caspase

Caspase-3 activator 1 (compound 4b), a Ru(III) metal complex, effectively inhibits gastric tumor growth and metastasis by mediating caspase-3 cleavage. This cleavage enables Caspase-3 to process gasdermin E (GSDME), which results in the production of the GSDME-N terminus, leading to perforation of the gastric tumor cell membrane. Furthermore, compound 4b induces pyroptosis and subsequent immune responses. It can be incorporated with decitabine (DCT) into the 4b-DCT-Lip lipid delivery system [1].

Caspase-8-IN-1 is a potent caspase-8 inhibitor [1] .

Caspase-3 activator 3 (compound 2h) effectively induces apoptosis in HL-60 and K562 cells by substantially activating caspase-3, demonstrating antileukemic activity with IC50 values of 42.89 μM and 33.61 μM, respectively [1].

Caspase-3 Activator 2 (Compound 2f) is a caspase 3 activator with cytotoxic effects on HL-60 and K562 cells, exhibiting IC 50 values of 33.52 μM and 76.90 μM, respectively [1]. It facilitates apoptosis, rendering it useful in cancer research.

Z-DEVD-FMK, a Caspase-3 Inhibitor, is an irreversible, cell-permeable inhibitor of caspase-3/CPP32 that impedes tumor cell apoptosis. In vivo studies show it offers neuroprotection in rat hippocampi post-seizures and considerably diminishes post-traumatic apoptosis, enhancing neurological recovery in rats before and after traumatic brain injury induction.

Caspase-9 Inhibitor III (Ac-LEHD-cmk), a caspase-9 inhibitor, exhibits protective effects against ischemia-reperfusion-induced myocardial injury.

Caspase-6-IN-1 is a novel Allosteric Inhibitor of Caspase-6 Activation, blocking the interaction between C6 and mHTT1-586.

Caspase-3-IN-1 is a potent inhibitor of Caspase-3 (IC50: 14.5 nM).

Caspase-3/7 Activator 2 is a potent compound that selectively activates Caspase-3/7, demonstrating tumor specificity, anti-proliferative properties, and a high capacity for inducing apoptosis.

Caspase-3/7 Activator 3 is a potent and tumor-selective compound that effectively activates Caspase-3/7, demonstrating significant anti-proliferative activity and a high capacity to induce apoptosis.

Z-VAD-FMK (Caspase Inhibitor VI) is a broad-spectrum inhibitor of caspases.Z-VAD-FMK binds to activated caspases and inhibits apoptosis.Z-VAD-FMK does not inhibit UCHL1 activity, even at concentrations up to 440 μM.

Caspase-3 Inhibitor I (N-acetyl-asp-glu-val-asp-al) is a specific inhibitor of Caspase-3.

Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) is a selective caspase 8 inhibitor, which has cell permeable.

Z-DEVD-FMK (Caspase-3 Inhibitor) is a selective, irreversible Caspase-3 inhibitor, and also exhibits effective inhibition activity on caspase-6, caspase-7, caspase-8, and caspase-10.

Ac-YVAD-CMK (Ac-Tyr-Val-Ala-Asp-CMK) is a selective and irreversible inhibitor of Caspase-1 and inhibits pyroptosis, IL-1β and IL-18. Ac-YVAD-CMK shows neuroprotective and anti-inflammatory capacity.

MMPSI (Caspase-3/7 Inhibitor I) is a novel, non-peptide small molecule caspase 3 and caspase 7 inhibitor that reduces ischemic injury in isolated rabbit heart or cardiomyocytes and inhibits apoptosis of H16c2 cells in a concentration-dependent manner.MMPSI can be used to study cardioprotection and myocardial injury.

Ivachtin (Caspase-3 Inhibitor VII) is a nonpeptide, noncompetitive and reversibl caspase-3 inhibitor(IC50 = 23 nM) and is a modest inhibitor of the remaining caspases.

Procyanidin C1 is a natural product, with anti-inflammatory effects, and induces apoptosis.

Anisperimus (LF 15-0195) is an immunosuppressant that enhances activation-induced T-cell death by promoting caspase-8 and caspase-10 activation at the DISC level, and prevents CNS autoimmunity by promoting the development of Foxp3-expressing regulatory CD4 T cells.

Iptacopan (LNP023) is an inhibitor with high affinity for factor B.

Z-VAD(OMe)-FMK is a pan-caspase inhibitor with irreversible properties; Z-VAD(OMe)-FMK is also an inhibitor of ubiquitin C terminal hydrolase L1 (UCHL1), which is irreversibly modified by targeting the UCHL1 active site.

CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 ( OC2, a master regulator of androgen receptor) with a K d of 7.43 uM in SPR assays, directly binds to OC2-HOX domain. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the mouse model of prostate cancer [1]

1. Chelidonine (Stylophorin) isolated from Chelidonium majus efficiently induced apoptosis in HeLa cells through possible alteration of p38-p53 and AKT/PI3 kinase signalling pathways. 2. Chelidonine is a promising model compound for overcoming MDR and for enhancing cytotoxicity of chemotherapeutics, especially against leukaemia cells, its efficacy needs to be confirmed in animal models. 3. Chelidonine may be a potential therapeutic agent against metastasis of invasive human cancer cells, exhibits antimigratory and antiinvasive effects in MDA-MB-231 cells, by suppressing COL-induced integrin signaling, through inhibiting the formation of the IPP complex and subsequent downregulation of IPP downstream signaling molecules, such as Akt and ERK1/2.

Diclofenac Potassium (CGP-45840B) is a nonsteroidal anti-inflammatory drug taken to reduce inflammation and as an analgesic reducing pain in certain conditions.

2-methoxycinnamaldehyde is a natural compound of Cinnamomum cassia,has been widely studied with regard to its antitumor activity.

Belnacasan (VX-765) is an orally active IL-converting enzyme/caspase-1 inhibitor.

1. Bufotalin (Bufotaline)e is a kind of poisonous secretions of toads.

1. Orientin (Luteolin-8-glucoside) may be regarded as a candidate therapeutic agent for treatment of vascular inflammatory diseases via inhibition of the HMGB1 signaling pathway. 2. Orientin protects vascular barrier integrity by inhibiting hyperpermeability, expression of CAMs, and adhesion and migration of leukocytes, thereby endorsing its usefulness as a therapy for vascular inflammatory diseases. 3. Orientin has neuroprotection effect by the intracellular mediation of caspase activity; may alleviate cognitive deficits and oxidative stress in AD mice; can exert antidepressant-like effects on CUMS mice, specifically by improving central oxidative stress, neurotransmission, and neuroplasticity.

1. Glaucocalyxin A (Leukamenin F)-SBE-β-CD could be useful with a better solubility and sustained function in drug delivery. 2. Glaucocalyxin A activates caspase-3, decreases BAD phosphorylation, and reduces the expression of X-linked inhibitor of apoptosis protein. 3. Glaucocalyxin A inhibits Akt phosphorylation, suppresses proliferation, and promotes apoptosis in a dose-dependent manner, but not in normal glial cells. 4. Glaucocalyxin A inhibits collagen-stimulated tyrosine phosphorylation of Syk, LAT, and phospholipase Cγ2, the signaling events in collagen receptor GPⅥ pathway. 5. Glaucocalyxin A could potentially be developed as an antiplatelet and antithrombotic agent, can inhibit platelet p-selectin secretion and integrin activation by convulxin, is a GPVI selective ligand.

2-Methoxyestradiol (2-ME2) is an orally bioavailable estradiol metabolite with potential antineoplastic activity. 2-Methoxyestradiol inhibits angiogenesis by reducing endothelial cell proliferation and inducing endothelial cell apoptosis. This agent also inhibits tumor cell growth by binding to tubulin, resulting in antimitotic activity, and by inducing caspase activation, resulting in cell cycle arrest in the G2 phase, DNA fragmentation, and apoptosis.

Magnolin reduces the renal oxidative stress, suppresses caspase-3 activity, and increases Bcl-2 expression in vivo and in vitro. Magnolin has anti-inflammatory and antioxidative effects.

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead

TCH-165 is a small molecule modulator of proteasome assembly, resulting in an increase in 20S levels. The increase in the level of free 20S corresponds to enhanced proteolysis of IDPs.

Crustecdysone (Hydroxyecdysone) is a steroid hormone that regulates the processes of molting or ecdysis in insects.

VU0285655-1(BML-280) is a potent and selective phospholipase D2 (PLD2) inhibitor that inhibits the proliferation of PLD2-deficient cells.VU0285655-1 has an inhibitory effect on high glucose-induced caspase-3 cleavage and reduction of cell viability.VU0285655-1 is used in the study of diabetic retinopathy.

SKLB-163 acts by downregulating RhoGDI, activating JNK-1 signaling pathway and caspase-3, and reducing phosphorylated Akt and p44/42 MAPK.

Ac-YVAD-AOM is a selective and potent caspase-1 inhibitor showing antitumor activity and potential analgesic activity.

(-)-Anonaine can be extracted from several species of Magnoliaceae and Annelidae and has antimalarial, antibacterial, antifungal, antioxidant, anticancer, antidepressant and vasodilatory activities. (-)-Anonaine induces apoptosis in human cervical cancer (HeLa) cells, induces DNA damage and inhibits the growth and migration of human lung cancer h1299 cells through Bax and caspase-dependent pathways.

Arg-Gly-Asp-Ser acetate is an integrin binding sequence that directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1. Arg-Gly-Asp-Ser acetate inhibits integrin receptor function.

SF5 is an inhibitor of the apoptosis pathway. Which is through the JNK-p53-caspase apoptotic cascade.

EF24 (3,5-Bis[(2-fluorophenyl)Methylene]-4-piperidinone) treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK. EF24 shows potent anti-tumor activity in oral squamous cell carcinoma (OSCC) via deactivation of the MAPK/ERK signaling pathway.

PAF (C16) is a potent MAPK and MEK/ERK activator that induces increased vascular permeability. PAF (C16) (PAF (C16)) is a platelet-activating factor, a phospholipid-derived mediator and a ligand for PAF G protein-coupled receptor (PAFR). PAF (C16) has shown anti-apoptotic and anti-inflammatory activity in vitro, inhibiting Caspase-dependent apoptosis by interacting with its receptor (PAF-R) to perform cell signaling.

OUP-186 is a high affinity and human/rat species-selective antagonist of histamine H3 receptor. OUP-186 suppressed the proliferation of breast cancer cells. The IC50 values at 48 hours for OUP-186 was approximately 50 μM. OUP-186 potently induced cell dea

EP1013 is a broad-spectrum selective inhibitor of Caspase used in the study of type 1 diabetes.

Cysteine protease inhibitor 2 is a cysteine protease inhibitor. Cysteine protease inhibitor 2 inhibited DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.

GS-6201 (CVT-6883) is a selective antagonist of adenosine A2B receptor. GS-6201 shows high affinity and selectivity for the human adenosine A2B receptors with a Ki of 22 nM.

Ubiquitin Isopeptidase Inhibitor I, G5 is a caspase-independent inducer of cell necrosis that induces cell death via the death receptor pathway (IC50 of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively).

Fraxetin (7,8-dihydroxy-6-methoxy coumarin) has dual-antioxidative ,hepatoprotective and antihyperglycemic functions, it shows potent protective effects against CCl4 induced oxidative stress and hepatic fibrosis, has a marked inhibitory effect on S.aureus proliferation. It increased the level of Nrf2/ARE, and HO-1, inhibit the formation of ROS, cytochrome c release, activation of caspase-3 and 9, and suppressed the up-regulation of Bax.

Tauroursodeoxycholate sodium (TUDC) is an endoplasmic reticulum (ER) stress inhibitor, used for the treatment of gallstones and liver cirrhosis.

Citronellol ((±)-β-Citronellol) is used in insect repellents and perfumes and as a mite attractant.

Diclofenac (Diclofenacum) is a nonsteroidal benzeneacetic acid derivative with anti-inflammatory activity. Diclofenac binds and chelates both isoforms of cyclooxygenase (COX-1 and-2), thereby blocking the conversion of arachidonic acid to pro-inflammatory-proprostaglandins.

Diclofenac Epolamine (DHEP) is a non-steroidal anti-inflammatory agent (NSAID) with analgesic and antipyretic actions.

Diclofenac deanol is a nonsteroidal anti-inflammatory drug (NSAID) of the phenylacetic acid class with anti-inflammatory, analgesic, and antipyretic properties. Contrary to the action of many traditional NSAIDs, diclofenac inhibits cyclooxygenase (COX)-2 enzyme with greater potency than it does COX-1.

5-hydroxy Diclofenac is a metabolite of the NSAID diclofenac formed by the cytochrome P450 (CYP) isoform CYP3A4. Diclofenac is a non-selective COX inhibitor. It inhibits human COX-1 and -2 with IC50 values of 0.9-2.7 and 1.5-20 μM, respectively. Diclofenac inhibits ovine COX-1 and -2 with IC50 values of 60 and 220 nM, respectively.

Diclofenac sodium (GP 45840) is a non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.

Diclofenac Diethylamine, a non-selective COX inhibitor, is utilized as a nonsteroidal anti-inflammatory drug (NSAID).