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Pathways Recommended: Apoptosis
Targets Recommended: Apoptosis SNIPER

Results for "Apoptosis Activators" in MCE Product Catalog:

138

Inhibitors & Agonists

3

Screening Libraries

9

Peptides

50

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-103349
    PETCM

    Caspase Apoptosis Cancer
    PETCM is an activator of caspase-3 and acts as an cytochrome c (cyto c)-dependent manner. PETCM promotes Apaf-1 oligomerization and induces cell apoptosis in HeLa cells.
  • HY-N0052A
    Sanguinarine chloride

    Pseudochelerythrine chloride; Sanguinarium chloride

    Apoptosis Autophagy Bacterial Parasite Cancer
    Sanguinarine chloride, a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB.
  • HY-N0052
    Sanguinarine

    Pseudochelerythrine; Sanguinarin

    Apoptosis Autophagy Cancer
    Sanguinarine, a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB.
  • HY-123054
    BTSA1

    Bcl-2 Family Apoptosis Cancer
    BTSA1 is a potent, high affinity and orally active BAX activator with an IC50 of 250 nM and an EC50 of 144 nM. BTSA1 binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis.
  • HY-15098
    Apoptozole

    Apoptosis Activator VII

    HSP Apoptosis Cancer
    Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with Kds of 0.21 and 0.14 μM, respectively, and can induce apoptosis.
  • HY-N2632
    Uvarigrin

    Apoptosis Cancer
    Uvarigrin, isolated from the roots of Uvaria calamistrata, induces tumor multidrug resistance cell apoptosis and triggers Caspase-9 activation.
  • HY-13735A
    Quinacrine dihydrochloride

    Mepacrine dihydrochloride; SN-390 dihydrochloride

    Parasite Apoptosis Autophagy Mitophagy Cancer Infection
    Quinacrine dihydrochloride (Mepacrine dihydrochloride) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine dihydrochloride suppresses NF-κB and activate p53 signaling, which results in the induction of the apoptosis.
  • HY-13735B
    Quinacrine hydrochloride hydrate

    Mepacrine hydrochloride hydrate; SN-390 hydrochloride hydrate

    Parasite Apoptosis Autophagy Mitophagy Cancer Infection
    Quinacrine hydrochloride hydrate (Mepacrine hydrochloride hydrate) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine hydrochloride hydrate suppresses NF-κB and activates p53 signaling, which results in the induction of the apoptosis.
  • HY-100548
    GSK621

    AMPK Autophagy Apoptosis Cancer
    GSK621 is a specific AMPK activator, with IC50 values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation.
  • HY-13523
    PAC-1

    Procaspase activating compound 1

    Caspase Autophagy Apoptosis Cancer
    PAC-1 is an activator of procaspase-3 induces apoptosis in cancer cells with EC50 of 2.08 μM.
  • HY-N7526
    Naphthazarin

    DHNQ; 5,8-Dihydroxy-1,4-naphthoquinone

    Apoptosis Cancer Neurological Disease
    Naphthazarin (DHNQ) is a naturally occurring compound. Naphthazarin is effective by various cellular mechanisms including oxidative stress, activation of mitochondrial apoptosis-inducing factor (AIF), depolymerization of microtubules, interference with lysosomal function and p53-dependent p21 activation. Naphthazarin triggers apoptosis and has anti-tumor effects.
  • HY-10999
    Trametinib

    GSK1120212; JTP-74057

    MEK Autophagy Apoptosis Cancer
    Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis.
  • HY-13719
    Oleandrin

    Na+/K+ ATPase Apoptosis Cancer
    Oleandrin inhibits the Na +, K +-ATPase activity with an IC50 of 620 nM. Oleandrin induces apoptosis via activating endoplasmic reticulum stress.
  • HY-18633
    MDK83190

    Apoptosis Cancer
    MDK83190 is a potent apoptosis activator, induces Apaf-1 oligomerization, increases procaspase-9 processing and subsequent caspase-3 activation in a cyto c-dependent Manner.
  • HY-114372
    Lycopodine

    Lipoxygenase Caspase Apoptosis Cancer
    Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity. Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation.
  • HY-N6258
    Kahweol

    AMPK Apoptosis Metabolic Disease
    Kahweol is one of the consituents of the coffee from Coffea Arabica with anti-inflammatory anti-angiogenic, and anti-cancerous activities. Kahweol inhibits adipogenesis and increase glucose uptake by AMP-activated protein kinase (AMPK) activation. Kahweol induces apoptosis.
  • HY-100016
    AZD0156

    ATM/ATR Apoptosis Cancer
    AZD0156 is a potent, selective and orally active ATM inhibitor with an IC50 of 0.58 nM. AZD0156 inhibits the ATM-mediated signaling, prevents DNA damage checkpoint activation, disrupts DNA damage repair, and induces tumor cell apoptosis.
  • HY-Y0152
    Cinchonine

    (8R,9S)-Cinchonine; LA40221

    Apoptosis Parasite Cancer
    Cinchonine is a natural compound present in Cinchona bark. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells.
  • HY-13259
    MG-132

    Z-Leu-Leu-Leu-al; MG132

    Proteasome Autophagy Apoptosis Cancer
    MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis.
  • HY-100487
    TAK-243

    MLN7243

    E1/E2/E3 Enzyme NF-κB Apoptosis Cancer
    TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.
  • HY-N0168
    Hesperetin

    p38 MAPK Apoptosis Autophagy Neurological Disease Cancer
    Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
  • HY-W011303
    Phytosphingosine

    Apoptosis Cancer
    Phytosphingosine is a phospholipid and has anti-cancer activities. Phytosphingosine induces cell apoptosis via caspase 8 activation and Bax translocation in cancer cells.
  • HY-50714
    Quiflapon sodium

    MK-591 sodium

    FLAP Apoptosis Inflammation/Immunology
    Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.
  • HY-136268
    AQX-435

    Phosphatase Apoptosis Inflammation/Immunology
    AQX-435 is a potent SHIP1 phosphatase activator. AQX-435 reduces PI3K activation downstream of the B-cell receptor (BCR) and induces apoptosis of malignant B cells, and reduces lymphoma growth.
  • HY-13649
    Indibulin

    ZIO 301; D 24851

    Microtubule/Tubulin Apoptosis Cancer Neurological Disease
    Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis.
  • HY-13757A
    Tamoxifen

    ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively. Tamoxifen activates autophagy and induces apoptosis.
  • HY-12041
    SP600125

    JNK Autophagy Apoptosis Ferroptosis Cancer
    SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 inhibits autophagy and activates apoptosis.
  • HY-10999A
    Trametinib (DMSO solvate)

    GSK-1120212 (DMSO solvate); JTP-74057 (DMSO solvate)

    MEK Apoptosis Cancer
    Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis.
  • HY-108638
    NSC 146109 hydrochloride

    MDM-2/p53 Cancer
    NSC 146109 hydrochloride is a small-molecule p53 activator that target MDMX and could be of value in treating breast cancer. NSC 146109 hydrochloride is a pseudourea derivative, promotes breast cancer cells to undergo apoptosis through activating p53 and inducing expression of proapoptotic genes[1].
  • HY-118266
    BTdCPU

    Phosphatase Apoptosis Cancer
    BTdCPU is a potent heme-regulated eIF2α kinase (HRI) activator. BTdCPU promotes eIF2α phosphorylation and induced apoptosis in resistant cell.
  • HY-127019
    Nigericin

    Sodium Channel NOD-like Receptor (NLR) Bacterial Apoptosis Antibiotic Cancer Infection
    Nigericin is an antibiotic derived from Streptomyces hygroscopicus that act as a K +/H + ionophore, promoting K +/H + exchange across mitochondrial membranes.Nigericin can be a NLRP3 activator that induces the release of IL-1β as a NALP3-dependent manner. Nigericin triggers eryptosis, an effect paralleled by ROS formation, and in part due to induction of oxidative stress. Nigericin triggers apoptosis.
  • HY-N0831
    Jaceosidin

    Bcl-2 Family COX Apoptosis Cancer Inflammation/Immunology
    Jaceosidin is a flavonoid isolated from Artemisia vestita, induces apoptosis in cancer cells, activates Bax and down-regulates Mcl-1 and c-FLIP expression. Jaceosidin exhibits anti-cancer, anti-inflammatory activities, decreases leves of inflammatory markers, and suppresses COX-2 expression and NF-κB activation.
  • HY-133558
    VII-31

    E1/E2/E3 Enzyme Apoptosis Cancer
    VII-31 is a potent NEDDylation pathway activator to inhibit the tumor progression in vitro and in vivo. VII-31 induces apoptosis via intrinsic and extrinsic pathways.
  • HY-N0168A
    (Rac)-Hesperetin

    p38 MAPK Apoptosis Autophagy Cancer Neurological Disease
    (Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
  • HY-13757
    Tamoxifen Citrate

    ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively. Tamoxifen Citrate activates autophagy and induces apoptosis.
  • HY-P2228
    Chlamydocin

    HDAC Apoptosis Cancer
    Chlamydocin, a fungal metabolite, is a highly potent HDAC inhibitor, with an IC50 of 1.3 nM. Chlamydocin exhibits potent antiproliferative and anticancer activities. Chlamydocin induces apoptosis by activating caspase-3.
  • HY-P1740
    RGD peptide (GRGDNP)

    Integrin Apoptosis Inflammation/Immunology
    RGD peptide (GRGDNP) acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation. RGD peptide (GRGDNP) promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing.
  • HY-B1193
    Terfenadine

    (±)-Terfenadine; MDL-991

    Potassium Channel Histamine Receptor Na+/Ca2+ Exchanger Caspase Apoptosis Cancer Inflammation/Immunology Endocrinology
    Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca 2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
  • HY-N0047
    Polyphyllin I

    JNK mTOR Akt PDK-1 Autophagy Apoptosis Cancer
    Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis.
  • HY-P1740A
    RGD peptide (GRGDNP) (TFA)

    Integrin Apoptosis Inflammation/Immunology Cancer
    RGD peptide (GRGDNP) (TFA) acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation. RGD peptide (GRGDNP) (TFA) promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing.
  • HY-33350
    Clofilium tosylate

    Potassium Channel Apoptosis Cancer Cardiovascular Disease
    Clofilium tosylate, a potassium channel blocker, induces apoptosis of human promyelocytic leukemia (HL-60) cells via Bcl-2-insensitive activation of caspase-3. Antiarrhythmic agent.
  • HY-N0048
    Polyphyllin II

    Apoptosis Cancer
    Polyphyllin II is one of the most significant saponins in Rhizoma Paridis and has toxic effects on kinds of cancer cells. Polyphyllin II induces apoptosis through caspases activation and cell-cycle arrest.
  • HY-111617
    BTR-1

    Apoptosis Cancer
    BTR-1 is an active anti-cancer agent, causes S phase arrest, and affects DNA replication in leukemic cells. BTR-1 activates apoptosis and induces cell death.
  • HY-N0492
    α-Lipoic Acid

    Thioctic acid; (±)-α-Lipoic acid; DL-α-Lipoic acid

    NF-κB HIV Mitochondrial Metabolism Endogenous Metabolite Apoptosis Cancer Infection Inflammation/Immunology
    α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells.
  • HY-136477
    Pentagamavunon-1

    PGV-1

    Apoptosis COX VEGFR NF-κB Cancer
    Pentagamavunon-1 (PGV-1), a Curcumin analog with oral activity, targets on several molecular mechanisms to induce apoptosis including inhibition of angiogenic factors cyclooxygenase-2 (COX-2) and vascular endothelial growth factor (VEGF). PGV-1 inhibits NF-κB activation.
  • HY-N6681
    15-Acetoxyscirpenol

    Caspase Bacterial Apoptosis Antibiotic Infection
    15-acetoxyscirpenol, one of acetoxyscirpenol moiety mycotoxins (ASMs), strongly induces apoptosis and inhibits Jurkat T cell growth in a dose-dependent manner by activating other caspases independent of caspase-3.
  • HY-W011241
    Cinchonine hydrochloride

    (8R,9S)-Cinchonine hydrochloride; LA40221 hydrochloride

    Apoptosis Parasite Cancer
    Cinchonine hydrochloride ((8R,9S)-Cinchonine hydrochloride) is a natural compound present in Cinchona bark. Cinchonine hydrochloride activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells.
  • HY-117433
    4-Hydroperoxy cyclophosphamide

    DNA Alkylator/Crosslinker Apoptosis Reactive Oxygen Species Drug Metabolite
    4-Hydroperoxy cyclophosphamide is the active metabolite form of the prodrug Cyclophosphamide. 4-Hydroperoxy cyclophosphamide crosslinks DNA and induces T cell apoptosis independent of death receptor activation, but activates mitochondrial death pathways through production of reactive oxygen species (ROS). 4-Hydroperoxy cyclophosphamide is used to treat lymphomas and autoimmune disorders.
  • HY-N4202
    Dihydrorotenone

    Mitochondrial Metabolism Apoptosis Neurological Disease
    Dihydrorotenone, a natural pesticide, is a potent mitochondrial inhibitor. Dihydrorotenone probably induces Parkinsonian syndrome. Dihydrorotenone induces human plasma cell apoptosis by triggering endoplasmic reticulum stress and activating p38 signaling pathway.
  • HY-13567
    Bendamustine

    SDX-105 free base

    DNA Alkylator/Crosslinker Apoptosis Cancer
    Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties.
  • HY-N0605
    Ginsenoside Rh2

    20(S)-Ginsenoside Rh2; 20(S)-Rh2; Ginsenoside-Rh2

    Caspase Apoptosis Endogenous Metabolite Cancer
    Ginsenoside Rh2 is isolated from the root of Ginseng. Ginsenoside Rh2 induces the activation of caspase-8 and caspase-9. Ginsenoside Rh2 induces cancer cell apoptosis in a multi-path manner.
  • HY-N3005
    Britannin

    Apoptosis Autophagy Cancer Inflammation/Immunology
    Britannin, isolated from Inula aucheriana, is a sesquiterpene lactone. Britannin induces apoptosis and autophagy by activating AMPK regulated by ROS in liver cancer cells. Britannin has anti-proliferative and anti-inflammatory activities.
  • HY-N0220
    Dauricine

    NF-κB Apoptosis Cancer Inflammation/Immunology
    Dauricine, a bisbenzylisoquinoline alkaloid in Asiatic Moonseed Rhizome, possesses anti-inflammatory activity. Dauricine inhibits cell proliferation and invasion, and induces apoptosis by suppressing NF-κB activation in a dose- and time-dependent manner in colon cancer.
  • HY-101180
    C2 Ceramide

    Ceramide 2

    Phosphatase Mitochondrial Metabolism Apoptosis Endocrinology Metabolic Disease
    C2 Ceramide (Ceramide 2) is the main lipid of the stratum corneum and a protein phosphatase 1 (PP1) activator. C2 Ceramide activates PP2A and ceramide-activated protein phosphatase (CAPP). C2 Ceramide induces cells differentiation and apoptosis, inhibits mitochondrial respiratory chain complex III. C2 Ceramide is also a skin conditioning agent that protects the epidermal barrier from water loss.
  • HY-103269
    BAI1

    Bcl-2 Family Cancer
    BAI1 is a selective and allosteric inhibitor of BAX, an apoptosis regulator. BAI1 directly binds to BAX and allosterically inhibits BAX activation. BAI1 has the potential for the research of diseases mediated by BAX-dependent cell death.
  • HY-119931
    2-Hydroxychalcone

    Bcl-2 Family Apoptosis NF-κB Cancer Metabolic Disease
    2-hydroxychalcone, a natural flavonoid, is a potent antioxidant, inhibiting lipid peroxidation. 2-Hydroxychalcone induces apoptosis by Bcl-2 downregulation. 2-Hydroxychalcone inhibits the activation of NF-kB.
  • HY-13721
    Phenoxodiol

    Idronoxil; Dehydroequol; Haginin E

    Caspase Apoptosis Topoisomerase Cancer
    Phenoxodiol, a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. This agent also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21 WAF1 via a p53 independent manner.
  • HY-10037
    Quiflapon

    MK-591

    FLAP Apoptosis Inflammation/Immunology
    Quiflapon (MK-591) is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.6 nM in a FLAP binding assay. Quiflapon is also a potent and orally active Leukotriene biosynthesis (LT) inhibitor, shows IC50 values of 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively. Quiflapon induces cell apoptosis.
  • HY-B0097
    Floxuridine

    5-Fluorouracil 2'-deoxyriboside

    Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Bacterial CMV HSV Cancer Infection
    Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis. Floxuridine has antiviral effects against HSV and CMV.
  • HY-13520
    Nocodazole

    Oncodazole; R17934

    Microtubule/Tubulin Bcr-Abl CRISPR/Cas9 Autophagy Apoptosis Cancer
    Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, and activates CRISPR/Cas9.
  • HY-N3376
    Liriodenine

    Spermatheridine; VLT045

    Others Cancer
    Liriodenine (Spermatheridine; VLT045) is an aporphine alkaloid isolated from the plant Mitrephora sirikitiae and has anti-cancer activities. Liriodenine induces cell apoptosis, activates the intrinsic pathway by induction of caspase-3 and caspase-9.
  • HY-100738
    Ubiquitin Isopeptidase Inhibitor I, G5

    NSC144303

    Apoptosis Cancer
    Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303) is an apoptosome-independent caspase and apoptosis activator with IC50 values of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively.
  • HY-N6727
    Gliotoxin

    Aspergillin

    Apoptosis PKA NF-κB Bacterial Fungal Antibiotic Infection Inflammation/Immunology
    Gliotoxin is a secondary metabolite, the most abundant mycotoxin secreted by A. fumigatus, inhibits the phagocytosis of macrophages and the immune functions of other immune cells . Gliotoxin inhibits inducible NF-κB activity by preventing IκB degradation, which consequently induces host-cell apoptosis. Gliotoxin activates PKA and increases intracellular cAMP concentration; modulates actin cytoskeleton rearrangement to facilitate A. fumigatus internalization into lung epithelial cells.
  • HY-N6690
    Destruxin B

    Bcl-2 Family Caspase Apoptosis Cancer Infection
    Destruxin B, isolated from entomopathogenic fungus Metarhizium anisopliae, is one of the cyclodepsipeptides with insecticidal and anticancer activities. Destruxin B induces apoptosis via a Bcl-2 Family-dependent mitochondrial pathway in human nonsmall cell lung cancer cells. Destruxin B significantly activates caspase-3 and reduces tumor cell proliferation through caspase-mediated apoptosis, not only in vitro but also in vivo.
  • HY-N6872
    Actein

    JNK Akt Apoptosis Autophagy Cancer
    Actein is a triterpene glycoside isolated from the rhizomes of Cimicifuga foetida. Actein suppresses cell proliferation, induces autophagy and apoptosis through promoting ROS/JNK activation, and blunting AKT pathway in human bladder cancer. Actein has little toxicity in vivo.
  • HY-B1899A
    Taurodeoxycholic acid sodium hydrate

    Sodium taurodeoxycholate monohydrate

    Caspase Metabolic Disease Inflammation/Immunology
    Taurodeoxycholic acid sodium hydrate (Sodium taurodeoxycholate monohydrate) prevents apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid sodium hydrate is investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis.
  • HY-N6861
    Lucidenic acid B

    Apoptosis Cancer
    Lucidenic acid B is a natural compound isolated from Ganoderma lucidum, induces apoptosis of cancer cells, and causes the activation of caspase-9 and caspase-3, and cleavage of PARP. Lucidenic acid B does not affect the cell cycle profile, or the number of necrotic cells.
  • HY-19619
    m-3M3FBS

    Phospholipase Apoptosis Cancer
    m-3M3FBS is a potent phospholipase C (PLC) activator. m-3M3FBS stimulates superoxide generation in human neutrophils, upregulates intracellular calcium concentration, and stimulates inositol phosphate generation in various cell lines. m-3M3FBS induces monocytic leukemia cell apoptosis.
  • HY-P1061A
    Colivelin TFA

    STAT Amyloid-β Neurological Disease
    Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin TFA exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin TFA has the potential for the treatment of alzheimer's disease and ischemic brain injury.
  • HY-10619B
    Niraparib tosylate

    MK-4827 tosylate

    PARP Apoptosis Cancer
    Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • HY-14590
    Kaempferol

    Kempferol; Robigenin

    Estrogen Receptor/ERR Autophagy Mitophagy Apoptosis HIV Parasite Endogenous Metabolite Cancer
    Kaempferol (Kempferol), a flavonoid found in many edible plants, inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK. Kaempferol can be uesd for the research of breast cancer.
  • HY-125355
    SEC

    Apoptosis Cancer
    SEC induces activation of ANXA7 GTPase via the AMPK/mTORC1/STAT3 signaling pathway. SEC selectively promotes apoptosis in cancer cells, expressing a high level of ITGB4 by inducing ITGB4 nuclear translocation.
  • HY-15615A
    TIC10

    ONC-201

    TNF Receptor Apoptosis Cancer
    TIC10 is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer which acts by inhibiting Akt and ERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. TIC10 can cross the blood-brain barrier.
  • HY-N1970
    5,7-Dihydroxychromone

    Keap1-Nrf2 Arenavirus Caspase PARP Neurological Disease
    5,7-Dihydroxychromone, the extract of Cudrania tricuspidata, activates Nrf2/ARE signal and exerts neuroprotective effects against 6-hydroxydopamine (6-OHDA)-induced oxidative stress and apoptosis. 5,7-Dihydroxychromone inhibits the expression of activated caspase-3 and caspase-9 and cleaved PARP in 6-OHDA-induced SH-SY5Y cells.
  • HY-10619
    Niraparib

    MK-4827

    PARP Apoptosis Cancer
    Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • HY-10619A
    Niraparib hydrochloride

    MK-4827 hydrochloride

    PARP Apoptosis Cancer
    Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • HY-B0075
    Melatonin

    N-Acetyl-5-methoxytryptamine

    Melatonin Receptor Autophagy Mitophagy Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress.
  • HY-10201
    Sorafenib

    Bay 43-9006

    Raf VEGFR FLT3 Autophagy Apoptosis Ferroptosis Cancer
    Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator.
  • HY-18980
    Rottlerin

    Mallotoxin; NSC 56346; NSC 94525

    PKC Autophagy Apoptosis Infection Cancer
    Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation.
  • HY-10201A
    Sorafenib Tosylate

    Bay 43-9006 Tosylate

    Raf VEGFR FLT3 Autophagy Ferroptosis Apoptosis Cancer
    Sorafenib Tosylate (Bay 43-9006 Tosylate) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. SorafenibTosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib Tosylate induces autophagy and apoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib Tosylate is a ferroptosis activator.
  • HY-W011434
    Triglycidyl isocyanurate

    TGIC; Teroxirone

    MDM-2/p53 Cancer Inflammation/Immunology
    Triglycidyl isocyanurate (TGIC; Teroxirone) is a triazene triepoxide with antiangiogenic and antineoplastic activities. Triglycidyl isocyanurate inhibits the growth of non-small-cell-lung cancer cells via p53 activation. Triglycidyl isocyanurate induces cell apoptosis. Triglycidyl isocyanurate can be used for cancer research.
  • HY-19759
    SRT 2183

    Sirtuin Apoptosis Cancer
    SRT 2183 is a selective Sirtuin-1 (SIRT1) activator with an EC1.5 value of 0.36 μM. SRT 2183 induces growth arrest and apoptosis, concomitant with deacetylation of STAT3 and NF-κB, and reduction of c-Myc protein levels.
  • HY-13434
    Ionomycin

    SQ23377

    Calcium Channel PKC Bacterial Apoptosis Antibiotic Cancer Infection
    Ionomycin (SQ23377) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin (SQ23377) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin (SQ23377) promotes apoptosis. Ionomycin also induces the activation of protein kinase C (PKC).
  • HY-B0075S
    Melatonin D4

    N-Acetyl-5-methoxytryptamine D4

    Melatonin Receptor Autophagy Mitophagy Cancer Inflammation/Immunology Neurological Disease
    Melatonin D4 is deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Antioxidative and anti-inflammatory properties. Melatonin is a selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation.
  • HY-N7043
    Isosilybin A

    Apoptosis Cancer
    Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis.
  • HY-W058849
    MT 63-78

    AMPK mTOR Apoptosis Cancer
    MT 63-78 is a specific and potent direct AMPK activator with an EC50 of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis. MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects.
  • HY-N1381
    Periplocin

    Apoptosis Cancer Inflammation/Immunology
    Periplocin is a cardiotonic steroid isolated from Periploca forrestii. Periplocin promotes tumor cell apoptosis and inhibits tumor growth. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase.
  • HY-110084
    BTZO-1

    Apoptosis Cardiovascular Disease
    BTZO-1 binds to Macrophage migration inhibitory factor (MIF) with a Kd value of 68.6 nM, and its binding requires the N-terminal Pro1. BTZO-1 can activate antioxidant response element (ARE)-mediated gene expression and suppress oxidative stress-induced cardiomyocyte apoptosis in vitro.
  • HY-N0817
    Polyphyllin G

    Apoptosis Autophagy Bacterial Cancer Inflammation/Immunology
    Polyphyllin G is isolated from the rhizomes of Paris yunnanensis, with antimicrobial and anticancer activity. Polyphyllin G prevents the growth of both Gram-positive and Gram-negative bacteria with minimum inhibitory concentrations (MICs). Polyphyllin G induces apoptosis dependent on the activations of caspase-8, -3, and -9, induces autophagy.
  • HY-P2343
    BH3 hydrochloride

    Apoptosis Cancer
    BH3 hydrochloride, a BBB penetrated peptide, provoke apoptosis either by direct activation of pro-apoptotic Bax/Bak or by neutralizing anti-apoptotic Bcl-2 proteins (Bcl-2, Bcl-XL, Bcl-w, Mcl-1 and A-1) via their BH3 domian.
  • HY-122534
    Mensacarcin

    Mitochondrial Metabolism ADC Cytotoxin Apoptosis Cancer
    Mensacarcin, a highly complex polyketide, strongly inhibits cell growth universally in cancer cell lines and potently induces apoptosis in melanoma cells. Mensacarcin targets to mitochondria, affects energy metabolism in mitochondria, and activates caspase-dependent apoptotic pathways. Mensacarcin, an antibiotic, can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
  • HY-N0179
    Ecdysone

    α-Ecdysone

    Endogenous Metabolite Apoptosis Metabolic Disease
    Ecdysone (α-Ecdysone), a major steroid hormone in insects and herbs, triggers mineralocorticoid receptor (MR) activation and induces cellular apoptosis. Ecdysone plays essential roles in coordinating developmental transitions and homeostatic sleep regulation through its active metabolite 20-hydroxyecdysone (Crustecdysone; 20E; HY-N6979).
  • HY-135897
    Urolithin C

    Calcium Channel Reactive Oxygen Species Apoptosis Endogenous Metabolite Metabolic Disease
    Urolithin C, a gut-microbial metabolite of Ellagic acid, is a glucose-dependent activator of insulin secretion. Urolithin C is a L-type Ca 2+ channel opener and enhances Ca 2+ influx. Urolithin C induces cell apoptosis through a mitochondria-mediated pathway and also stimulates reactive oxygen species (ROS) formation.
  • HY-129239
    ASLAN003

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Apoptosis Cancer
    ASLAN003 is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. ASLAN003 inhibits protein synthesis via activation of AP-1 transcription factors. ASLAN003 induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice.
  • HY-N6693
    Valinomycin

    NSC 122023

    Bacterial Apoptosis Antibiotic Infection
    Valinomycin (NSC 122023) is a cyclic depsipeptide antibiotic first isolated from Streptomyces fulvissimus, act as a potassium selective ionophore. Valinomycin (NSC 122023) inhibits lymphocyte proliferation by its effects on the cell membrane, and induces apoptosis in CHO cells. Valinomycin induces activation of PINK1 leading to Parkin Ser65 phosphorylation.
  • HY-125858
    MI-1061

    MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53, induces apoptosis, and has anti-tumor activity.
  • HY-15598
    20-HETE

    20-hydroxy Arachidonic Acid

    Potassium Channel NF-κB NO Synthase Reactive Oxygen Species NADPH Oxidase Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease
    20-HETE (20-hydroxy Arachidonic Acid) is a CYP450 metabolite and a potent vasoconstrictor. 20-HETE is an endogenous inhibitor of the large-conductance Ca 2+-activated K + channel in renal arterioles. 20-HETE constricts smooth muscles, stimulates smooth muscle proliferation and migration. 20-HETE increases NADPH oxidase, ROS, and NF-κB activity. 20-HETE also inhibits endothelial NO synthase and inhibits apoptosis of pulmonary artery smooth muscle cells.
  • HY-N0636
    Eriocitrin

    Apoptosis Cancer
    Eriocitrin is a flavonoid isolated from lemon, which is a strong antioxidant agent. Eriocitrin could inhibit the proliferation of hepatocellular carcinoma cell lines by arresting cell cycle in S phase through up-regulation of p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating mitochondria-involved intrinsic signaling pathway.
  • HY-116364
    AZT triphosphate

    3'-Azido-3'-deoxythymidine-5'-triphosphate

    HIV DNA/RNA Synthesis HBV Reactive Oxygen Species Apoptosis Infection
    AZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate also inhibits the DNA polymerase of HBV. AZT triphosphate activates the mitochondria-mediated apoptosis pathway.
  • HY-128588
    STAT3-IN-3

    STAT Cancer
    STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity. STAT3-IN-3 induces apoptosis in breast cancer cells. STAT3-IN-3 acts as a promising mitochondria-targeting STAT3 inhibitor for cancer research.
  • HY-10108
    LY294002

    PI3K Casein Kinase DNA-PK Autophagy Apoptosis Cancer Infection
    LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitorr that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an autophagy and apoptosis activator.
  • HY-13434A
    Ionomycin calcium

    SQ23377 calcium

    Calcium Channel PKC Bacterial Apoptosis Antibiotic Cancer Infection
    Ionomycin calcium (SQ23377 calcium) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin calcium (SQ23377 calcium) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin (SQ23377) promotes apoptosis. Ionomycin calcium (SQ23377 calcium) also induces the activation of protein kinase C (PKC).
  • HY-18676
    OSU-T315

    Integrin Autophagy Apoptosis Cancer
    OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner. OSU-T315 causes cell death through apoptosis and autophagy.
  • HY-116364A
    AZT triphosphate TEA

    3'-Azido-3'-deoxythymidine-5'-triphosphate TEA

    HIV DNA/RNA Synthesis HBV Reactive Oxygen Species Apoptosis Infection
    AZT triphosphate TFA (3'-Azido-3'-deoxythymidine-5'-triphosphate TFA) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TFA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TFA also inhibits the DNA polymerase of HBV. AZT triphosphate TFA activates the mitochondria-mediated apoptosis pathway.
  • HY-13716
    Noscapine

    (S,R)-Noscapine

    Opioid Receptor Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can crosse the blood-brain barrier.
  • HY-101761
    TM5441

    PAI-1 Apoptosis Cancer
    TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM and induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence.
  • HY-13716A
    Noscapine hydrochloride

    (S,R)-Noscapine hydrochloride

    Opioid Receptor Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Noscapine hydrochloride ((S,R)-Noscapine hydrochloride) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine hydrochloride exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine hydrochloride disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine hydrochloride possesses anticancer, neuroprotective, anti-inflammatory activities, and can crosse the blood-brain barrier.
  • HY-W046353
    2-Methoxycinnamaldehyde

    o-Methoxycinnamaldehyde

    Apoptosis Cancer
    2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound of Cinnamomum cassia, with antitumor activity. 2-Methoxycinnamaldehyde inhibits proliferation and induces apoptosis by mitochondrial membrane potential (ΔΨm) loss, activation of both caspase-3 and caspase-9. 2-Methoxycinnamaldehyde effectively inhibits platelet-derived growth factor (PDGF)-induced HASMC migration.
  • HY-107738
    Guggulsterone

    Z/E-Guggulsterone

    Apoptosis JNK Akt Caspase FXR Autophagy Cancer
    Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively.
  • HY-10254
    PD0325901

    PD325901

    MEK Autophagy Apoptosis Cancer
    PD0325901 (PD325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC50 of 0.33 nM. PD0325901 exhibits a Ki app of 1 nM against activated MEK1 and MEK2. PD0325901 suppresses the expression of p-ERK1/2 and induces apoptosis. PD0325901 has anti-cancer activity for a broad spectrum of human tumor xenografts.
  • HY-13027
    DAPT

    GSI-IX

    γ-secretase Amyloid-β Autophagy Notch Apoptosis Cancer Inflammation/Immunology Neurological Disease
    DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC50s of 115 nM and 200 nM for total amyloid-β (Aβ) and 42, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment.
  • HY-108556A
    RWJ-56110 dihydrochloride

    Protease-Activated Receptor (PAR) Apoptosis Cardiovascular Disease
    RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.
  • HY-15036
    Diclofenac

    COX Apoptosis Inflammation/Immunology
    Diclofenac is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
  • HY-N2787
    8-​Prenylnaringenin

    Apoptosis Cancer
    8-prenylnaringenin is a prenylflavonoid isolated from hop cones (Humulus lupulus), with cytotoxicity. 8-prenylnaringenin has anti-proliferative activity against HCT-116 colon cancer cells via induction of intrinsic and extrinsic pathway-mediated apoptosis. 8-Prenylnaringenin also promotes recovery from immobilization-induced disuse muscle atrophy through activation of the Akt phosphorylation pathway in mice .
  • HY-P1075
    CALP3

    Calcium Channel Cancer Neurological Disease
    CALP3, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ channels and pumps. CALP3 has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.
  • HY-15038
    Diclofenac potassium

    COX Apoptosis Inflammation/Immunology
    Diclofenac potassium is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac potassium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
  • HY-P1077
    CALP1

    Calcium Channel mGluR Phosphodiesterase (PDE) Inflammation/Immunology
    CALP1 is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity.
  • HY-15036A
    Diclofenac diethylamine

    COX Apoptosis Inflammation/Immunology
    Diclofenac diethylamine is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac diethylamine induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
  • HY-P1077A
    CALP1 TFA

    Calcium Channel mGluR Phosphodiesterase (PDE) Inflammation/Immunology
    CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity.
  • HY-10626
    T0901317

    LXR FXR ROR Apoptosis Cancer Metabolic Disease Cardiovascular Disease
    T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα. T0901317 activates FXR with an EC50 of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.
  • HY-15037
    Diclofenac Sodium

    GP 45840

    COX Apoptosis Inflammation/Immunology
    Diclofenac Sodium (GP 45840) is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac Sodium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
  • HY-115463
    EB-3D

    AMPK Apoptosis Cancer
    EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity.
  • HY-N2447
    Amarogentin

    AMPK Apoptosis Cancer Metabolic Disease
    Amarogentin is a secoiridoid glycoside that is mainly extracted from Swertia and Gentiana roots. Amarogentin exhibits many biological effects, including anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin exerts hepatoprotective and immunomodulatory effects. Amarogentin promotes apoptosis, arrests G2/M cell cycle and downregulates of PI3K/Akt/mTOR signalling pathways. Amarogentin exerts beneficial vasculo-metabolic effect by activating AMPK.
  • HY-19618
    BRD3308

    HDAC HIV Infection Metabolic Disease
    BRD3308 is a highly selective HDAC3 inhibitor with an IC50 of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 (IC50 of 1.26 μM) or HDAC2 (IC50 of 1.34 μM). BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines or glucolipotoxic stress, and increases functional insulin release. BRD3308 activates HIV-1 transcription and disrupts HIV-1 latency.
  • HY-116624
    MAZ51

    VEGFR Apoptosis Cancer
    MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity.
  • HY-16350
    NKP-1339

    IT-139; KP-1339

    DNA/RNA Synthesis Apoptosis Cancer
    NKP-1339 (IT-139; KP-1339) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. NKP-1339 induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway. NKP-1339 has a high tumor targeting potential, strongly binds to serum proteins such as albumin and transferrin and activates in the reductive tumor milieu.
  • HY-123931
    ZLDI-8

    Notch Phosphatase Apoptosis Cancer
    ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC50 of 31.6 μM and a Ki of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC50 of 5.32 μM.
  • HY-N0103A
    Sophocarpine monohydrate

    Autophagy Apoptosis PI3K Akt Influenza Virus Cancer Infection Inflammation/Immunology
    Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine (monohydrate) significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine (monohydrate) has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
  • HY-122815
    Fusicoccin

    Fusicoccin A

    Apoptosis Cancer
    Fusicoccin (Fusicoccin A), a fungal pytotoxin, is a stabilizer of specific 14-3-3 protein-protein interactions. Fusicoccin sabilizes H +-ATPase/14-3-3 cmplex in pants, maintaining the enzyme in activated state. Fusicoccin also stabilizes 14-3-3 protein interactions with binding partners containing a C-terminal 14-3-3 recognition motif (a mode 3 motif), such as ERα, GPIbα, TASK3, CTFR, and p53. Fusicoccin induces apoptosis in cancer cells and has anticancer activity.
  • HY-N0103
    Sophocarpine

    Autophagy Apoptosis PI3K Akt Influenza Virus Cancer Infection Inflammation/Immunology
    Sophocarpine is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
  • HY-19896
    COTI-2

    MDM-2/p53 Apoptosis Cancer
    COTI-2, an anti-cancer drug with low toxicity, is an orally available third generation activator of p53 mutant forms. COTI-2 acts both by reactivating mutant p53 and inhibiting the PI3K/AKT/mTOR pathway. COTI-2 induces apoptosis in multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutant p53 to wild-type conformation.
  • HY-N6818
    5,​7,​4'-​Trimethoxyflavone

    Apoptosis Caspase PARP Cancer
    5,7,4'-Trimethoxyflavone is isolated from Kaempferia parviflora (KP) that is a famous medicinal plant from Thailand. 5,7,4'-Trimethoxyflavone induces apoptosis, as evidenced by increments of sub-G1 phase, DNA fragmentation, annexin-V/PI staining, the Bax/Bcl-xL ratio, proteolytic activation of caspase-3, and degradation of poly (ADP-ribose) polymerase (PARP) protein.5,7,4'-Trimethoxyflavone is significantly effective at inhibiting proliferation of SNU-16 human gastric cancer cells in a concentration dependent manner.
  • HY-N6002
    3'-Hydroxypterostilbene

    Apoptosis Autophagy Cancer
    3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 µM for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the PI3K/Akt/mTOR/p70S6K, and p38MAPK pathways and activates the ERK1/2, JNK1/2 MAPK pathways.
  • HY-121638A
    (5Z,2E)-CU-3

    Apoptosis Cancer
    (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.
  • HY-136065A
    bpV(phen) hydrate

    PTEN Phosphatase Parasite Apoptosis Cancer Infection Metabolic Disease Inflammation/Immunology
    bpV(phen) hydrate is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) hydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) hydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) hydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
  • HY-136065
    bpV(phen)

    PTEN Phosphatase Parasite Apoptosis Cancer Infection Metabolic Disease Inflammation/Immunology
    bpV(phen) is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
  • HY-108543
    NSC 95397

    Phosphatase Apoptosis Cancer
    NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor (Ki=32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C); IC50=22.3 nM (human Cdc25A), 56.9 nM (human Cdc25C), 125 nM (Cdc25B)). NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway.
  • HY-N2515
    Ginsenoside Rk1

    NF-κB PI3K JAK Apoptosis Cancer Inflammation/Immunology
    Ginsenoside Rk1 is a unique component created by processing the ginseng plant (mainly Sung Ginseng, SG) at high temperatures. Ginsenoside Rk1 has anti-inflammatory effect, suppresses the activation of Jak2/Stat3 signaling pathway and NF-κB. Ginsenoside Rk1 has anti-tumor effect, antiplatelet aggregation activities, anti-insulin resistance, nephroprotective effect, antimicrobial effect, cognitive function enhancement, lipid accumulation reduction and prevents osteoporosis. Ginsenoside Rk1 induces cell apoptosis by triggering intracellular reactive oxygen species (ROS) generation and blocking PI3K/Akt pathway.