iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1) (AIFM2) with an EC50 of 103 nM. iFSP1 selectively induces ferroptosis in GPX4-knockout cells which overexpressed FSP1. iFSP1 is able to sensitize a variety of human cancer cell lines to the ferroptosis inducer, such as (1S,3R)-RSL3 (HY-100218A)[1].
BTZO-1 binds to Macrophage migration inhibitory factor (MIF) with a Kd value of 68.6 nM, and its binding requires the N-terminal Pro1. BTZO-1 can activate antioxidant response element (ARE)-mediated gene expression and suppress oxidative stress-induced cardiomyocyte apoptosis in vitro[1].
MMP-9-IN-3 is a MMP-9 inhibitor (IC50: 5.56 nM) that forms hydrogen bond with MMP-9. MMP-9-IN-3 also inhibits AKT activity (IC50: 2.11 nM). MMP-9-IN-3 shows cell cytotoxicity and induces cell apoptosis. MMP-9-IN-3 can be used in the research of cancers[1].
TIC10 is a potent, orally active, and stable TRAIL inducer, also inhibits Akt and ERK activity.
Gallium maltolate (GAM) is an apoptosis inducer with anti-cancer and anti-inflammatory activity. Gallium maltolate (GAM)-induced apoptosis involves the oxidative stress and p53 pathways[1][2].
W146 TFA is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM.
S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells[1].
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.
BTSA1 is a potent, high affinity and orally active BAX activator with an IC50 of 250 nM and an EC50 of 144 nM. BTSA1 binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis[1].
Flavokawain C is a natural chalcone found in Kava root. Flavokawain C exerts cytotoxicity against human cancer cell lines, with an IC50 of 12.75 μM for HCT 116 cells[1].
Drozitumab (PRO 95780) is a human agonistic monoclonal antibody which binds the death receptor DR5. Drozitumab has potent antitumor activity against rhabdomyosarcoma[1][2][3].
FX1 is a potent and specific BCL6 inhibitor, with an IC50 of around 35 μM.
Angiogenesis inhibitor 2 (compound 72) is a potent angiogenesis inhibitor. Angiogenesis inhibitor 2 inhibits the proliferation of HUVEC and HCT-15 cells, with IC50 values of 1.93 and 0.21 μM. Angiogenesis inhibitor 2 induces the apoptosis of HUVEC and HCT-15 cells. Angiogenesis inhibitor 2 shows anticancer activity, and suppresses the invasion of cancer cells. Angiogenesis inhibitor 2 inhibits the angiogenesis in zebrafish embryos[1].
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].
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.
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[1]
αβ-Tubulin-IN-1 is a potent and orally active αβ-Tubulin inhibitor. αβ-Tubulin-IN-1 induces cell cycle arrest at G2/M and efficient apoptosis. αβ-Tubulin-IN-1 inhibits tumor cell migration and Metastasis. αβ-Tubulin-IN-1 shows significant antitumor efficacy in a dose dependent manner[1].
L6H21, a derivative of chalcone, is an orally active and potent MD-2 (myeloid differentiation factor 2) inhibitor. L6H21 inhibits TLR4-NF-κB signaling and NLRP3 inflammasome activation in macrophages. L6H21 inhibits EtOH + LPS-induced apoptosis and mitochondrial damage in RAW264.7 cells. L6H21 effectively inhibits EtOH + LPS-induced hepatic fat accumulation and liver injury. L6H21 shows neuroprotective effect in a model of prediabetes[1][2].
Benzyl isothiocyanate is a member of natural isothiocyanates with antimicrobial activity[1][2]. Benzyl isothiocyanate potent inhibits cell mobility, migration and invasion nature and matrix metalloproteinase-2 (MMP-2) activity of murine melanoma cells[2].
MA242 free base is a specific dual inhibitor of MDM2 and NFAT1. MA242 free base directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 free base induces apoptosis in pancreatic cancer cell lines regardless of p53 status[1].
Helichrysetin, isolated from the flowers of Helichrysum odoratissimum, is an ID2 (inhibitor of DNA binding 2) inhibitor, and suppresses DCIS (ductal carcinoma in situ) formation. Helichrysetin possess strong inhibitory effects on cell growth and is capable of inducing apoptosis in A549 cells[1][2].
NSC 146109 hydrochloride is a small-molecule p53 activator that target MDMX and could be of value in treating breast cancer.NSC 146109 hydrochloride is a pseudourea derivative, promotes breast cancer cells to undergo apoptosis through activating p53 and inducing expression of proapoptotic genes[1].
PI3K-IN-34 (Compound 6g) is a highly selective PI3K inhibitor with IC50 values of 11.73, 6.09 and 11.18 μM for PI3K-α、PI3K-β and PI3K-δ , respectively. PI3K-IN-34 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-34 can be used in leukemia research[1].
Tomuzotuximab (Anti-Human EGFR Recombinant Antibody) is a fully human glycoengineered IgG1 monoclonal antibody against EGFR. Tomuzotuximab has anticancer effects[1].
Pancratistatin is an isoquinoline alkaloid that can be isolated from Hymenocallis littoralis. Pancratistatin induces apoptosis of human melanoma cells. Pancratistatin can be used for the research of neuroblastoma, leukemia and breast cancer[1].
7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) is a flavonoid from the herb Lippia nodiflora L. (Verbenaceae) which has been documented to exhibit anti-inflammatory, antipyretic, antitussive, antidiabetic, anticancer, and antimelanogenesis properties. 7,3',4'-Tri-O-methylluteolin obviously reduces the prodn of pro-inflammatory cytokines, such as TNF-α, IL-6, and IL-1β in a concentration-dependent manner. 7,3',4'-Tri-O-methylluteolin significantly induces reduction in the mRNA expressions of inducible nitric oxide synthase and cyclooxygenase-2, representing that inhibition occurs at the transcriptional level[1].
α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC50 of 9 μM. α-NETA is a potent ALDH1A1 (IC50=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC50=84 µM) and acetylcholinesterase (AChE; IC50=300 µM). α-NETA has anti-cancer activity[1][2].
Nutlin 3a is an active enantiomer of Nutlin-3, acts as a murine double minute (MDM2) antagonist that inhibits MDM2-p53 interactions and stabilizes the p53 protein, and thereby induces cell cycle arrest and apoptosis.
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[1].