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[1][2][3].
Pralnacasan (VX-740) is a potent, selective, non-peptide and orally active interleukin-1β converting enzyme (ICE, caspase 1) inhibitor with a Ki of 1.4 nM. Pralnacasan inhibits proinflammatory cytokines IL-18, IL-1β , and IFN-γ. Pralnacasan has the potential for osteoarthritis and rheumatoid arthritis treatment[1][2].
Z-LEHD-FMK TFA is an irreversible caspase-9 inhibitor, protects against lethal reperfusion injury and attenuate apoptosis[1][2].
Caspase-3-IN-1 (compound 11b) is a potent Caspase-3 inhibitor, with an IC50 of 14.5 nM[1].
Z-YVAD-pNA (Z-Tyr-Val-Ala-Asp-pNA) is a caspase-1 substrate[1].
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[1].
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[1].
PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis[1].
Ac-VAD-CHO (Ac-Val-Ala-Asp-CHO) is a pan-caspase inhibitor. Ac-VAD-CHO inhibits dissipation of MMP and cytochrome c release in hypoxia-exposed cells[1].
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[1][2].
Mca-YVADAP-Lys(Dnp)-OH is a fluorogenic substrate for caspase-1 and angiotensin-converting enzyme 2 (ACE2)[1].
Z-YVAD-CMK is a caspase-1 and caspase-3 inhibitor[1].
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.
QM31 (SVT016426, Apaf-1 inhibitor QM31) is a cytoprotective agent that inhibits the formation of the apoptosome (IC50=7.9 uM in vitro), the caspase activation complex composed by Apaf-1, cytochrome c, dATP and caspase-9; suppresses the Apaf-1-dependent intra-S-phase DNA damage checkpoint; QM31 can interfere with the two known functions of Apaf-1, namely apoptosome assembly/activation and intra-S-phase cell cycle arrest.
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[1][2][3].
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[1].
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[1].
Ac-Tyr-Val-Lys-Asp-aldehyde is a caspase-1 inhibitor, can be used for disease research including anemia-associated to chronic diseases, chemotherapy-induced anemia and Diamond-Blackfan anemia[1].
Belnacasan (VX-765) is an oral prodrug of VRT-043198, a potent and selective caspase-1 inhibitor with a Ki of 0.8 nM.
PETCM is an activator of caspase-3. PETCM can induces cell apoptosis and stimulate apoptosome formation in HeLa cell cytosols[1].
YVAD-CHO is an interleukin-1β converting enzyme (ICE, caspase 1) inhibitor that can partially delay motoneurone death in lesioned facial nerve mice[1].
Dehydrocorydaline (13-Methylpalmatine) is an alkaloid isolated from traditional Chinese herb Corydalis yanhusuo W.T. Wang. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP.
Ac-VDVAD-pNA is a caspase-2 substrate. Ac-VDVAD-pNA can be used to test the activity of caspase-2[1].
28-Deoxonimbolide is a nimbin (HY-N3187) type limonoid, that can be isolated from Azadirachta indica seed extracts. 28-Deoxonimbolide shows anticancer activity. 28-Deoxonimbolide induces apoptotic cell death in HL60 cells via both the mitochondrial- and the death receptor-mediated pathways[1].
Astin B is a orally active and potent cyclic pentapeptide, that can be isolated from Aster tataricus. Astin B has hepatotoxic effects in vitro and in vivo and that hepatic injury was primarily mediated by apoptosis in a mitochondria/caspase-dependent manner. Astin B induces autophagy in L-02 cells, increases LC3-II and decreases p62 expression[1].
6,8-Diprenylorobol, a prenylated isoflavone, is a nature product that could be isolated from the leaves of Cudrania tricuspidata. 6,8-Diprenylorobol antiproliferative effect and induces apoptosis through activation of p53 and generation of ROS[1][2].
Z-Ala-Ala-Asp-CMK (Z-AAD-CMK) is a selective granzyme B inhibitor[1].
Heptelidic acid (Koningic acid) is a sesquiterpene antibiotic[1]. Heptelidic acid inhibits Etoposide-induced apoptosis via downregulation of caspases[2]. Koningic acid (KA) is a specific GAPDH inhibitor with an IC50of 90 μM[3].
OT-82 is a potent, selective and orally active inhibitor of NAMPT. OT-82 is selectively toxic to cells of hematopoietic origin and induces cell death in a NAD+ dependent manner. OT-82 is a promising antineoplastic agent for the study of hematological malignancies[1].
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 p21WAF1 via a p53 independent manner[1][2].