Apoptosis Inducer

GSK2656157 is a selective and ATP-competitive inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) with an IC₅₀ of 0.9 nM.

L-Methionine is an L-isomer of orally active Methionine, an essential amino acid. Methionine is a strong liver antidote that acts as a liver protector. L-Methionine can inhibit cell proliferation and induce cell apoptosis. L-Methionine has antitumor and antioxidant activity.

Buparlisib (BKM120; NVP-BKM120) is a pan-class I PI3K inhibitor, with blood-brain barrier permeability. Buparlisib has IC₅₀s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.

Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) is an orally active gallic tannin compound and an inducer of apoptosis and autophagy. Pentagalloglucose induces cell apoptosis and autophagy through the GSK3β/β-catenin pathway. Pentagalloylglucose inhibits UBE2T-mediated p53 ubiquitination, upregulates p53, downregulates RRM1/RRM2 in pancreatic cancer organoids. Pentagalloglucose has antioxidant, anti mutagenic, anti-inflammatory, anticonvulsant, cardioprotective, anti allergic, cholesterol lowering, and anti-tumor activities.

Prednisone (Adasone) is a corticosteroid agent with anti-inflammatory and immunosuppressive effects that can be used to study diseases related to systemic lupus erythematosus.

Iberdomide (CC-220) is an orally active and potent cereblon (CRBN) E3 ligase modulator (CELMoD) with an IC₅₀ of ~150 nM for cereblon-binding affinity. Iberdomide, a derivative of Thalidomide (HY-14658), has antitumor and immunostimulatory activities.

Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC₅₀ of 5.22 nM.

Eragidomide (CC-90009) is a GSPT1 Molecular Glue degrader. Eragidomide exhibits antiproliferative and pro-apoptotic (apoptosis) activities against acute myeloid leukemia cells. Eragidomide recruits the CRL4CRBN E3 ubiquitin ligase complex to selectively target GSPT1 for ubiquitination and proteasomal degradation. Eragidomide reduces leukemia cell engraftment and eliminates leukemia stem cells. Eragidomide promotes the activation of the GCN1/GCN2/ATF4 pathway and the integrated stress response pathway, inhibits global protein translation, promotes preferential translation of ATF4, and induces the accumulation of ATF4, CHOP and ATF3. The response to Eragidomide is regulated by the ILF2/ILF3 heterodimer complex, the mTOR signaling pathway and the integrated stress response. Eragidomide can be used in research related to acute myeloid leukemia and relapsed/refractory acute myeloid leukemia.

Mezigdomide (CC-92480), a cereblon E3 ubiquitin ligase modulating agent (CELMoD), acts as a molecular glue. Mezigdomide shows high affinity to cereblon, resulting in potent antimyeloma activity.

ODN 1826 sodium is a class B CpG ODN (oligodeoxynucleotide) and TLR9 agonist. ODN 1826 sodium induces NO and iNOS production and enhances Apoptosis. ODN 1826 sodium enhances immune surveillance. ODN 1826 sodium increases aortic atherosclerotic plaque size. ODN 1826 sodium has antitumor activity against lung cancer, glioma and melanoma.

FB23-2 is a potent and selective inhibitor of mRNA N⁶-methyladenosine (m⁶A) demethylase FTO, with an IC₅₀ of 2.6 μM. FB23-2 has anti-proliferation activity. FB23-2 can be used for the research of acute myeloid leukemia (AML).

DT2216 is a potent and selective BCL-XL (Bcl-2 family member) degrader based on PROTAC technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets.

AKT inhibitor VIII (AKTi-1/2) is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity with IC₅₀s of 58 nM, 210 nM, and 2119 nM, respectively.

Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC₅₀ of 1 nM.

R406 is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a K_i of 30 nM, potently inhibits Syk kinase activity in vitro with an IC₅₀ of 41 nM, measured at an ATP concentration corresponding to its K_m value. R406 reduces immune complex-mediated inflammation. R406 also inhibits Lyn (IC₅₀=63 nM) and Lck (IC₅₀=37 nM).

BCH (2-Amino-2-norbornanecarboxylic acid) is a selective and competitive inhibitor of large neutral amino acid transporter 1 (LAT1) significantly inhibit cellular uptake of amino acids and mTOR phosphorylation, which induces the suppression of cancer growth and apoptosis.

Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).

Tubastatin A is a potent and selective HDAC6 inhibitor with an IC₅₀ of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).

ARV-825 is a BET protein PROTAC degrader that recruits cereblon, and it targets BRD2, BRD3, and BRD4 for degradation via the ubiquitin-proteasome pathway. ARV-825 downregulates c-MYC, PLK1, MYCN, CDK4/6, JAK2, pSTAT3/5, PIM1, and Bcl-xL, upregulates p21 and p27, and modulates H3K27Ac-mediated transcription, the G2/M checkpoint, the Wnt/β-catenin pathway, and amino acid transport pathways. ARV-825 induces G1 phase cell cycle arrest, caspase 3/PARP-mediated apoptosis, DNA damage, and reactive oxygen species (ROS) production, reduces mitochondrial respiration, and simultaneously inhibits cell proliferation, clonogenic growth, and cell migration. ARV-825 is used in research on gastric cancer, leukemia, neuroblastoma, and cholangiocarcinoma.

Rosmarinic acid is a widespread phenolic ester compound in the plants. Rosmarinic acid inhibits MAO-A, MAO-B and COMT enzymes with IC₅₀s of 50.1, 184.6 and 26.7 μM, respectively.