting their proliferation, migration, and invasion. AZA1 serves as a valuable tool for research into the molecular mechanisms of prostate cancer progression and potential therapeutic interventions. -
Tyrosinase Inhibitor
Norartocarpetin is a potent tyrosinase inhibitor, demonstrating significant inhibition with an IC50 value of 0.47 μM. This compound serves as an effective antibrowning agent for food systems research and exhibits notable anticancer activity against lung carcinoma cells (NCI-H460) with an IC50 of 22 μM. Its antiproliferative effects are mediated through targeting the Ras/Raf/MAPK signaling pathway, inducing mitochondrial-mediated apoptosis, causing S-phase cell cycle arrest, and inhibiting cell migration and invasion in human lung carcinoma cells. -
PROTAC RIPK degrader
PROTAC RIPK degrader-6 is a Cereblon-based protein-targeting chimeric molecule designed for the degradation of RIP Kinase. This compound employs a RIP2 kinase inhibitor linked through a suitable spacer to a cereblon ligand, facilitating targeted proteolysis of RIPK. Prominent applications include investigations into kinase-related signaling pathways and the development of innovative therapeutic strategies for diseases associated with RIPK dysregulation. -
HDAC Inhibitor
HC-Toxin is a potent histone deacetylase (HDAC) inhibitor with an IC50 of 30 nM. This cyclic tetrapeptide effectively induces apoptosis in tumor cells, demonstrating significant anticancer activity. Its mechanism of action makes it valuable for research in cancer therapy and the modulation of gene expression. -
Apoptosis Inducer
epi-Eriocalyxin A is a diterpenoid compound that serves as an apoptosis inducer in colon cancer cells. It effectively inhibits the activation of ERK1/2 and JNK pathways, leading to the suppression of Bcl-2 expression. This compound is valuable for research focused on cancer treatment and the mechanisms of apoptosis. -
Cdc42 GTPase Inhibitor
ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines. -
Monounsaturated Fatty Acid
Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid. Oleic acid is a Na+/K+ ATPase activator. -
Iron Chelator
Deferoxamine (Deferoxamine B) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine upregulates HIF-1α levels with good antioxidant activity. Deferoxamine also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19. -
Anticancer Agent
(+)-Erinacin A (Erinacine A) is a cyanoditerpenoid isolated from Hericium erinaceus with anticancer, anti-inflammatory and neuroprotective activities. (+)-Erinacin A can induce cancer cell death by activating extrinsic and intrinsic apoptosis pathways. (+)-Erinacin A can also inhibit the expression of NO synthase (iNOS) and the production of nitrotyrosine to exert inflammatory and neuroprotective effects, thereby reducing ischemic brain damage. -
Ionophore
Enniatin complex is a mixture of cyclohexadepsipeptides isolated largely from Fusarium species of fungi, and has ionophoric, antibiotic, and in vitro hypolipidaemic properties. Enniatin complex inhibits enzymes like acyl-CoA: cholesterol acyl transferase and induces apoptosis in several cancer lines . -
Topoisomerase IV Inhibitor
Ciprofloxacin is a potent topoisomerase IV inhibitor that demonstrates significant antibacterial activity as a fluoroquinolone antibiotic. It induces both mitochondrial and nuclear DNA damage, leading to mitochondrial dysfunction and increased reactive oxygen species (ROS) production. Ciprofloxacin exhibits anti-proliferative properties and triggers apoptotic pathways, making it a valuable tool for research applications focused on bacterial infections, oxidative stress, and cancer biology. -
Tubulin Inhibitor
Demecolcine is a potent tubulin inhibitor that effectively disrupts microtubule polymerization, exhibiting an IC50 value of 2.4 μM. By binding to tubulin dimers, Demecolcine exerts anti-mitotic effects, hindering cellular division. This compound is primarily utilized in research related to inflammatory disorders and various cancer pathways, making it valuable for studies focused on cell cycle regulation and targeted therapies. -
AMPK Agonist
10-Gingerol is an AMPK agonist derived from ginger oleoresin, exhibiting notable anti-inflammatory, antioxidant, and anti-proliferative properties. It effectively suppresses neointimal hyperplasia and inhibits the proliferation of vascular smooth muscle cells. Demonstrating significant radical scavenging activities, 10-Gingerol has IC50 values of 10.47 μM against DPPH, 1.68 μM against superoxide, and 1.35 μM against hydroxyl radicals. This compound also inhibits MDA-MB-231 tumor cell line proliferation with an IC50 of 12.1 μM, while targeting the PI3K/Akt signaling pathway to suppress proliferation, migration, invasion, and promote apoptosis. It holds potential for research applications in ulcerative colitis. -
TNF Receptor Inhibitor
Muscone, a TNF receptor inhibitor, is derived from the traditional Chinese medicine musk. It effectively inhibits NF-κB signaling and NLRP3 inflammasome activation, resulting in a significant reduction of inflammatory cytokines such as IL-1β, TNF-α, and IL-6. This compound is valuable in research focused on inflammation, cardiac function restoration, and improving survival rates in various pathological conditions. -
Cysteine Residues Modifier
N-Ethylmaleimide (NEM) is a potent chemical reagent that irreversibly alkylates free sulfhydryl groups, specifically targeting cysteine residues. This compound serves as an effective inhibitor of cysteine proteases and significantly affects phosphate transport in mitochondria. With an IC50 value of 6.3 μM, N-Ethylmaleimide is valuable for modifying cysteine residues in proteins and peptides, making it an essential tool in biochemical research and studies involving protein functionality and structure. -
Apoptosis Inducer
Sanguinarine chloride is a benzophenanthridine alkaloid that functions as an apoptosis inducer primarily through the generation of reactive oxygen species (ROS). This compound is known to activate key signaling pathways, specifically JNK and NF-κB, facilitating programmed cell death. Sanguinarine chloride is widely utilized in cancer research and studies investigating apoptotic mechanisms. -
Bcl-xL/Bcl-2 Inhibitor
BM-1244 is a selective inhibitor of Bcl-xL and Bcl-2, exhibiting Ki values of 134 nM and 450 nM, respectively. This compound induces apoptosis and suppresses tumor growth through the release of cytochrome C and Smac from mitochondria, leading to caspase-3 activation and PARP cleavage. BM-1244 has demonstrated synergistic effects with chemotherapy in vivo, making it a valuable research tool for studying colorectal cancer, acute myeloid leukemia, and gastric cancer. -
Bcl-2/Bcl-xl Inhibitor
Pelcitoclax is a potent inhibitor of Bcl-2 and Bcl-xl, designed to induce apoptosis in cancer cells. Its primary mechanism involves disrupting the anti-apoptotic activity of these proteins, leading to increased cell death in malignant tissues. Pelcitoclax is utilized in research to explore therapeutic strategies against various malignancies and to study apoptotic pathways in cellular models.

