MK-2206 is a potent and selective allosteric inhibitor of Akt that enhances antitumor efficacy of several standard chemotherapeutic agents.
Inhibits USP7 and the closely related USP47. Inhibits neuroblastoma growth via induction of p53-mediated apoptosis
Highly selective, potent, cell permeable inhibitor of Aurora A with off-target binding at GABAA. Induces apoptosis and autophagy in breast cancer and melanoma cells via suppression of activation of the p38 MAPK pathway
Potent inhibitor of the BET family of bromodomains with no activity at BAZ2B, SP140, ATAD2, CREBBO and PCAF. Inhibition of BET bromodomains results in downregulation of Myc transcription.
Potent and selective TRPC5 blocker with therapeutic benefit in a rat model of hypertensive proteineuric kidney disease. Active in vivo
LY2603618 inhibits Chk1, an important regulator of cellular response to DNA damage. It has been shown to cause dramtice suppression of cell growth in MCF-7 and MDA-MB-31 breast cancer cells
Potent inhibitor of Brd4 (IC50 = 100 nM). BI 2536 has been shown to suppress cMyc-expression in MM.1S multiple myeloma cells.
Protects cells from ferroptosis caused by iron catalyzed formation of free radicals from lipid peroxides. Treatment of several treatment-resistant cancer cell lines exhibiting a high mesenchymal state resulted in selective induction of ferroptosis
RS-1 has been used to exploit the RAD51 overexpression in cancerous cells by inducing lethality via genotoxic RAD51 protein complexes. RS-1 has also been found to a potent enhancer of CRISPR- and TALEN- based gene editing.
UNC0379 is a selective inhibitor of the lysine methyltransferase SETD8. Treatment of SY5Y and NGP neuroblastoma cell lines lead to activation of p53 and decreased tumor growth in an ex-vivo tumorigenicity assay.
An important tool for probing the involvement of AhR in the toxicity of various environmental toxins such as TCDD and other dioxins.
Significantly decreased IL-1β and IL-18 levels in LPS-stimulated human blood-derived macrophages as well as IL-1β release and caspase 1 activity in human blood neutrophils with no effect on TNFα levels.
Inhibits the cystine-glutamate antiporter, system Xc- leading to activation of an ER stress response. Inhibition of system Xc- leads to cysteine starvation, glutathione depletion and induction of ferroptosis.
Sensitizes cancer cells to carious chemotherapeutic agents
Prevents necroptosis, virus-induced necrosis and TLR3-induced necrosis.
NAcM-OPT is a potent and selective NEDD8 ligation inhibitor, IC50=80 nM (in vitro).
SBI-0206965 (1884220-36-3) is a potent and selective inhibitor of the autophagy kinase ULK-1, IC50=108 and 711 nM for ULK1 and 2 respectively.
Displays selective cytotoxic effects on human oral cancer cell lines. Inhibits hepatocellular carcinoma cell growth via modulation of the Wnt/β-catenin pathway.
KA can selectively kill high-glycolytic cancer cells via glucose dependent ATP depletion and been used in a predictive model for selective targeting of the Warburg effect, the most prominent hallmark of cancer cell metabolism.
SMED-1 displays strong synergism at 10 μM plus 1 mM Dex and exhibits little activity alone (IC50>20 μM).
A potent and selective fatty acid synthase (FASN) inhibitor acting via interfering with cofactor binding.
Dienamide A2 (24738-51-0) is an analog of the natural amides occurring in Echinacea which represent a new class of cannabinomimetic compounds.
17-AHA-geldanamycin is a semi-synthetic analog of geldanamycin containing a linker bearing a free NH2 functional group for conjugation.
C-DIM 12 (178946-89-9) activates the orphan nuclear receptor Nurr1 and inhibits bladder cancer growth.
Tropodithietic acid (750590-18-2) displays potent broad-spectrum anticancer activity.
C22 Ceramide is a long-chain ceramide containing behenic acid. Mitochondrial-to-cytosolic stress response (MCSR) is a recently identified stress response which can be induced by increased synthesis of fatty acids.
N-Acetyl Puromycin (22852-13-7) down regulates SnoN and Ski protein expression. Induces TGF-β signaling, independently of MAPK activation. Does not bind ribosomes or block protein synthesis.
Exo2 (304684-77-3) disrupts the Golgi apparatus and stimulates Golgi-ER fusion in mammalian cells.1 May be used to completely ablate the Golgi apparatus.
TRO19622 (220033-87-0) is a neuroregenerative and neuroprotective agent acting at components of the mitochondrial permeability transition pore (MPTP).
Ilicicolin H (12689-26-8) is a potent inhibitor of the mitochondrial cytochrome bc1 reductase.1 Displays potent and broad spectrum antifungal activity.
Leu-Leu-OMe (16689-14-8) is a lysosomal damaging agent (lysosomotropic). It is condensed into a membranolytic polymer via the transpeptidase action of cathepsin C within lysosomes.
P0108 (893449-38-2) is a potent inhibitor of phosphatase of regenerating liver-3 (PRL-3), IC50=0.9 μM.1 Reduces the invasive properties of mouse melanoma B16F10 cells in a cellular model.
17-PAAG is a semi-synthetic analog of geldanamycin which possesses an acetylenic side chain for coupling to other probes, fluorophores and bioactive molecules such as steroids via click chemistry.