Immunosuppressive activity in BALB/c mouse splenic T cells assessed as inhibition of PMA/CD28 induced cell proliferation after 24 hrs by [methyl-3H]thymidine incorporation assay
Immunosuppressive activity in collagen-induced DBA/1J mouse arthritis model at 0.3 to 1 mg/kg, po administered for 8 weeks after 9 weeks of immunization with bovine type II collagen measured at 21 to 42 days after primary immunization
Competitive inhibition of BRD2 in PMA /ionomycin activated human Jurkat cell lysate in presence of (S)-4-{3'-Cyano-4'-[3-(3-{2-[5-((3aR,6S,6aS)-2-oxo-hexahydro-thieno[3,4-d]imidazol-6-yl)-pentanoylamino]-ethyldisulfanyl}-propionylamino)-propoxy]-biphenyl-4-yl}-2,3,9-trimethyl-6H-1-thia-5,7,8,9a-tetraaza-cyclopenta[e]azulene-6-yl]acetic acid ethyl ester/avidin-resin by pull down assay
Competitive inhibition of BRD3 in PMA /ionomycin activated human Jurkat cell lysate in presence of (S)-4-{3'-Cyano-4'-[3-(3-{2-[5-((3aR,6S,6aS)-2-oxo-hexahydro-thieno[3,4-d]imidazol-6-yl)-pentanoylamino]-ethyldisulfanyl}-propionylamino)-propoxy]-biphenyl-4-yl}-2,3,9-trimethyl-6H-1-thia-5,7,8,9a-tetraaza-cyclopenta[e]azulene-6-yl]acetic acid ethyl ester/avidin-resin by pull down assay
Competitive inhibition of BRD4 in PMA /ionomycin activated human Jurkat cell lysate in presence of (S)-4-{3'-Cyano-4'-[3-(3-{2-[5-((3aR,6S,6aS)-2-oxo-hexahydro-thieno[3,4-d]imidazol-6-yl)-pentanoylamino]-ethyldisulfanyl}-propionylamino)-propoxy]-biphenyl-4-yl}-2,3,9-trimethyl-6H-1-thia-5,7,8,9a-tetraaza-cyclopenta[e]azulene-6-yl]acetic acid ethyl ester/avidin-resin by pull down assay
Inhibition of Flag-tagged BRD4 (unknown origin)-biotinylated AcH4 (Lys5, 8, 12, 16) histone peptide binding expressed in CHO cells after 60 mins by TR-FRET assay
Inhibition of Flag-tagged BRD3 (unknown origin)-biotinylated AcH4 (Lys5, 8, 12, 16) histone peptide binding expressed in CHO cells after 60 mins by TR-FRET assay
Inhibition of Flag-tagged BRD2 (unknown origin)-biotinylated AcH4 (Lys5, 8, 12, 16) histone peptide binding expressed in CHO cells after 60 mins by TR-FRET assay