LCS-1 is a superoxide dismutase 1 (SOD1) inhibitor. LCS-1 inhibits SOD1 activity with an IC50 value of 1.07 μM. LCS-1 induces the early- and late-stage apoptosis of multiple myeloma (MM.1S) cells[1][2][3].
TL4-12 is a selective MAP4K2/GCK inhibitor, dose-dependently downregulates IKZF1 and BCL-6 and leads to MM cell proliferation inhibition (IC50=37 nM) accompanied by induction of apoptosis. TL4-12 can be used to overcome immunomodulatory drug resistance in multiple myeloma (MM)[1].
Ginsenoside F2, a metabolite from Ginsenoside Rb1, induces apoptosis accompanied by protective autophagy in breast cancer stem cells[1].
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].
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].
Butylated hydroxytoluene is an antioxidant widely used in foods and in food-related products[1]. Butylated hydroxytoluene is a Ferroptosis inhibitor[2].
MT 63-78 is a specific and potent direct AMPK activator with an EC50 of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis. MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects[1].
Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC50 values of 61 and 108 μM[1]. Euscaphic acid induces apoptosis[2].
STAT3-IN-11 (7a) is a selective STAT3 inhibitor that inhibits the phosphorylation of STAT3 at site pTyr705. STAT3-IN-11 inhibits the phosphorylation of downstream genes (Survivin and Mcl-1) without affecting its upstream tyrosine kinases (Src and JAK2) levels and p-STAT1 expression. STAT3-IN-11 can induce cancer cell apoptosis, which is potential for the discovery of effective STAT3 inhibitors and antitumor agents against cancers[1].
Neihulizumab (ALTB-168) is an immune checkpoint agonistic antibody that binds to human CD162 (PSGL-1), leading to downregulation of activated T-cells. Neihulizumab can be uesd for steroid-refractory acute graft-versus-host-disease (SR-aGVHD), psoriasis, psoriatic arthritis and ulcerative colitis research[1].
Inauhzin is a dual SirT1/IMPDH2 inhibitor, and acts as an activator p53, used in the research of cancer.
Picrasidine I is an anti-inflammatory and anti-osteoclastogenic dimeric alkaloid that can be isolated from Picrasma quassioides. Picrasidine I inducs cell cycle arrest, and triggers cell Apoptosis by downregulats ERK and Akt pathways. Picrasidine I inhibits the activation of MAPKs, NF-κB and ROS generation, and suppresses the expression of c-Fos and NFATc1[1][2].
XMU-MP-3 is a potent non-covalent BTK inhibitor with IC50s of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation in the presence of 10 μM ATP, respectively. XMU-MP-3 also induces apoptosis[1].
Laquinimod (ABR-215062) sodium, an orally available carboxamide derivative, is a potent immunomodulator which prevents neurodegeneration and inflammation in the central nervous system. Laquinimod sodium reduces astrocytic NF-κB activation to protect from Cuprizone-induced demyelination. Laquinimod sodium has the potential for relapsing remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases research[1][2][3][4].
Novel antitumor agent, inducing PKR-mediated apoptosis and synergizing with IFN
Temozolomide-d3 (NSC 362856-d3) is the deuterium labeled Temozolomide. Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects[1][2].
Anti-CSCs agent-1 is a potent anti-CSCs agent. Anti-CSCs agent-1 inhibits cell growth and cell migration. Anti-CSCs agent-1 induces apoptosis. Anti-CSCs agent-1 inhibits the viability of CSCs. Anti-CSCs agent-1 enhances the production of ROS in CSCs. Anti-CSCs agent-1 shows antitumor activity[1].
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].
Antitumor agent-59 (Compound 13b) is a potent antitumor agent. Antitumor agent-59 effectively inhibits the proliferation and migration of HCT116 cells. Antitumor agent-59 induces HCT116 cell apoptosis and arrests the cell cycle at the G2/M phase[1].
ZINC02092166 is a novel potent, and selective small-molecule inhibitor for the β-catenin/Tcf4 protein-protein interaction with Ki of 1.7 and 7.0 uM in AlphaScreen and FP assay (wild-type β-catenin), respectively; remain affinity for muant catenin V511S, V511S/I569S and R469A with Ki of 20-50 uM; exhibits dual selectivity for β-catenin/Tcf over β-catenin/cadherin and β-catenin/APC PPIs.
LBW242, a 3-mer and Smac mimetic, is a potent and orally active proapoptotic IAP inhibitor. LBW242 shows effects on mutant FLT3-expressing cells. LBW242 has activity against multiple myeloma[1].
AV123 (compound 12) is a non-cytotoxic RIPK1 inhibitor (IC50=12.12 µM). AV123 blocks the TNF-α-induced necroptotic (EC50=1.7 μM) but not the apoptotic cell death. AV123 can be used in the study of necrotic chronic conditions such as ischemia-reperfusion injury of the brain, heart and kidney, inflammatory diseases, neurodegenerative diseases and infectious diseases[1].
Polyporenic acid C is a lanostane-type triterpenoid isolated from P. cocos. Polyporenic acid C induces cell apoptosis through the death receptor-mediated apoptotic pathway without the involvement of the mitochondria. Polyporenic acid C is promising agent for lung cancer therapy[1].
Oleic acid-13C18 (9-cis-Octadecenoic acid-13C18) is the 13C labeled Oleic acid. Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid[1]. Oleic acid is a Na+/K+ ATPase activator[2].
Z-LEHD-FMK TFA is an irreversible caspase-9 inhibitor, protects against lethal reperfusion injury and attenuate apoptosis[1][2].
A non-immunosuppressive FTY720 analogue, PKCδ activator with higher antiproliferative potency with IC50 of 2.4, 2.4, and 3.5 uM in Huh7, Hep3B, and PLC5 cells, respectively; exhibited higher in vitro antiproliferative efficacy relative to FTY720 against HCC cells without cytotoxicity in normal hepatocytes, although devoid of S1P1 receptor activity; induces caspase-dependent apoptosis through ROS-dependent PKCδ activation in HCC tumor cells.
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].
Mcl1-IN-3 is an inhibitor of Mcl1 extracted from patent WO2015153959A2, compound example 57; has an IC50 and Ki of 0.67 and 0.13 μM, respectively.
Hypaconitine, an active and highly toxic constituent derived from Aconitum species, is widely used to treat rheumatism. IC50 value:Target:In vitro: The present study investigated the metabolism of hypaconitine in vitro using male human liver microsomes. The primary contributors toward HA metabolism were CYP3A4 and 3A5, with secondary contributions by CYP2C19, 2D6 and CYP2E1 [1].In vivo:
PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor with IC50 of 2 nM. PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis in hepatocellular carcinoma models[1].