For research use only. Not for therapeutic Use.
Roginolisib (MSC2360844; IOA-244) is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. Roginolisib shows highly selective against a panel of 278 additional kinases[1].
Roginolisib (0-10 μM; 1 hours) completely abolished BCR-induced pAkt in Ramos B cells in a concentration-dependent manner with IC50 values of 280 nM[1].
Roginolisib inhibits B cell proliferation in a concentration-dependent manner with an IC50 of 48 nM. Roginolisib blocks BCR- and TCR-mediated responses in lymphocytes and TLR-induced IFNα by pDC in human primary cells[1].
Roginolisib (6.6-66 mg/kg; daily from week 2 to 10) ameliorates disease manifestations in a murine SLE model[1].
| Catalog Number | I016823 |
| CAS Number | 1305267-37-1 |
| Synonyms | [6-fluoro-1-[4-(morpholin-4-ylmethyl)phenyl]-5,5-dioxo-4H-thiochromeno[4,3-c]pyrazol-3-yl]-morpholin-4-ylmethanone |
| Molecular Formula | C26H27FN4O5S |
| Purity | ≥95% |
| InChI | InChI=1S/C26H27FN4O5S/c27-22-3-1-2-20-24-21(17-37(33,34)25(20)22)23(26(32)30-10-14-36-15-11-30)28-31(24)19-6-4-18(5-7-19)16-29-8-12-35-13-9-29/h1-7H,8-17H2 |
| InChIKey | NFHSJYKXENYICE-UHFFFAOYSA-N |
| SMILES | C1COCCN1CC2=CC=C(C=C2)N3C4=C(CS(=O)(=O)C5=C4C=CC=C5F)C(=N3)C(=O)N6CCOCC6 |
| Reference | [1]. Haselmayer P, et al. Characterization of Novel PI3Kδ Inhibitors as Potential Therapeutics for SLE and Lupus Nephritis in Pre-Clinical Studies. Front Immunol. 2014 May 22;5:233. |
