6-Formylpterin is an inhibitor of Xanthine Oxidase. 6-Formylpterin induces intracellular ROS generation and apoptosis in HL-60 cells. 6-Formylpterin suppresses cell proliferation in PanC-1 cells[1].
Ginsenoside Rg6 is the component isolated from notoginseng. Ginsenoside Rg6 inhibits TNF-α-induced NF-κB transcriptional activity with an IC50 of 29.34±2.22 μM in HepG2 cells. Ginsenoside Rg6 also exhibits apoptosis-inducing effect.
Jaceosidin is a flavonoid isolated from Artemisia vestita, induces apoptosis in cancer cells, activates Bax and down-regulates Mcl-1 and c-FLIP expression[1]. Jaceosidin exhibits anti-cancer[2], anti-inflammatory activities, decreases leves of inflammatory markers, and suppresses COX-2 expression and NF-κB activation[3].
SRS16-86 is a potent inhibitor of ferroptosis[1]. SRS16-86 is more stable than more stable to metabolism and plasma than Ferrostatin-1 in vivo. SRS16-86 can be used for renal ischemia-reperfusion injury (IRI) and spinal cord injury (SCI) research[2][3].
EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAFV600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively[1].
VRT-043198, the drug metabolite of VX-765 (Belnacasan), is a potent, selective and blood-brain barrier permeable inhibitor of interleukin-converting enzyme/caspase-1 subfamily caspases. VRT-043198 exhibits Ki values of 0.8 nM and 0.6 nM for ICE/caspase-1 and caspase-4, respectively[1].
(+)-Medioresinol is a furofuran type lignan with antifungal, antibacterial and lesishmanicidal activities. (+)-Medioresinol leads to intracellular ROS accumulation and mitochondria-mediated apoptotic cell death in Candida albicans. (+)-Medioresinol can reduce the cardiovascular disease risk[1][2].
AT-406 is a potent and orally bioavailable Smac mimetic and an antagonist of IAPs, and it binds to XIAP, cIAP1, and cIAP2 proteins with Ki of 66.4, 1.9, and 5.1 nM, respectively.
Sanggenol L induces caspase-dependent and caspase-independent apoptosis in melanoma skin cancer cells[1]. Sanggenol L induces of apoptosis via suppression of PI3K/Akt/mTOR signaling and cell cycle arrest via activation of p53 in p
Boc-Asp(OME)-Fluoromethyl Ketone is a broad range caspase inhibitor that inhibits Fas-mediated phagocytosis and oxidative rupture inhibition, but does not affect the chemotactic activity of IL-8[1][2].
RIP1 kinase inhibitor 1 (compound 22) is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor (pKi=9.04)[1].
BU224 hydrochloride is a selective and high affinity imidazoline I2 receptor ligand, with a Ki of 2.1 nM. BU224 hydrochloride is sometimes used as an I2 receptor antagonist. BU224 hydrochloride exerts neuroprotective effects, with anti-inflammatory and anti-apoptotic properties. BU224 hydrochloride improves memory in 5XFAD mice, enlarging dendritic spines and reducing Aβ-induced changes in NMDARs. BU224 hydrochloride can be used for Alzheimer's disease research[1][2][3].
IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies[1].
Resistomycin, a pentacyclic polyketide antibiotic, possesses anticancer activity and induces apoptosis[1][2][3][4].
1-Decarboxy-3-oxo-ceanothic acid is an anticancer agent. 1-Decarboxy-3-oxo-ceanothic acid inhibits DNA synthesis. 1-Decarboxy-3-oxo-ceanothic acid induces Apoptosis[1].
Xerophilusin B, an anticancer agent isolated from Isodon xerophilus, exhibits antiproliferative effects on esophageal squamous cell carcinoma (ESCC) cell lines, induces G2/M cell cycle arrest, and mediates apoptosis[1].
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[1].
Z-LEHD-FMK is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK exhibits the neuroprotective effect in a rat model of spinal cord trauma[1][2][3].
MG-115 is a potent and reversible proteasome inhibitor, with Kis of 21 nM and 35 nM for 20S and 26S proteasome, respectively. MG-115 specifically inhibit the chymotrypsin-like activity of the proteasome, induces p53-dependent apoptosis[1][2][3].
Apoptotic agent-1 (Compound 8a) is an apoptotic agent with high antiproliferative activity against cancer cells and low cytotoxic effect. Apoptotic agent-1 induces over-expression of Fas receptor and Cyto C genes[1].
Tripeptide-32isa bioactive peptide with anti-aging effect and has been reported used as a cosmetic ingredient[1].
Costunolide, a sesquiterpene lactone, exhibits anti-inflammatory and anti-oxidant properties and mediates apoptosis.IC50 Value: 6.2 - 9.8 ug/mL(sarcoma cells viability)[3]Target: Apoptosis inducerin vitro: Costunolide significantly inhibited RANKL-induced BMM differentiation into osteoclasts in a dose-dependent manner without affecting cytotoxicity. Costunolide did not regulate the early signaling pathways of RANKL, including the mitogen-activated protein kinase and NF-κB pathways. However, costunolide suppressed nuclear factor of activated T-cells, cytoplasmic 1 (NFATc1) expression via inhibition of c-Fos transcriptional activity without affecting RANKL-induced c-Fos expression. The inhibitory effects ofcostunolide were rescued by overexpression of constitutively active (CA)-NFATc1 [1]. Exposure of T24 cells to costunolide was also associated with increased expression of Bax, down-regulation of Bcl-2, survivin and significant activation of caspase-3, and its downstream target PARP [2]. Both costunolide and dehydrocostus lactone inhibited cell viability dose- and time-dependently. IC50 values ranged from 6.2 ug/mL to 9.8 ug/mL. Cells treated with costunolide showed no changes in cell cycle, little in caspase 3/7 activity, and low levels of cleaved caspase-3 after 24 and 48 h [3].in vivo: Neither costunolide nor alpha-MGBL affected the blood-ethanol elevation in pylorus-ligated rats or that induced by intraperitoneal and intraduodenal ethanol administration [4]. Costunolide and alpha-MGBL suppressed gastric emptying in rats given 20% ethanol and 1% sodium carboxymethyl cellulose.Clinical trial:
Tubulysin B is a highly cytotoxic peptide and potent microtubule destabilizing agents isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin B has IC50 values in the picomolar range against many cancer cell lines, including those with multidrug resistant properties[1].Tubulysin B is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[2].
MPT0E028 is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively[1]. MPT0E028 reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. MPT0E028 has good anticancer activity[2].
ABT-737 is a selective and BH3 mimetic Bcl-xL, Bcl-2 and Bcl-w inhibitor with EC50s of 78.7 nM, 30.3 nM and 197.8 nM, respectively.
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].
Sanguinarine (Sanguinarin) gluconate, a benzophenanthridine alkaloid, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB[1].
Pyridoclax is a potential Mcl-1 inhibitor.
Isoliensinine is a bisbenzylisoquinoline alkaloid extracted from the seed embryo of Nelumbo nucifera, with anti-oxidant and anti-inflammatory and anti-cancer activities. Isoliensinine induces apoptosis in triple-negative human breast cancer cells[1][2].
Apoptosis inducer 8 (Compound 7c) is a galectin-1 (gal-1) mediated apoptosis-inducing agent against global major leading lung cancer burden. Apoptosis inducer 8 significantly reduced the gal-1 protein level. Apoptosis inducer 8 is also a PET imaging agent[1].