|S1029||Lenalidomide (CC-5013)||<1 mg/mL||52 mg/mL||<1 mg/mL|
|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|
|S5913||Cambinol||<1 mg/mL||21 mg/mL||<1 mg/mL|
|S8641||Nec-1s (7-Cl-O-Nec1)||<1 mg/mL||56 mg/mL||9 mg/mL|
|S9090||Corilagin||-1 mg/mL||100 mg/mL||-1 mg/mL|
|S8642||GSK'963||<1 mg/mL||46 mg/mL||46 mg/mL|
|S8034||Apremilast (CC-10004)||<1 mg/mL||92 mg/mL||<1 mg/mL|
|S1623||Acetylcysteine||33 mg/mL||33 mg/mL||33 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|
Adalimumab is the first fully human, recombinant IgG1 monoclonal antibody that specifically targets human TNF-alpha, MW: 144.19 KD.
Lenalidomide (CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs.
MM1S were treated with AT9283 (0.125 μM), lenalidomide (2 μM) or combined therapy for 72 hours. Annexin/PI staining show increased apoptosis associated with caspase 8 and PARP cleavage after 18 and 36 hours of exposure.
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.
TE7 cells (2 × 105) were pretreated with PD98059 (20 μM), QNZ (EVP4593; 20 μM), AZD5363 (20 μM), S1155 (20 μM) and Tra (40 ng/ml) for 1 h and stimulated with IL6 (40 ng/ml) for 48 h.
Cambinol is a novel uncompetitive nSMase2 inhibitor with a K i value of 7 μM (IC50 = 5 ± 1 μM).
Nec-1s is a stable variant of Necrostatin-1. It is a more specific RIPK1 inhibitor lacking the IDO-targeting effect, with >1000-fold more selective for RIPK1 than for any other kinase out of 485 human kinases.
Corilagin, discovered in many medicinal plants such as Phyllanthus speices etc., has multiple activities including anti-oxidative, anti-inflammatory, anti-apoptotic, hepatoprotective and others. It is an inhibitor of TNF-α.
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.
Apremilast (CC-10004) is a potent and orally active PDE4 and TNF-α inhibitor with IC50 of 74 nM and 77 nM, respectively.
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.
(C) Double immunolabeling showed CK-labeled cells (green) co-expressed with 40, 6-diamidino-2-phenylindole (DAPI) (blue), scale bars are 50 μm.
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.