SC75741 is a broad and efficient NF-κB inhibitor with an IC50 of 200 nM for p65[1]. SC75741 blocks influenza viruses (IV) replication in non-toxic concentrations. SC75741 impairs DNA binding of the NF-κB subunit p65, resulting in reduced expression of cytokines, chemokines, and pro-apoptotic factors. SC75741 subsequently inhibits caspase activation and blocks caspase-mediated nuclear export of viral ribonucleoproteins[2].
TC11 is a MCL1 degradator and Caspase-9 and CDK1 activator. TC11 structurally relates to immunomodulatory drugs as phenylphthalimide derivative. TC11 induces apoptotic death caused by degradation of MCL1 during prolonged mitotic arrest[1][2].
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[1].
Ac-AAVALLPAVLLALLAP-YVAD-CHO is a cell-permeable caspase-1 inhibitor that has antitumor activity[1].
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[1].
Aspirin (Acetylsalicylic Acid) lithium is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin lithium induces apoptosis. Aspirin lithium inhibits the activation of NF-κB. Aspirin lithium also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis[1][2][3][4][5][6].
Boc-Ala-Ala-Asp-pNA is a chromogenic substrate of granzyme B. Boc-Ala-Ala-Asp-pNA can be used to test functional activity of granzyme B[1].
Coenzyme Q0 (CoQ0) is a potent, oral active ubiquinone compound can be derived from Antrodia cinnamomea. Coenzyme Q0 induces apoptosis and autophagy, suppresses of HER-2/AKT/mTOR signaling to potentiate the apoptosis and autophagy mechanisms. Coenzyme Q0 regulates NFκB/AP-1 activation and enhances Nrf2 stabilization in attenuation of inflammation and redox imbalance. Coenzyme Q0 has anti-angiogenic activity through downregulation of MMP-9/NF-κB and upregulation of HO-1 signaling[1][2][3].
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].
Ac-Trp-Glu-His-Asp-Aldehyde is a potent and selective caspase-1 inhibitor with a Ki value of 56 pM[1][2].
Ac-VETD-AMC is a synthetic peptide substrate for caspase 8. Ac-VETD-AMC also has potential to assess functional activity of recombinant phytaspase[1].
AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor (IC50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation[1].
Ac-Trp-Glu-His-Asp-AMC (Ac-Trp-Glu-His-Asp-AMC) is a potent fluorogenic substrate of caspase-1[1].
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[1]. Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation[2].
Ac-YVAD-cmk (Caspase-1 Inhibitor II) is a selective caspase-1 (IL-1beta converting enzyme, ICE)) inhibitor with neuroprotective and anti-inflammatory effects. Ac-YVAD-cmk effectively suppresses the expression of IL-1β and IL-18. Ac-YVAD-cmk inhibits pyroptosis in many diseases[1][2].
Tripeptide-32isa bioactive peptide with anti-aging effect and has been reported used as a cosmetic ingredient[1].
Nenocorilant (Relacorilant) is a potent, orally activity glucocorticoid receptor (GR) antagonist with Ki value of 0.15 nM. Nenocorilant has pro-apoptotic effects and improves potency combined with cytotoxic agent. Nenocorilant can be used for cancer research[1][2][3].
Euptox A (9-Oxo-10, 11-dehydroageraphorone), a cadenine sesquiterpene, is the main toxin that can be isolated from Eupatorium adenophorum. Euptox A induces apoptosis by improving the gene expression level of apoptotic proteases such as caspase-10 in HeLa cells[1].
PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4 degrader with IC50 value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research[1].
Taurodeoxychloic Acid (sodium hydrate) prevents apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxychloic Acid (sodium hydrate) is investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis[1].
Crustecdysone (20-Hydroxyecdysone) is a naturally occurring ecdysteroid hormone isolated from Cyanotis arachnoides C.B.Clarke which controls the ecdysis (moulting) and metamorphosis of arthropods, it inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP[1].Crustecdysone exhibits regulatory or protective roles in the cardiovascular system[2].
Arnicolide D is a sesquiterpene lactone isolated from Centipeda minima. Arnicolide D modulates the cell cycle, activates the caspase signaling pathway and inhibits the PI3K/AKT/mTOR and STAT3 signaling pathways. Arnicolide D inhibits Nasopharyngeal carcinoma (NPC) cell viability in a concentration- and time-dependent manner[1].
M867 is a selective and reversible inhibitor of caspase-3 with an IC50 of 1.4 nM and Ki of 0.7 nM. M867 has anti apoptotic activity[1].
PHA-690509 is an anti-ZikV compound that inhibits ZikV replication. PHA-690509 is also a CDK inhibitor, and inhibits caspase-3 activity[1][2].
Tauroursodeoxycholate 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.
Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor; inhibits apoptosis stimulated by TNF-α with an IC50 of 39 µM.
Tauroursodeoxycholate dihydrate (TUDCA dihydrate; UR 906 dihydrate; Taurolite 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[1][2].
Aviculin, a lignan glycoside, is a potent anticancer agent. Aviculin reduces metabolic activity on MCF-7 cells below 50%, with an IC50 of 75.47 μM. Aviculin induces breast cancer cell apoptosis through the intrinsic apoptosis pathway. Aviculin increases expression of initiator caspase-9, executioner caspase-7, and poly (ADP-ribose) polymerase (PARP). Aviculin shows an increase in the Bax/Bcl-2 ratio[1].
Euphornin is a anticaner agent, that can be isolated from E. helioscopia. Euphornin induces apoptosis via caspase-mediated pathways. Euphornin induces cell cycle arrest by increasing the level of the phospho-CDK1 (Tyr15) protein[1].
Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt[1]. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively[2].