- Inhibitory Selectivity
|Catalog No.||Product Name||Solubility(25°C)|
|S1567||Pomalidomide||<1 mg/mL||54 mg/mL||<1 mg/mL|
|S1193||Thalidomide||<1 mg/mL||51 mg/mL||2 mg/mL|
|S8037||Necrostatin-1||<1 mg/mL||51 mg/mL||<1 mg/mL|
|S4902||QNZ (EVP4593)||<1 mg/mL||5 mg/mL||<1 mg/mL|
|S1623||Acetylcysteine||33 mg/mL||33 mg/mL||33 mg/mL|
|S8642||GSK'963||<1 mg/mL||46 mg/mL||46 mg/mL|
|S4238||Cepharanthine||<1 mg/mL||100 mg/mL||<1 mg/mL|
|S8484||GSK2982772||<1 mg/mL||75 mg/mL||30 mg/mL|
|S7609||GW4869||<1 mg/mL||<1 mg/mL||<1 mg/mL|
|S8169||GSK481||<1 mg/mL||75 mg/mL||<1 mg/mL|
|S7942||Bioymifi||<1 mg/mL||43 mg/mL||<1 mg/mL|
- TNF-alpha Inhibitors (12)
- New TNF-alpha Products
|Catalog No.||Information||Product Use Citations||Product Validations|
Adalimumab is the first fully human, recombinant IgG1 monoclonal antibody that specifically targets human TNF-alpha, MW: 144.19 KD.
Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs.
MM.1S cells were cultured with Len (lenalidomide) or Pom (pomalidomide) for 48 h.
Thalidomide was introduced as a sedative drug, immunomodulatory agent and also is investigated for treating symptoms of many cancers. Thalidomide inhibits an E3 ubiquitin ligase, which is a CRBN-DDB1-Cul4A complex.
(E) MM.1S cells were treated with Thal(Thalidomide) or Pom for 48 hours. In each case, western blot was carried out using cell lysates and the indicated Abs.
Necrostatin-1 is a specific RIP1 inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM in 293T cells.
Cytosolic extracts or nuclear extracts were examined by Western blot analysis using Abs against p105/p50, p100/p52 and phospho-p65. Solid arrowhead indicates a non-specific band. A nuclear marker, PARP, and cytosolic marker, b-tubulin, were used to assess the purity of each fraction.
QNZ (EVP4593) shows potent inhibitory activity toward both NF-κB activation and TNF-α production with IC50 of 11 nM and 7 nM in Jurkat T cells, respectively.
NF-κB partly mediated resveratrol (Res) inhibition on PKD inflammation. (A) Expression of p-p65, p65, p105, p50, TNF-α, MCP-1 and CFB in QNZ-treated OX161 cells. (B) OX161 cells were pretreated with QNZ for 2 h and followed by the treatment of resveratrol for 46 h. The expression of p-p65, p65, p105, p50, TNF-α, MCP-1 and CFB were evaluated by western blot. (C) MCP-1 or CFB of QNZ-and/or resveratroltreated OX161 cell supernatants were measured by ELISA. One representative of three independent experiments is shown.
Acetylcysteine(N-acetyl-l-cysteine) is a ROS(reactive oxygen species) inhibitor that antagonizes the activity of proteasome inhibitors. It is also a tumor necrosis factor production inhibitor, used mainly as a mucolytic, protects against acetaminophen overdose-induced hepatotoxicity by maintaining or restoring hepatic concentrations of glutathione.
GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases.
Cepharanthine is a biscoclaurine alkaloid inhibiting tumor necrosis factor (TNF)-α-mediated NFκB stimulation, plasma membrane lipid peroxidation and platelet aggregation and suppressing cytokine production.
GSK2982772 is an ATP competitive receptor-interacting protein-1 (RIP1) kinase inhibitor with the IC50 value of 1 nM. It has exquisite kinase specificity and excellent activity in blocking many TNF-dependent cellular responses.
GW4869 is a neutral, noncompetitive inhibitor of sphingomyelinase (SMase) with an IC50 of 1 μM. It is selective for N-SMase, and does not inhibit acid SMase at up to at least 150 μM.
GSK481 is a RIP1(Receptor Interacting Protein Kinase1) inhibitor. Inhibition of RIP1 has been shown to hinder cell necrotic death.
Bioymifi, a small-molecule death receptor 5 (DR5) agonist, binds to the extracellular domain(ECD) of DR5 with a Kd of 1.2 μM but showed little binding affinity to the DR4 ECD. It induces DR5 clustering and aggregation, leading to apoptosis.