Description
Pomalidomide can inhibit TNF-alpha release with IC50 of 13 nM.
Storage
2 years at -20centigrade Powder
Molecular Formula
C13H11N3O4
Chemical Name
4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione
Solubility
DMSO 55 mg/mL Water
In vitro
Pomalidomide can inhibit TNF-alpha release with IC50 of 13 nM. Pomalidomide (CC-4047) exhibit anti-angiogenic, anti-proliferative, and pro-erythropoietic activities. Pomalidomide (CC-4047) shows anti-inflammatory effects on LPS-stimulated monocytes and decrease TNF-alpha. Pomalidomide (CC-4047) also shows costimulatory effects on anti-CD3 stimulated T cells and enhance T cell proliferation and proinflammatory cytokine production. Pomalidomide (CC-4047) can cause augmentation of NK-cell cytotoxic activity against tumour-cell targets. Pomalidomide cause cell cycle arrest in Burkitts lymphoma and multiple myeloma cell lines by increasing the level of p21(WAF-1) expression. Pomalidomide modify the chromatin structure of the p21(WAF-1) promoter through demethylation and acetylation of H3K9. In this way, pomalidomide plays an important role in the regulation of gene transcription. Pomalidomide used alone or in combination with hydroxyurea, may improve erythropoiesis and increase the ratio of fetal to adult hemoglobin.
In vivo
In Tsk-1 mice and in bleomycin-induced dermal fibrosis, treatment with pomalidomide in doses from 0.3 to 30 mg/kd/day prevented skin fibrosis in a dose-dependent manner and reduced the expression of transforming growth factor (TGF) beta-target genes such as PAI-1, CTGF and col 1a1.
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