| Identification | Back Directory | [Name]
NSC228155 | [CAS]
113104-25-9 | [Synonyms]
NSC228155
NSC-228155;NSC 228155
NSC228155;NSC-228155;NSC 228155
2-[(7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)thio]pyridine 1-oxide | [Molecular Formula]
C11H6N4O4S | [MDL Number]
MFCD30742994 | [MOL File]
113104-25-9.mol | [Molecular Weight]
290.25 |
| Chemical Properties | Back Directory | [storage temp. ]
Keep in dark place,Sealed in dry,2-8°C | [solubility ]
≥29 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH | [form ]
solid |
| Hazard Information | Back Directory | [Biological Activity]
nsc228155 is a potent inhibitor of kix-kid interaction.cyclic-amp response-element binding protein (creb) is identified as a stimulus-activated transcription factor. its transcription activity needs its binding with creb-binding protein (cbp) after creb is phosphorylated at ser133. the domains involved for creb-cbp interaction are kinase-inducible domain (kid) from creb and kid-interacting domain (kix) from cbp. | [in vitro]
previous study found that nsc228155 could dose-dependently inhibit kix–kid interaction as measured by the split rluc assay. in living hek 293t cells, nsc228155 could inhibit creb-mediated gene transcription with an ic50 of 2.09 μm. nsc228155 also inhibited vp16-creb-mediated gene transcription with an ic50 of 6.14 μm. though this was around 3-fold higher than the ic50 of creb-mediated gene transcription, such results indicated that nsc228155 was not particularly selective in inhibiting kix–kid interaction inside these living cells. therefore, although nsc228155 was a potent inhibitor of kix-kid interaction, it was not selective against creb-mediated gene transcription, and further sar studies identified a 4-aniline substituted analog displaying a higher selectivity index [1]. | [target]
| EGFR | KIX-KID 0.36 μM (IC 50 ) | | [IC 50]
0.36 μm for kix-kid interaction | [storage]
Store at -20°C | [References]
[1] xie f, li bx, broussard c, xiao x. identification, synthesis and evaluation of substituted benzofurazans as inhibitors of creb-mediated gene transcription. bioorg med chem lett. 2013 oct 1;23(19):5371-5. |
|
|