NSC-66811

MLN-4924

产品介绍 Containing the active ingredient of MLN4924 which acts as a substrate-assisted inhibitor of the NEDD8-activating enzyme (NAE). NAE activates NEDD8 (Neural precursor cell expressed, developmentally down-regulated 8) for conjugation to a variety of ubiquitin E3 ligases. NAE inhibitor binds to and inhibits NAE, which may result in the inhibition of tumor cell proliferation and survival. This cell permeable compound selectively inhibits NAE activity and results in inhibition of the NEDD8 pathway. Treatment of cells with MLN4924 results in inhibition of the NEDD8 pathway, making MLN4924 a new approach to targeting the UPS for the treatment of cancer.

MDBN

产品介绍 An irreversible inhibitor of p97/vasolin (IC50=1.7 µM) identified in a cell-based protein degradation assay. Cell permeable.

Lactacystin

产品介绍 Lactacystin is a cell-permeable, potent and selective proteasome inhibitor that binds irreversibly to the catalytic beta-subunit of the 20S proteasome inhibiting its chymotrypsin-like and trypsin-like activities. Also known to inhibit NF-κappaB activation (IC50 = 10 µM).

Aclacinomycin A

产品介绍 Aclacinomycin A is a specific inhibitor of the 20S proteasome chymotrypsin-like activity and calpain activity. Aclarubicin acts by forming a stable complex with DNA. It was originally identified as an antitumor agent. Cell permeable.

Tubacin

产品介绍 Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor . Tubacin does not inhibit HDAC6 histone deacetylase activity; instead, tubacin is specific for the tubulin deacetylase activity of HDAC6. It reversibly inhibits α-tubulin deacetylation in mammalian cells and increases α-tubulin acetylation levels with no effect on histone acetylation or cell cycle progression.

Tankyrase Inhibitors (TNKS) 49

背景介绍 Tankyrase 1 and tankyrase 2 are members of PARP family. They can use NAD+ as substrates to transfer ADP-ribose polymers onto target proteins. The tankyrases bind and PARSylate axin proteins which are the negative regulator of Wnt pathway. Thus tankyrasesa re promising targets for treatment for adenomatous polyposis coli. Tankyrase inhibitor 49 is an optimization of the previous hit compound inhibitor 8 with improved potency and selectivity. It has excellent effects in both tankyrase assay and cellular assay (total β-catenin degradation assay in SW480 cells) with IC50 values of 0.1 nM and 1.9 nM, respectively. In addition, it is found to be a dual binder with both the nicotinamide pocket and the induced pocket of the enzymes. In the in vivo studies in rodents, tankyrase inhibitor 49 is found to potently inhibit TNKS2 autoparsylation with IC50 = 7.6 nM. It also causes stabilization and accumulation of axin protein in SW480 cells with EC50= 4 nM. In DLD-1 cells with truncated APC, the inhibitor inhibits the STF reporter transcription with IC50 = 0.3 nM, suggesting its downstream inhibitory activity on Wnt-associated transcription. 产品介绍 Tankyrase Inhibitor 49 (TNKSi49) is a potent, selective and orally bioavailable inhibitor of tankyrase with IC50 value of 0.1 nM.

Tankyrase Inhibitors (TNKS) 22

背景介绍 Tankyrase 1 and tankyrase 2 are members of PARP family. They can use NAD+ as substrates to transfer ADP-ribose polymers onto target proteins. The tankyrases bind and PARSylate axin proteins which are the negative regulator of Wnt pathway. Thus tankyrasesa re promising targets for treatment for adenomatous polyposis coli. Tankyrase inhibitor 22 is an optimization of the previous hit compound inhibitor 8 with improved potency and selectivity. It has excellent effects in both tankyrase assay and cellular assay (total β-catenin degradation assay in SW480 cells) with IC50 values of 0.1 nM and 3.7 nM, respectively. In addition, it is found to be a dual binder with both the nicotinamide pocket and the induced pocket of the enzymes. In the in vivo studies in rodents, tankyrase inhibitor 22 is found to potently inhibit TNKS2 autoparsylation with IC50 = 4.1 nM. It also causes stabilization and accumulation of axin protein in SW480 cells with EC50 = 3.9 nM. In DLD-1 cells with truncated APC, the inhibitor inhibits the STF reporter transcription with IC50 = 0.6 nM suggesting its downstream inhibitory activity on Wnt-associated transcription 产品介绍 Tankyrase Inhibitor 22 (TNKSi22) is a potent, selective and orally bioavailable inhibitor of tankyrase with IC50 value of 0.1 nM.

Sodium Phenylbutyrate

产品介绍 Sodium Phenylbutyrate is a transcriptional regulator that acts by altering chromatin structure via the modulation of HDAC activity.