SP100030

SP100030 is an inhibitor of gene transcription mediated by NF-κB and activator protein-1 (AP-1).¹ It inhibits NF-κB- and AP-1-mediated transcription in a reporter assay using Jurkat T cells (IC₅₀ = 0.05 µM for both) and decreases IL-2 and IL-8 levels in Jurkat T cells (IC₅₀ = 0.03 µM for both). SP100030 (20 mg/kg per day for three days) reduces eosinophil and T cell infiltration into bronchoalveolar lavage fluid (BALF) and reduces Ap-1 and phosphorylated Ap-1 levels in isolated lung tissue in an ovalbumin-sensitized rat model of asthma.² It prevents tumor-induced decreases in skeletal muscle, brown adipose tissue, spleen, kidney, and heart mass in a rat model of cachexia when administered at a dose of 1 mg/kg per day.³ SP100030 (10 mg/kg per day) inhibits bleomycin-induced decreases in body weight, increases in wet-dry lung weight ratio, and increases in lung total protein, myeloperoxidase (Mpo), elastase, collagen, and IL-1β levels in a mouse model of pulmonary fibrosis.⁴

WARNING This product is not for human or veterinary use.

1. Sullivan, R.W., Bigam, C.G., Erdman, P.E., et al. 2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3',5'-bis(trifluoromethyl)phenyl)-carboxamid e: A potent inhibitor of NF-κB- and AP-1-mediated gene expression identified using solution-phase combinatorial chemistry. J. Med. Chem. 41(4), 413-419 (1998).

2. Huang, T.J., Adcock, I.M., and Chung, K.F. A novel transcription factor inhibitor, SP100030, inhibits cytokine gene expression, but not airway eosinophilia or hyperresponsiveness in sensitized and allergen-exposed rat. Br. J. Pharmacol. 134(5), 1029-1036 (2001).

3. Moore-Carrasco, R., Busquets, S., Almendro, V., et al. The AP-1/NF-κB double inhibitor SP100030 can revert muscle wasting during experimental cancer cachexia. Int. J. Oncol. 30(5), 1239-1245 (2007).

4. Fujimoto, H., D'Alessandro-Gabazza, C.N., Palanki, M.S.S., et al. Inhibition of nuclear factor-κB in T cells suppresses lung fibrosis. Am. J. Respir. Crit. Care Med. 176(12), 1251-1260 (2007).