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Ivachtin (Caspase-3 Inhibitor VII; compound 7a) is a nonpeptide, noncompetitive and reversibl caspase-3 inhibitor with an IC50 of 23 nM. Ivachtin has modest selectivity for the remaining caspases .
Caspase-3 activator 1 (compound 4b) is a Ru(III) metal complex that inhibits gastric tumor growth and metastasis. Caspase-3 activator 1 mediates caspase-3 cleavage, which in turn causes Caspase-3 to cleave gasdermin E (GSDME) to produce the GSDME-N terminus, causing gastric tumor cell membrane perforation. Caspase-3 activator 1 is capable of inducing pyroptosis and pyroptosis-induced immune responses and can be assembled with decitabine DCT (HY-A0004) into a 4b-DCT-Lip lipid delivery system .
Caspase-3 activator 2 (Compound 2f) is a caspase 3 activator that induces apoptosis and can be used in cancer research. Caspase-3 activator 2 is cytotoxic to HL-60 cells and K562 cells, with IC50 values of 33.52 μM and 76.90 μM respectively .
Caspase-3 activator 3 (compound 2h) induces apoptosis in HL-60 and K562 cells via significant caspase 3 activation. Caspase-3 activator 3 shows antileukemic acticity against HL-60 and K562 cells, with IC50 values of 42.89 and 33.61 μM, respectively .
Ac-DEVD-CMK (Caspase-3 Inhibitor III) is a selective and irreversible caspase-3 inhibitor. Ac-DEVD-CMK significantly inhibits apoptosis induced by high levels of glucose or 3,20-dibenzoate (IDB; HY-137295). Ac-DEVD-CMK can be used in a variety of experimental approaches to inhibit apoptosis [3].
Ac-DEVD-CMK (Caspase-3 Inhibitor III) TFA is a selective and irreversible caspase-3 inhibitor. Ac-DEVD-CMK TFA significantly inhibits apoptosis induced by high levels of glucose or 3,20-dibenzoate (IDB; HY-137295). Ac-DEVD-CMK TFA can be used in a variety of experimental approaches to inhibit apoptosis [3].
Caspase-3/7 activator 1 is an effective activator of Caspase-3/7. Caspase-3/7 activator 1 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability .
Caspase-3/7 activator 2 is an effective activator of Caspase-3/7. Caspase-3/7 activator 2 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability .
Caspase-3/7 activator 3 is an effective activator of Caspase-3/7. Caspase-3/7 activator 3 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability .
FITC-C6-DEVD-FMK, a fluorescently labeled caspase-3 inhibitor, can be used for detection of active caspase-3 in mammalian cells undergoing apoptosis. FITC-C6-DEVD-FMK provides a convenient means for sensitive detection of activated caspase-3 in living cells. Z-DEVD-FMK is a specific caspase-3 inhibitor .
Ac-ESMD-CHO is an inhibitor of caspase-3 and caspase-7. Ac-ESMD-CHO inhibits proteolytic cleavage of the caspase-3 precursor peptide (CPP32) at the Glu-Ser-Met-Asp (ESMD) site .
Raptinal, a agent that directly activates caspase-3, initiates intrinsic pathway caspase-dependent apoptosis. Raptinal is able to rapidly induce cancer cell death by directly activating the effector caspase-3, bypassing the activation of initiator caspase-8 and caspase-9 .
M826 is a potent, selective and reversible non-peptide caspase-3 inhibitor with an IC50 value of 0.005 μM for enzymatic activity against caspase-3. M826 displays potent anti-apoptotic activity in animal models in vitro and in vivo. M826 can be used for nervous system diseases research .
M50054 is a potent inhibitor of apoptosis. M50054 inhibits Etoposide-induced caspase-3 activation of U937 cells with an IC50 of 79 μg/mL. M50054 does not directly inhibit the enzymatic activity of caspase-3. M50054 can be used for the research anti-Fas-antibody-induced hepatitis and chemotherapy-induced alopecia .
Z-DEVD-AFC is a cell-permeant substrate for caspase-3, which causes a shift in fluorescence uponcleavage of the AFC fluorophore. Z-DEVD-AFC can be used to detect caspase-3-like enzymes activity .
Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Tauroursodeoxycholate (Tauroursodeoxycholic acid; TUDCA) sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
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 .
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 .
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 .
Lactonic sophorolipid is a natural antimicrobial surfactant for oral hygiene . Lactonic sophorolipid, a potential anticancer agent, induces apoptosis in human HepG2 cells through the caspase-3 pathway .
Emricasan (PF 03491390) is an orally active and irreversible pan-caspase inhibitor. Emricasan inhibits Zika virus (ZIKV)-induced increases in caspase-3 activity and protected human cortical neural progenitors .
Dehydrotrametenolic acid is a sterol isolated from the sclerotium of Poria cocos. Dehydrotrametenolic acid induces apoptosis through caspase-3 pathway. Dehydrotrametenolic acid has anti-tumor activity, anti-inflammatory, anti-diabetic effects .
Ac-DMQD-AMC is an inhibitor of caspase-3. Ac-DMQD-AMC is an aromatic amine using aminium-based coupling reagent HATU in the presence of 2,4,6-trimethylpyridine (TMP) .
Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK .
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 .
Demethoxyfumitremorgin C is a secondary metabolite of the marine fungus, Aspergillus fumigatus. Demethoxyfumitremorgin C induces prostate cancer cell apoptosis. Demethoxyfumitremorgin C activates caspase-3, -8, and -9, leading to PARP/ cleavage .
Z-DEVD-AMC is a selective caspase-3 substrate that can be measured by fluorescence spectrometry. AMC can be used as a fluorescence reference standard for AMC-based enzyme substrates including AMC-based caspase substrates .
Triclabendazole is an orally active parasite inhibitor. Triclabendazole has anti-Leishmania activity and induces gasdermin E (GSDME)-dependent pyroptosis by caspase-3 activation. Triclabendazole can be used for the research of fasciola hepatica[3].
Tauroursodeoxycholate-d5 is the deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Tauroursodeoxycholate-d4 is deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Limonin glucoside can be isolated from seeds of Citrus reticulata. Limonin glucoside induces activation of caspase-3. Limonin glucoside inhibits the proliferation of human colon adenocarcinoma (SW480) cells (IC50: 37.39 μM) .
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 .
Tauroursodeoxycholate-d4 (sodium) is the deuterium labeled Tauroursodeoxycholate sodium. Tauroursodeoxycholate (Tauroursodeoxycholic acid; TUDCA) sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Tauroursodeoxycholate-d4-1 is the deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Patuletin is a flavonol, that can be isolated from the flowers of Tagetes patula. Patuletin shows anti-proliferative activity against cancer cells. Patuletin causes significant nuclear fragmentation and has a great capacity to induce caspase-3 activation .
Z-FF-FMK is a selective cathepsin-L inhibitor. Z-FF-FMK can prevent β-amyloid to induce apoptotic changes such as activation of caspase-3, cleavage of the DNA repair enzyme, poly-ADP ribose polymerase, and DNA fragmentation .
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 .
Allethrin, a pyrethroid insecticide is a major mosquito repellent agent. Allethrin induces oxidative stress, apoptosis and calcium release in rat testicular carcinoma cells (LC540). Allethrin induces BCL-2, caspase-3 activation and release of intracellular calcium .
Apoptotic agent-2 (compound 14b) induces apoptosis by down-regulation of Bcl-2 and up-regulation of Bax and caspase-3. Apoptotic agent-2 exhibits anti-proliferative activities and can be used for cancer research .
3-Methoxy-9H-Carbazole induces caspase-3 activities and the cellular generation of eactive oxygen species. 3-Methoxy-9H-Carbazole inhibits cancer cell proliferation and induces apoptosis .
NVP 231 is a potent, specific, and reversible ceramide kinase (CerK) inhibitor(IC50=12 nM) that competitively inhibits binding of ceramide to CerK . NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage .
Antitumor agent-72 (compound 6w) is a potent anticancer agent. Antitumor agent-72 has anticancer activity and induces apoptosis through activation of caspase-3 and cleavage of PARP. Antitumor agent-72 can be used for cancer research .
Ac-WLA-AMC is a fluorogenic substrate of caspase-3. Ac-WLA-AMC is cleaved to release the fluorescent moiety 7-amino-4-methylcoumarin (AMC), which can be used to quantify the β5c subunit activity .
MTP is a PKM2 inhibitor. MTP induces cancer cell apoptosis by modulating caspase-3 activation. MTP induces autophagy and increases ROS generation. MTP also inhibits JAK2 signaling. MTP can be used for research of oral squamous cell carcinoma .
Agkistrodon halys batroxobin is a thrombin-like serine protease. Agkistrodon halys batroxobin reduces the expression of Sirt1 and extracellular signal-regulated kinase activation in brain tissue. Agkistrodon halys batroxobin reduces cleaved caspase-3 expression and inhibits neuronal apoptosis in rat .
MMPSI is a potent and selective small molecule caspase 3 and caspase 7 inhibitor with an IC50 of 1.7 μM for human caspase-3. MMPSI can significantly reduce ischemia-reperfusion-induced infarct size in the isolated rabbit heart, and reduce apoptosis in both the ischemic myocardium and isolated cardiomyocytes. MMPSI can be used for researching cardioprotection .
Sesaminol, isolated from Sesamum indicum, has antioxidative activity, Sesaminol inhibits lipid peroxidation and shows neuroprotection effect. Sesaminol potently inhibits MAPK cascades by preventing phosphorylation of JNK, p38 MAPKs, and caspase-3 but not ERK-MAPK expression [3] .
Physalin A is a withanolide isolated from Physalis alkekengi var. franchetii. Physalin A induces apoptosis associated with up-regulation of caspase-3 and caspase-8 expression. Physalin A induces autophagy, found to antagonize apoptosis in HT1080 cells. Physalin A has the potential for the research of cancer disease .
(S)-(-)-Perillic acid is a terpenoid plant extract with antimicrobial and anticancer activities. (S)-(-)-Perillic acid induces cell apoptosis and cell cycle arrest, and increases the levell of Bax, Bcl2, p21 and caspase-3 proteins. (S)-(-)-Perillic acid can be used for cancer and infection research [3].
Mofarotene (Ro 40-8757), an arotinoid, is anticancer compound. Mofarotene induces apoptosis, associated with mitochondrial membrane depolarization, activation of caspase-3 and -9, and enhanced production of reactive oxygen species. Mofarotene inhibits hematopoiesis in vitro by inhibiting maturation from primitive progenitor cells [3].
AMXT-1501 tetrahydrochloride is an orally active polyamine transport inhibitor. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells . Combination of DFMO and AMXT‐1501 induces caspase‐3 mediated apoptosis in NB cell lines .
Cystamine is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC50 value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD) [3].
Cystamine (dihydrochloride) is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC50 value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD) [3].
Fluorescein-6-carbonyl-Asp(OMe)-Glu(OMe)-Val-DL-Asp(OMe)-fluoromethylketone is a cell-permeable, non-toxic inhibitor that binds irreversibly to activated caspase-3 in apoptotic cells. The fluorescence intensity can be measured by flow cytometry, microwell plate reader, or fluorescence microscopy .
Cinchonine is a natural compound present in Cinchona bark with antimalarial, antitumor, anti-inflammatory, anti platelet-aggregation and anti-obesity properties. Cinchonine inhibits cells proliferation and autophagy and induces apoptosis through activation of Caspase-3. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells .
Crenulatin is a gallotannin that can be isolated from Rhodiola rosea. Crenulatin can be used as a biomarker to identify potentially adulterated R. rosea products. Crenulatin has dual- direction effects on apoptosis of cerebral microvascular endothelial cells, via regulating Fas/Bcl-2 expression and caspase-3 activity [3].
BML-280 (VU0285655-1) is a potent and selective phospholipase D2 (PLD2) inhibitor. BML-280 has the ability to prevent caspase-3 cleavage and reduction in cell viability induced by high glucose. BML-280 can be used for rheumatoid arthritis research .
Z-VDVAD-AFC is a fluorogenic substrate. Z-VDVAD-AFC is used to measure the activity of cysteine protease 3 (Caspase-3). Z-VDVAD-AFC undergoes hydrolysis to release 7-amino-4-trifluoromethylcoumarin (AFC). AFC is fluorescent under ultraviolet light and can emit fluorescent signals .
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 .
FPR2 agonist 2 is a potent and permeates the blood−brain barrier FPR2 agonist with an EC50 of 0.13 µM, 1.1 µM for FPR2 and FPR1, respectively. FPR2 agonist 2 inhibits the production of pro-inflammatory cytokines, counterbalances the changes in mitochondrial function, and inhibits caspase-3 activity .
Chlorin e6 is a photosensitizer and has strong absorption peaks at wavelength of 402 and 662 nm, as well as exhibiting intense fluorescence at 668 nm. Chlorin e6 has antimicrobial efficacy and anticancer activity. Chlorin e6 induces cell apoptosis via caspase-3 activation and can be used for the research of cancer [3].
HJC0416 is a potent and orally active STAT3 inhibitor. HJC0416 shows antiprolifeative activity and induces apoptosis. HJC0416 decreases the expression of p-STAT3 (Tyr-705), Cyclin D1 and increases the expression of cleaved caspase-3 protein. HJC0416 shows anti-tumor activity .
VEGFR-2-IN-40 is a VEGFR-2 inhibitor. VEGFR-2-IN-40 boosts early and late apoptosis. VEGFR-2-IN-40 decreases the levels immunomodulatory proteins TNF-α and IL-6 while showing a four-fold rise in an apoptotic marker caspase-3 .
Ac-FLTD-CMK, a gasdermin D (GSDMD)-derived inhibitor, is a specific inflammatory caspases inhibitor. Ac-FLTD-CMK is effective against caspases-1 (IC50 of 46.7 nM), caspases-4 (IC50 of 1.49 μM), caspases-5 (IC50 of 329 nM), and caspases-11 , but not the apoptotic caspases such as caspase-3 .
AC-VEID-CHO (TFA) is a peptide-derived caspase inhibitor and has potency of inhibition for Caspase-6, Caspase-3 and Caspase-7 with IC50 values of 16.2 nM, 13.6 nM and 162.1 nM, respectively. AC-VEID-CHO (TFA) can be used for the research of neurodegenerative conditions including Alzheimer’s and Huntington’s disease .
Akt1/Akt2-IN-2 (compound 7) is an allosteric dual Akt1 and Akt2 inhibitor (IC50=138 nM and 212 nM, respectively). Akt1/Akt2-IN-2 increases activity of caspase-3, and inhibits viability of a number of tumor cells .
Cannflavin A can be isolated from Cannabis sativa L. Cannflavin A has anti-cancer, neuroprotective and anti-inflammatory activity. Cannflavin A inhibits Aβ1-42 aggregation. Cannflavin A also inhibits kynurenine-3-monooxygenase (KMO). Cannflavin A activates apoptosis via caspase-3 cleavage [3] .
Talampanel (LY300164) is an orally and selective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor antagonis with anti-seizure activity . Talampanel (IVAX) has neuroprotective effects in rodent stroke models . Talampanel attenuates caspase-3 dependent apoptosis in mouse brain .
Koumine is an alkaloid separated from Gelsemium elegans, shows potent anti-tumor activity. Koumine up-regulates the Bax/Bcl-2 ratio and caspase-3 expression in human breast cancer cells . Koumine has anxiolytic, antistress, antipsoriatic, and analgesic activities [3], protects against the development of arthritis in Rheumatoid arthritis (RA) animal models .
DIDS is a dual inhibitor of ABCA1 and VDAC1. DIDS also inhibits RAD51, inhibiting RAD51-mediated homologous pairing and strand exchange reactions. DIDS inhibits anion exchange and binding to red blood cell membranes, inhibits the activation of caspase-3 and -9, and can be used in cancer research [3] .
DPP is a Platinum(IV) complex, bearing pterostilbene-derived axial ligand. DPP inhibit the JAK2-STAT3 pathway in breast cancer (BC) cells with antiproliferative activity, and activates caspase-3 and cleaved poly ADP-ribose polymerase to induces apoptosis. DPP promotes the maturation and antigen presentation of dendritic cells, and exhibits in vivo safety .
Pipernonaline is a piperine derivative with antiprostate cancer activity. Pipernonaline inhibits the proliferation of androgen-dependent/independent LNCaP/PC-3 prostate cells. Pipernonaline activates caspase-3 and promotes procaspase-3/PARP cleavage. Pipernonaline also mediates reactive oxygen species (ROS) production, increased intracellular Ca(2+), and mitochondrial membrane depolarization .
DIDS sodium salt (MDL101114ZA) is a dual inhibitor of ABCA1 and VDAC1. DIDS also inhibits RAD51, inhibiting RAD51-mediated homologous pairing and strand exchange reactions. DIDS inhibits anion exchange and binding to red blood cell membranes, inhibits the activation of caspase-3 and -9, and can be used in cancer research [3] .
CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound of Cinnamomum cassia, with antitumor activity [3]. 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 [3].
CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 hydrochloride induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the prostate cancer mouse model
Cystamine-d8 (dihydrochloride) is the deuterium labeled Cystamine (dihydrochloride)[1]. Cystamine (dihydrochloride) is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC50 value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD)[2][3][4].
Ganoderic acid T1 is a deacetylated derivative of Ganoderic acid T. Ganoderic acid T1 attenuates antioxidant defense system and induces apoptosis of cancer cells. Ganoderic acid T1 decreases mitochondrial membrane potential and activates caspase-9 and caspase-3, to trigger apoptosis. Ganoderic acid T1 also increases the generation of intracellular ROS to produce pro-oxidant activities and cytotoxicity .
Asperosaponin VI, A saponin component from Dipsacus asper, induces osteoblast differentiation through BMP‐2/p38 and ERK1/2 pathway . Asperosaponin Ⅵ inhibits apoptosis in hypoxia-induced cardiomyocyte by increasing the Bcl-2/Bax ratio and decreasing active caspase-3 expression, as well as enhancing of p-Akt and p-CREB .
Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca 2+ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis[3] .
Almorexant (ACT 078573) hydrochloride is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca 2+ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis[3] .
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 .
Dihydrocapsaicin, a capsaicin, is a potent and selective TRPV1 (transient receptor potential vanilloid channel 1) agonist. Dihydrocapsaicin reduces AIF, Bax, and Caspase-3 expressions, and increased Bcl-2, Bcl-xL and p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection following ischemic stroke via PI3K/Akt regulation in rat [3].
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) [3].
Anticancer agent 201 (Compound 2f) has IC50 values in the low micromolar range for multiple tumor cell lines. Anticancer agent 201 is highly cytotoxic to CCRF-CEM cells in vitro, inducing apotosis by activating caspase-3 in the intrinsic mitochondrial pathway and lysis of PARP, as well as reducing the expression of Bcl-2 and Bcl-XL proteins. Anticancer agent 201 can be used in cancer research .
Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
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 .
Tenuifolin is effective and has a protective action. Tenuifolin inhibits β-secretase decreases Aβ protein secretion, suppresses Aβ25-35 secretion, and subsequently caspase-3 and caspase-9 become active. Tenuifolin's ability to lower AChE activity, increase at the same time, increase the ability of the upper glands, and improve the ability to read and remember. Research on tenuifolin's potential for use in urinary disease (AD).
17-Hydroxy sprengerinin C (compound 10) is a glycoside compound isolated from rhizomes of Polygonatum sibiricum. 17-Hydroxy sprengerinin C possesses stronger anticancer activities. 17-Hydroxy sprengerinin C reduces the expression of Blc-2 and pro-caspase3 and increases the production of Bax .
Antitumor agent-36 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-36 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-36 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-36 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues .
Antitumor agent-37 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-37 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-37 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-37 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues .
Dasminapant (APG-1387), a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP). Dasminapant induces degradation of cIAP-1 and XIAP proteins, as well as caspase-3 activation and PARP cleavage, which leads to apoptosis. Dasminapant can be used for the research of hepatocellular carcinoma, ovarian cancer, and nasopharyngeal carcinoma [3] .
PT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity .
BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research .
BDS-I known as blood depressing substance, is a marine toxin which can be extracted from Anemonia sulcata. BDS-I is a specific inhibitor of Potassium Channel, targeting to Kv3.4. BDS-I inhibits Aβ1-42-induced enhancement of KV3.4 activity, caspase-3 activation, and abnormal nuclear morphology of NGF-differentiated PC-12 cells. BDS-I reverts the Aβ peptide-induced cell death .
Dihydrocapsaicin-d3is the deuterium labeledDihydrocapsaicin(HY-N0361) . Dihydrocapsaicin, a capsaicin, is a potent and selective TRPV1 (transient receptor potential vanilloid channel 1) agonist. Dihydrocapsaicin reduces AIF, Bax, and Caspase-3 expressions, and increased Bcl-2, Bcl-xL and p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection following ischemic stroke via PI3K/Akt regulation in rat [3] .
5,7,4’-Trimethoxyflavone can be isolated from the medicinal plant Kaempferia parviflora (KP). 5,7,4’-Trimethoxyflavone is a CFTR activator and EC50 is 64 μM. 5,7,4’-Trimethoxyflavone induces apoptosis, increases proteolytic activation of caspase-3, and degradation of ADP-ribose polymerase (PARP) protein. 5,7,4’-Trimethoxyflavone has antitumor activity. 5,7,4’-Trimethoxyflavone can be used to prevent skin aging and oxidative stress [3].
HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo .
Lacidipine- 13C8 is the deuterium labeled Lacidipine[1]. Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI)[2][3].
STAT3-IN-18 (compound SPP) is a platinum (IV) complex with an axial ligand derived from sandalwood. STAT3-IN-18 inhibits the JAK2-STAT3 pathway in breast cancer (BC) cells, with anti-proliferative activity. STAT3-IN-18 activates caspase-3 and increases cleaved polyADP-ribose polymerase to induce apoptosis. STAT3-IN-18 promotes maturation and antigen presentation of dendritic cells and demonstrates safety in vivo.
Antitumor photosensitizer-5 (Ru2) is a photosensitizer which effectively target tumor mitochondria with an IC50 of 0.3 μM for phototoxicity to A549 cells. Under 460 nm light irradiation, antitumor photosensitizer-5 induces the generation of reactive oxygen species and NADH depletion, causes mitochondrial damage and activation of caspase-3, inducing apoptosis and suppressing cell migration. Antitumor photosensitizer-5 has the potential to prevent the growth of malignant tumors, therefore, shows the potential to be applied to photodynamic therapy .
Lacidipine- 13C4 is 13C labeled Lacidipine (HY-B0347). Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
Anticancer agent 63 (compound 3h) shows active in reducing the viability of different cancer cell lines, including SW480, HeLa, A549 and MCF-7, with IC50 values at 24 h of 4.9, 11.5, 9.4, and 3.4 μM, respectively. Anticancer agent 63 induce apoptosis in MCF-7 cells via down-regulating the expression of Bcl-2 and up-regulating the expression of IL-2 and Caspase-3. Anticancer agent 63 also shows antioxidant activity .
p-nitro-Pifithrin-α, a cell-permeable analog of pifithrin-α, is a potent p53 inhibitor. p-nitro-Pifithrin-α suppresses p53-mediated TGF-β1 expression in HK-2 cells. p-nitro-Pifithrin-α inhibits the activation of caspase-3 by Zika virus (ZIKV) strains. p-nitro-Pifithrin-α attenuates steatosis and liver injury in mice fed a high-fat diet [4].
non-alcoholic fatty liver disease [3].
CDK1/2/4-IN-1 (compound 3a) is a potent CDK inhibitor with IC50 values of 1.47, 0.78 and 0.87 μM for CDK1, CDK2 and CDK4, respectively. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and induces apoptosis. CDK1/2/4-IN-1 elevates Bax, caspase-3, P53 levels and decreases Bcl-2 level. CDK1/2/4-IN-1 can be used for cancer research .
Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor (IC50: 14 nM) that efficiently targets triple-negative breast cancer cells. HDAC3-IN-2 is cytotoxic with an IC50 of 0.55 μM against 4T1 and an IC50 of 0.74 μM against MDA-MB-231. HDAC3-IN-2 has anti-tumor efficacy in vivo in tumor-bearing mouse models, selectively increasing the acetylation levels of H3K9, H3K27 and H4K12, increasing the contents of apoptosis-related caspase-3, caspase-7 and cytochrome c, and reducing Proliferation-related Bcl-2, CD44, EGFR, and Ki-67 levels .
Ac-VDVAD-AFC is a caspase-specific fluorescent substrate. Ac-VDVAD-AFC can measure caspase-3-like activity and caspase-2 activity and can be used for the research of tumor and cancer .
Juncuenin D induces caspase-3-mediated cytotoxicity in HT22 cells. Juncuenin D also has anti-bacterial activity against MRSA strains. Juncuenin D can be isolated from J. effusus .
KEA1-97 is a selective Thioredoxin-caspase 3 interaction disruptor (IC50=10 μM). KEA1-97 disrupts the interaction of thioredoxin with caspase 3, activates caspases, and induces apoptosis without affecting thioredoxin activity .
GPR is a three amino acid peptide. GPR can rescue cultured rat hippocampal neurons from Aβ-induced neuronal death by inhibiting caspase-3/p53 dependent apoptosis. GPR can be used for the research of Alzheimer's disease (AD).
Ac-DEVD-AMC is a fluorescent substrate of caspase-3/caspase-7. When treating Ac-DEVD-AMC with cell lysate, Ac-DEVD-AMC releases amino-4-methylcoumarin (AMC) for fluorescence detection, with an excitation wavelength of 380 nm and an emission wavelength of 460 nm [3].
Citronellol ((±)-Citronellol) is a monoterpene Pelargonium graveolens. Citronellol ((±)-Citronellol) induces necroptosis of cancer cell via up-regulating TNF-α, RIP1/RIP3 activities, down-regulating caspase-3/caspase-8 activities and increasing ROS (reactive oxygen species) accumulation .
Aristololactam I (AL-I), is the main metabolite of aristolochic acid I (AA-I), participates in the processes that lead to renal damage.
Aristololactam I (AL-I) directly injures renal proximal tubule cells, the cytotoxic potency of AL-I is higher than that of AA-I and that the cytotoxic effects of these molecules are mediated through the induction of apoptosis in a caspase-3-dependent pathway .
CAY10506 is a PPARγ ligand that can induce cell death and ROS production in a PPARγ-dependent manner in vitro. CAY10506 exhibits radiosensitizing effects, enhancing γ-radiations-induced apoptosis and caspase-3-mediated poly (ADP-ribose) polymerase (PARP) cleavage. CAY10506 can be used in cancer research .
Antitumor agent-78 is an antitumor agent, inhibits cancer cells growth and migration. Antitumor agent-78 triggers ferroptosis by inhibiting GPx-4 and elevating COX2. Antitumor agent-78 also activates intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and hinders Epithelial-mesenchymal transition (EMT) process of cancer cells .
Antitumor agent-77 is an antitumor agent, inhibits cancer cells growth and migration. Antitumor agent-77 triggers ferroptosis by inhibiting GPx-4 and elevating COX2. Antitumor agent-77 also activates intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and hinders Epithelial-mesenchymal transition (EMT) process of cancer cells .
Citronellol (Standard) is the analytical standard of Citronellol. This product is intended for research and analytical applications. Citronellol ((±)-Citronellol) is a monoterpene Pelargonium graveolens. Citronellol ((±)-Citronellol) induces necroptosis of cancer cell via up-regulating TNF-α, RIP1/RIP3 activities, down-regulating caspase-3/caspase-8 activities and increasing ROS (reactive oxygen species) accumulation .
MX1013 is a potent, irreversible dipeptide caspase inhibitor vith antiapoptotic activity. MX1013 inhibits recombinant human caspase 3 with an IC50 of 30 nM .
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 .
Neuroprotective agent 2 (Compd 28) is a potent neuroprotective agent which has a protective effect in both salsolinol and glutamate-induced neurodegeneration models. Neuroprotective agent 2 reduces oxidative stress and caspase-3/7 activity in the glutamate model .
2,3-Dihydro-3α-methoxynimbolide is a limonoid compound isolated from the extracts of bark, leaves, roots, and seeds of Azadirachta indica A. Juss. var. siamensis Valeton. 2,3-Dihydro-3α-methoxynimbolide exhibits potent cyto-toxicities against one or more cell lines. 2,3-Dihydro-3α-methoxynimbolide activates caspases-3, -8, and -9, while increases the ratio of Bax/Bcl-2. 2,3-Dihydro-3α-methoxynimbolide induces apoptosis via both mitochondrial and death receptor pathways in AZ521 .
WYC-209, a synthetic retinoid, is a retinoic acid receptor (RAR) agonist. WYC-209 induces apoptosis primarily via the caspase 3 pathway (IC50=0.19 μM for inmalignant murine melanoma TRCs), and has long-term effects with little toxicity .
Apoptotic agent-3 (compound 15f) promotes apoptosis through the potential mitochondria-mediated Bcl-2/Bax pathway and activation of the Caspase 3 pathway. Apoptotic agent-3 exhibits anti-proliferative activities and can be used for cancer research .
Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1.
EF24 is a curcumin analogue with greater anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK .
Malformin A1, a cyclic pentapeptide isolated from Aspergillus niger, possess a range of bioactive properties including antibacterial activity. Malformin A1 shows potent cytotoxic activities on human colorectal cancer cells. Malformin A1 induces apoptosis by activating PARP, caspase 3, -7, and -9 .
Senkyunolide I, isolated from Ligusticum chuanxiong Hort, is an anti-migraine compound. Senkyunolide I protects rat brain against focal cerebral ischemia-reperfusion injury by up-regulating p-Erk1/2, Nrf2/HO-1 and inhibiting caspase 3 .
Arg-Gly-Asp-Ser (TFA) is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser (TFA) directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1 .
PARP14 inhibitor H10, compound H 10, is a selective inhibitor against PARP14 (IC50=490 nM), over other PARPs (≈24 fold over PARP1). PARP14 inhibitor H10 induces caspase-3/7-mediated cell apoptosis .
SARS-CoV-2 Mpro-IN-6 is a covalent, irreversible and selective SARS-CoV-2 M pro inhibitor with an IC50 of 0.18 μM. SARS-CoV-2 Mpro-IN-6 does not inhibit human cathepsins B, F, K, and L, and caspase 3 .
Ac-DNLD-CHO (Ac-Asp-Asn-Leu-Asp-CHO) is a Caspase-3/7 inhibitor (IC50: 9.89, 245 nM respectively; Kiapp: 0.68, 55.7 nM respectively). Ac-DNLD-CHO can be used for research of caspase-mediated apoptosis diseases, such as neurodegenerative disorders and viral infection diseases .
Apoptosis inducer 9 induces apoptosis with IC50 value of 4.21 μM. Apoptosis inducer 9 induces apoptosis through the mitochondrial pathway and enhance the expression of Cl-caspase-3, Cl-caspase-9 and Cl-PARP. Apoptosis inducer 9 can be used the potential to develop new anti-proliferative agents .
Procyanidin C1 (PCC1), a natural polyphenol with oral activity, causes DNA damage, cell cycle arrest and induces apoptosis. Procyanidin C1 decreases the level of Bcl-2, but enhances BAX, caspase 3 and 9 expression in cancer cells. Procyanidin C1 shows senotherapeutic activity and increases lifespan in mice .
Pim-1 kinase inhibitor 10 (compound 13a) is a both competitive and non-competitive inhibitor of PIM-1/2 kinase. Pim-1 kinase inhibitor 10 can induce cell apoptosis and exhibits anticancer activity. Pim-1 kinase inhibitor 10 also induces caspase 3/7 activation .
Z-DEVD-R110 ((Z-Asp-Glu-Val-Asp)2-Rhodamine 110) is a fluorogenic caspase-3/7 substrate. Z-DEVD-R110 can be used to detect apoptosis. Z-DEVD-R110 is a rhodamine derivative with two four–amino acid (DEVD) peptides linked to the fuorophore .
2-Bromohexadecanoic acid (2-Bromopalmitic acid) can be converted to 2-bromopalmitate (2-BP). 2-BP is a palmitoylation inhibitor targeting DHHC (Asp-His-His-Cys) protein palmitoyltransferase. 2-BP inhibits palmitoylation of GSDME-C during pyroptosis and inhibits BAK/BAX-Caspase 3-GSDME pathway-mediated pyroptosis .
Anticancer agent 137 (8q) is a potent PI3k inhibitor. Anticancer agent 137 has broad-spectrum anticancer activity. Anticancer agent 137 induces G2/M cell cycle arrest and apoptosis. Anticancer agent 137 increases cleaved PARP, caspase 3, and 7. Anticancer agent 137 can be used in research of cancer .
AY254 is an analogue of AY77 (HY-138951). AY254 is ERK-biased PAR2 agonist with an EC50 of 2 nM. AY254 relieves cytokine-induced caspase 3/8 activation. AY254 also promotes scratch-wound healing and induced IL-8 secretion via PAR2-ERK1/2 signaling
RGD peptide (GRGDNP) is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) plays an important role in cell adhesion, migration, growth, and differentiation [3].
TD1092 is a pan-IAP degrader, degrades cIAP1, cIAP2, and XIAP. TD1092 activates Caspase 3/7, and promotes cancer cells apoptosis via IAP degradation. TD1092 inhibits TNFα mediated NF-κB pathway and reduces the phosphorylation of IKK, IkBα, p65, and p38. TD1092 can act as PROTAC, and is used for cancer research .
DCP-LA (FR236924), a linoleic acid derivative, selectively and directly activates PKCε. DCP-LA activates Ca( 2+)/calmodulin-dependent protein kinase II (CaMKII) and inhibits protein phosphatase-1 (PP-1) to stimulate AMPA receptor exocytosis. DCP-LA inhibits activation of caspase-3/-9 and protects neurons at least in part from oxidative stress-induced apoptosis [3].
RGD peptide (GRGDNP) TFA is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) TFA competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) TFA promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) TFA plays an important role in cell adhesion, migration, growth, and differentiation [3].
ASP3026 is a selective and orally active inhibitor of anaplastic lymphoma kinase (ALK). ASP3026 is a selective and oral active anaplastic lymphoma kinase (ALK) inhibitor with a IC50 value of 3.5 nM. ASP3026 can inhibit the phosphorylation of IGF-1R, STAT3, AKT and JNK proteins, and induce the cleavage of caspase 3 and PARP. It also inhibited ROS and ACK. ASP3026 can be used in anti-tumor research [3] .
GW779439X is a pyrazolopyridazine identified in an inhibitor of the S. aureus PASTA kinase Stk1. GW779439X potentiates the activity of β-lactam antibiotics against various MRSA and MSSA isolates, some even crossing the breakpoint from resistant to sensitive. GW779439X is an AURKA inhibitor and induces apoptosis by the caspases 3/7 pathway . MRSA:methicillin-resistant S. aureus; MSSA: methicillin-sensitive S. aureus
AKN-028, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3(FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 inhibits FLT3 autophosphorylation. AKN-028 induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 induces apoptosisby activation of caspase 3. AKN-028 can be used in research of acute myeloid leukemia (AML) .
Anticancer agent 56 (compound 4d) is a potent anti-cancer agent with agent-likeness properties, possessing anticancer activity against several cancer cell lines (IC50<3 μM). Anticancer agent 56 induces cell cycle arrest at G2/M phase and triggers mitochondrial apoptosis pathway. Anticancer agent 56 acts by accumulation of ROS, up regulation of BAX, down regulation of Bcl-2 and activation of caspases 3, 7, 9 .
AKN-028 acetate, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 acetate inhibits FLT3 autophosphorylation. AKN-028 acetate induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 acetate induces apoptosisby activation of caspase 3. AKN-028 acetate can be used in research of acute myeloid leukemia (AML).
Anticancer agent 58 (compound 16) has inhibitory activity against kinds of cancer cell lines, especially in A549 and T24 with IC50s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activating caspase 3/8/9 activity, and induces an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrial membrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model .
HDAC1-IN-5 is a potent HDAC1 inhibitor with IC50 values of 15 nM and 20 nM for HDAC1 and HDAC6, respectively. HDAC1-IN-5 can enhance the acetylation of histone H3 and α-tubulin, as well as promote the activation of caspase 3 in cancer cells, thereby inducing apoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitory activity against tumor growth in xenograft mice .
AR-42 (HDAC-42; OSU-HDAC42) is a potent, orally bioavailable pan-HDAC inhibitor (IC50=16 nM). AR-42 induces growth inhibition, cell-cycle arrest, apoptosis, and activation of caspases-3/7. AR-42 promotes hyperacetylation of H3, H4, and alpha-tubulin, and up-regulation of p21. AR-42 shows cytotoxicity against various human cancer cell lines .
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 [3]. Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection .
PI3K/AKT-IN-1 is an effective PI3K/AKT dual inhibitor (IC50 of 6.99, 4.01 and 3.36 μM for PI3Kγ, PI3Kδ and AKT, respectively). PI3K/AKT-IN-1 has anticancer activity and acts by inhibiting PI3K/AKT axis and inducing caspase 3 dependent apoptosis .
CAY10526 is a specific microsomal PGE2 synthase-1 (mPGES1) inhibitor. CAY10526 inhibits PGE2 production through the selective modulation of mPGES1 expression but does not affect COX-2. CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. CAY10526 reduces BCL-2 and BCL-XL (anti-apoptotic) protein levels and increases BAX and BAK (pro-apoptotic) as well as cleaved caspase 3 levels. CAY10526 inhibits cell viability (IC50<5 μM) in three melanoma cell lines expressing mPGES1 .
N1,N11-Diethylnorspermine (DENSPM) is a potent anticancer agent. N1,N11-Diethylnorspermine is a spermine analog that activates polyamine catabolism. N1,N11-Diethylnorspermine induces the release of cytochrome c from mitochondria, resulting in activation of caspase 3. N1,N11-Diethylnorspermine kills glioblastoma multiforme (GBM) cells through induction of SSAT (spermidine/spermine N1-acetyltransferase) coupled with H2O2 production [3].
T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research .
Z-DEVD-AFC is a cell-permeant substrate for caspase-3, which causes a shift in fluorescence uponcleavage of the AFC fluorophore. Z-DEVD-AFC can be used to detect caspase-3-like enzymes activity .
FITC-C6-DEVD-FMK, a fluorescently labeled caspase-3 inhibitor, can be used for detection of active caspase-3 in mammalian cells undergoing apoptosis. FITC-C6-DEVD-FMK provides a convenient means for sensitive detection of activated caspase-3 in living cells. Z-DEVD-FMK is a specific caspase-3 inhibitor .
Z-DEVD-AMC is a selective caspase-3 substrate that can be measured by fluorescence spectrometry. AMC can be used as a fluorescence reference standard for AMC-based enzyme substrates including AMC-based caspase substrates .
Ac-WLA-AMC is a fluorogenic substrate of caspase-3. Ac-WLA-AMC is cleaved to release the fluorescent moiety 7-amino-4-methylcoumarin (AMC), which can be used to quantify the β5c subunit activity .
DIDS sodium salt (MDL101114ZA) is a dual inhibitor of ABCA1 and VDAC1. DIDS also inhibits RAD51, inhibiting RAD51-mediated homologous pairing and strand exchange reactions. DIDS inhibits anion exchange and binding to red blood cell membranes, inhibits the activation of caspase-3 and -9, and can be used in cancer research [3] .
Ac-DEVD-AMC is a fluorescent substrate of caspase-3/caspase-7. When treating Ac-DEVD-AMC with cell lysate, Ac-DEVD-AMC releases amino-4-methylcoumarin (AMC) for fluorescence detection, with an excitation wavelength of 380 nm and an emission wavelength of 460 nm [3].
Agkistrodon halys batroxobin is a thrombin-like serine protease. Agkistrodon halys batroxobin reduces the expression of Sirt1 and extracellular signal-regulated kinase activation in brain tissue. Agkistrodon halys batroxobin reduces cleaved caspase-3 expression and inhibits neuronal apoptosis in rat .
Ac-DEVD-CMK (Caspase-3 Inhibitor III) TFA is a selective and irreversible caspase-3 inhibitor. Ac-DEVD-CMK TFA significantly inhibits apoptosis induced by high levels of glucose or 3,20-dibenzoate (IDB; HY-137295). Ac-DEVD-CMK TFA can be used in a variety of experimental approaches to inhibit apoptosis [3].
Ac-DEVD-CMK (Caspase-3 Inhibitor III) is a selective and irreversible caspase-3 inhibitor. Ac-DEVD-CMK significantly inhibits apoptosis induced by high levels of glucose or 3,20-dibenzoate (IDB; HY-137295). Ac-DEVD-CMK can be used in a variety of experimental approaches to inhibit apoptosis [3].
Ac-ESMD-CHO is an inhibitor of caspase-3 and caspase-7. Ac-ESMD-CHO inhibits proteolytic cleavage of the caspase-3 precursor peptide (CPP32) at the Glu-Ser-Met-Asp (ESMD) site .
Z-DEVD-AFC is a cell-permeant substrate for caspase-3, which causes a shift in fluorescence uponcleavage of the AFC fluorophore. Z-DEVD-AFC can be used to detect caspase-3-like enzymes activity .
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 .
Ac-DMQD-AMC is an inhibitor of caspase-3. Ac-DMQD-AMC is an aromatic amine using aminium-based coupling reagent HATU in the presence of 2,4,6-trimethylpyridine (TMP) .
Z-DEVD-AMC is a selective caspase-3 substrate that can be measured by fluorescence spectrometry. AMC can be used as a fluorescence reference standard for AMC-based enzyme substrates including AMC-based caspase substrates .
Z-FF-FMK is a selective cathepsin-L inhibitor. Z-FF-FMK can prevent β-amyloid to induce apoptotic changes such as activation of caspase-3, cleavage of the DNA repair enzyme, poly-ADP ribose polymerase, and DNA fragmentation .
Ac-WLA-AMC is a fluorogenic substrate of caspase-3. Ac-WLA-AMC is cleaved to release the fluorescent moiety 7-amino-4-methylcoumarin (AMC), which can be used to quantify the β5c subunit activity .
Fluorescein-6-carbonyl-Asp(OMe)-Glu(OMe)-Val-DL-Asp(OMe)-fluoromethylketone is a cell-permeable, non-toxic inhibitor that binds irreversibly to activated caspase-3 in apoptotic cells. The fluorescence intensity can be measured by flow cytometry, microwell plate reader, or fluorescence microscopy .
Z-VDVAD-AFC is a fluorogenic substrate. Z-VDVAD-AFC is used to measure the activity of cysteine protease 3 (Caspase-3). Z-VDVAD-AFC undergoes hydrolysis to release 7-amino-4-trifluoromethylcoumarin (AFC). AFC is fluorescent under ultraviolet light and can emit fluorescent signals .
AC-VEID-CHO (TFA) is a peptide-derived caspase inhibitor and has potency of inhibition for Caspase-6, Caspase-3 and Caspase-7 with IC50 values of 16.2 nM, 13.6 nM and 162.1 nM, respectively. AC-VEID-CHO (TFA) can be used for the research of neurodegenerative conditions including Alzheimer’s and Huntington’s disease .
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) [3].
BDS-I known as blood depressing substance, is a marine toxin which can be extracted from Anemonia sulcata. BDS-I is a specific inhibitor of Potassium Channel, targeting to Kv3.4. BDS-I inhibits Aβ1-42-induced enhancement of KV3.4 activity, caspase-3 activation, and abnormal nuclear morphology of NGF-differentiated PC-12 cells. BDS-I reverts the Aβ peptide-induced cell death .
Ac-VDVAD-AFC is a caspase-specific fluorescent substrate. Ac-VDVAD-AFC can measure caspase-3-like activity and caspase-2 activity and can be used for the research of tumor and cancer .
GPR is a three amino acid peptide. GPR can rescue cultured rat hippocampal neurons from Aβ-induced neuronal death by inhibiting caspase-3/p53 dependent apoptosis. GPR can be used for the research of Alzheimer's disease (AD).
Ac-DEVD-AMC is a fluorescent substrate of caspase-3/caspase-7. When treating Ac-DEVD-AMC with cell lysate, Ac-DEVD-AMC releases amino-4-methylcoumarin (AMC) for fluorescence detection, with an excitation wavelength of 380 nm and an emission wavelength of 460 nm [3].
Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1.
Malformin A1, a cyclic pentapeptide isolated from Aspergillus niger, possess a range of bioactive properties including antibacterial activity. Malformin A1 shows potent cytotoxic activities on human colorectal cancer cells. Malformin A1 induces apoptosis by activating PARP, caspase 3, -7, and -9 .
Arg-Gly-Asp-Ser (TFA) is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser (TFA) directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1 .
Ac-DNLD-CHO (Ac-Asp-Asn-Leu-Asp-CHO) is a Caspase-3/7 inhibitor (IC50: 9.89, 245 nM respectively; Kiapp: 0.68, 55.7 nM respectively). Ac-DNLD-CHO can be used for research of caspase-mediated apoptosis diseases, such as neurodegenerative disorders and viral infection diseases .
Z-DEVD-R110 ((Z-Asp-Glu-Val-Asp)2-Rhodamine 110) is a fluorogenic caspase-3/7 substrate. Z-DEVD-R110 can be used to detect apoptosis. Z-DEVD-R110 is a rhodamine derivative with two four–amino acid (DEVD) peptides linked to the fuorophore .
AY254 is an analogue of AY77 (HY-138951). AY254 is ERK-biased PAR2 agonist with an EC50 of 2 nM. AY254 relieves cytokine-induced caspase 3/8 activation. AY254 also promotes scratch-wound healing and induced IL-8 secretion via PAR2-ERK1/2 signaling
RGD peptide (GRGDNP) is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) plays an important role in cell adhesion, migration, growth, and differentiation [3].
RGD peptide (GRGDNP) TFA is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) TFA competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) TFA promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) TFA plays an important role in cell adhesion, migration, growth, and differentiation [3].
Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Tauroursodeoxycholate (Tauroursodeoxycholic acid; TUDCA) sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Dehydrotrametenolic acid is a sterol isolated from the sclerotium of Poria cocos. Dehydrotrametenolic acid induces apoptosis through caspase-3 pathway. Dehydrotrametenolic acid has anti-tumor activity, anti-inflammatory, anti-diabetic effects .
Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK .
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 .
Demethoxyfumitremorgin C is a secondary metabolite of the marine fungus, Aspergillus fumigatus. Demethoxyfumitremorgin C induces prostate cancer cell apoptosis. Demethoxyfumitremorgin C activates caspase-3, -8, and -9, leading to PARP/ cleavage .
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 .
Patuletin is a flavonol, that can be isolated from the flowers of Tagetes patula. Patuletin shows anti-proliferative activity against cancer cells. Patuletin causes significant nuclear fragmentation and has a great capacity to induce caspase-3 activation .
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 .
3-Methoxy-9H-Carbazole induces caspase-3 activities and the cellular generation of eactive oxygen species. 3-Methoxy-9H-Carbazole inhibits cancer cell proliferation and induces apoptosis .
Sesaminol, isolated from Sesamum indicum, has antioxidative activity, Sesaminol inhibits lipid peroxidation and shows neuroprotection effect. Sesaminol potently inhibits MAPK cascades by preventing phosphorylation of JNK, p38 MAPKs, and caspase-3 but not ERK-MAPK expression [3] .
Physalin A is a withanolide isolated from Physalis alkekengi var. franchetii. Physalin A induces apoptosis associated with up-regulation of caspase-3 and caspase-8 expression. Physalin A induces autophagy, found to antagonize apoptosis in HT1080 cells. Physalin A has the potential for the research of cancer disease .
Cinchonine is a natural compound present in Cinchona bark with antimalarial, antitumor, anti-inflammatory, anti platelet-aggregation and anti-obesity properties. Cinchonine inhibits cells proliferation and autophagy and induces apoptosis through activation of Caspase-3. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells .
Crenulatin is a gallotannin that can be isolated from Rhodiola rosea. Crenulatin can be used as a biomarker to identify potentially adulterated R. rosea products. Crenulatin has dual- direction effects on apoptosis of cerebral microvascular endothelial cells, via regulating Fas/Bcl-2 expression and caspase-3 activity [3].
Cannflavin A can be isolated from Cannabis sativa L. Cannflavin A has anti-cancer, neuroprotective and anti-inflammatory activity. Cannflavin A inhibits Aβ1-42 aggregation. Cannflavin A also inhibits kynurenine-3-monooxygenase (KMO). Cannflavin A activates apoptosis via caspase-3 cleavage [3] .
Koumine is an alkaloid separated from Gelsemium elegans, shows potent anti-tumor activity. Koumine up-regulates the Bax/Bcl-2 ratio and caspase-3 expression in human breast cancer cells . Koumine has anxiolytic, antistress, antipsoriatic, and analgesic activities [3], protects against the development of arthritis in Rheumatoid arthritis (RA) animal models .
Pipernonaline is a piperine derivative with antiprostate cancer activity. Pipernonaline inhibits the proliferation of androgen-dependent/independent LNCaP/PC-3 prostate cells. Pipernonaline activates caspase-3 and promotes procaspase-3/PARP cleavage. Pipernonaline also mediates reactive oxygen species (ROS) production, increased intracellular Ca(2+), and mitochondrial membrane depolarization .
2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound of Cinnamomum cassia, with antitumor activity [3]. 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 [3].
Ganoderic acid T1 is a deacetylated derivative of Ganoderic acid T. Ganoderic acid T1 attenuates antioxidant defense system and induces apoptosis of cancer cells. Ganoderic acid T1 decreases mitochondrial membrane potential and activates caspase-9 and caspase-3, to trigger apoptosis. Ganoderic acid T1 also increases the generation of intracellular ROS to produce pro-oxidant activities and cytotoxicity .
Asperosaponin VI, A saponin component from Dipsacus asper, induces osteoblast differentiation through BMP‐2/p38 and ERK1/2 pathway . Asperosaponin Ⅵ inhibits apoptosis in hypoxia-induced cardiomyocyte by increasing the Bcl-2/Bax ratio and decreasing active caspase-3 expression, as well as enhancing of p-Akt and p-CREB .
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 .
Dihydrocapsaicin, a capsaicin, is a potent and selective TRPV1 (transient receptor potential vanilloid channel 1) agonist. Dihydrocapsaicin reduces AIF, Bax, and Caspase-3 expressions, and increased Bcl-2, Bcl-xL and p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection following ischemic stroke via PI3K/Akt regulation in rat [3].
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 .
Tenuifolin is effective and has a protective action. Tenuifolin inhibits β-secretase decreases Aβ protein secretion, suppresses Aβ25-35 secretion, and subsequently caspase-3 and caspase-9 become active. Tenuifolin's ability to lower AChE activity, increase at the same time, increase the ability of the upper glands, and improve the ability to read and remember. Research on tenuifolin's potential for use in urinary disease (AD).
5,7,4’-Trimethoxyflavone can be isolated from the medicinal plant Kaempferia parviflora (KP). 5,7,4’-Trimethoxyflavone is a CFTR activator and EC50 is 64 μM. 5,7,4’-Trimethoxyflavone induces apoptosis, increases proteolytic activation of caspase-3, and degradation of ADP-ribose polymerase (PARP) protein. 5,7,4’-Trimethoxyflavone has antitumor activity. 5,7,4’-Trimethoxyflavone can be used to prevent skin aging and oxidative stress [3].
Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
Juncuenin D induces caspase-3-mediated cytotoxicity in HT22 cells. Juncuenin D also has anti-bacterial activity against MRSA strains. Juncuenin D can be isolated from J. effusus .
Citronellol ((±)-Citronellol) is a monoterpene Pelargonium graveolens. Citronellol ((±)-Citronellol) induces necroptosis of cancer cell via up-regulating TNF-α, RIP1/RIP3 activities, down-regulating caspase-3/caspase-8 activities and increasing ROS (reactive oxygen species) accumulation .
Aristololactam I (AL-I), is the main metabolite of aristolochic acid I (AA-I), participates in the processes that lead to renal damage.
Aristololactam I (AL-I) directly injures renal proximal tubule cells, the cytotoxic potency of AL-I is higher than that of AA-I and that the cytotoxic effects of these molecules are mediated through the induction of apoptosis in a caspase-3-dependent pathway .
Citronellol (Standard) is the analytical standard of Citronellol. This product is intended for research and analytical applications. Citronellol ((±)-Citronellol) is a monoterpene Pelargonium graveolens. Citronellol ((±)-Citronellol) induces necroptosis of cancer cell via up-regulating TNF-α, RIP1/RIP3 activities, down-regulating caspase-3/caspase-8 activities and increasing ROS (reactive oxygen species) accumulation .
Malformin A1, a cyclic pentapeptide isolated from Aspergillus niger, possess a range of bioactive properties including antibacterial activity. Malformin A1 shows potent cytotoxic activities on human colorectal cancer cells. Malformin A1 induces apoptosis by activating PARP, caspase 3, -7, and -9 .
Senkyunolide I, isolated from Ligusticum chuanxiong Hort, is an anti-migraine compound. Senkyunolide I protects rat brain against focal cerebral ischemia-reperfusion injury by up-regulating p-Erk1/2, Nrf2/HO-1 and inhibiting caspase 3 .
Procyanidin C1 (PCC1), a natural polyphenol with oral activity, causes DNA damage, cell cycle arrest and induces apoptosis. Procyanidin C1 decreases the level of Bcl-2, but enhances BAX, caspase 3 and 9 expression in cancer cells. Procyanidin C1 shows senotherapeutic activity and increases lifespan in mice .
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 [3]. Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection .
Caspase-3/CASP3 protein is a thiol protease critical in apoptosis and is activated by initiating caspases (CASP8, CASP9 and/or CASP10). It catalyzes the cleavage of multiple proteins in sympathetic neurons, including PARP1, SREBP, caspase-6, -7 and -9, huntingtin, and RET. Caspase-3/CASP3 Protein, Human is the recombinant human-derived Caspase-3/CASP3 protein, expressed by E. coli , with tag free. The total length of Caspase-3/CASP3 Protein, Human is 248 a.a., .
Caspase-3/CASP3 protein is a thiol protease critical in apoptosis and is activated by initiating caspases (CASP8, CASP9 and/or CASP10). It catalyzes the cleavage of multiple proteins in sympathetic neurons, including PARP1, SREBP, caspase-6, -7 and -9, huntingtin, and RET. Caspase-3/CASP3 Protein, Human (His, Strep) is the recombinant human-derived Caspase-3/CASP3 protein, expressed by E. coli , with N-Strep, N-6*His labeled tag. The total length of Caspase-3/CASP3 Protein, Human (His, Strep) is 277 a.a., .
Tauroursodeoxycholate-d4 (sodium) is the deuterium labeled Tauroursodeoxycholate sodium. Tauroursodeoxycholate (Tauroursodeoxycholic acid; TUDCA) sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Tauroursodeoxycholate-d5 is the deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Tauroursodeoxycholate-d4 is deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Tauroursodeoxycholate-d4-1 is the deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Cystamine-d8 (dihydrochloride) is the deuterium labeled Cystamine (dihydrochloride)[1]. Cystamine (dihydrochloride) is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC50 value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD)[2][3][4].
Dihydrocapsaicin-d3is the deuterium labeledDihydrocapsaicin(HY-N0361) . Dihydrocapsaicin, a capsaicin, is a potent and selective TRPV1 (transient receptor potential vanilloid channel 1) agonist. Dihydrocapsaicin reduces AIF, Bax, and Caspase-3 expressions, and increased Bcl-2, Bcl-xL and p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection following ischemic stroke via PI3K/Akt regulation in rat [3] .
Lacidipine- 13C8 is the deuterium labeled Lacidipine[1]. Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI)[2][3].
Lacidipine- 13C4 is 13C labeled Lacidipine (HY-B0347). Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
Cleaved-Caspase 3 p12 Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 32 kDa, targeting to Cleaved-Caspase 3 p12. It can be used for WB,ICC/IF assays with tag free, in the background of Human, Mouse, Rat.
Caspase-3 Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 32 kDa, targeting to Caspase-3. It can be used for WB,ICC/IF,IHC-P,IP,FC assays with tag free, in the background of Human.
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