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| | NSC228155 Basic information |
| Product Name: | NSC228155 | | Synonyms: | NSC228155;NSC228155;NSC-228155;NSC 228155;2-[(7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)thio]pyridine 1-oxide;NSC-228155;NSC 228155;Epidermal growth factor receptor,Histone Acetyltransferase,EGFR,HER1,HATs,inhibit,Inhibitor,NSC-228155,HAT,Epigenetic Reader Domain,NSC 228155,ErbB-1;2,1,3-Benzoxadiazole, 4-nitro-7-[(1-oxido-2-pyridinyl)thio]- | | CAS: | 113104-25-9 | | MF: | C11H6N4O4S | | MW: | 290.25 | | EINECS: | | | Product Categories: | | | Mol File: | 113104-25-9.mol |  |
| | NSC228155 Chemical Properties |
| Boiling point | 627.3±65.0 °C(Predicted) | | density | 1.72±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C(protect from light) | | solubility | ≥29 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH | | form | solid | | pka | -1.48±0.10(Predicted) |
| | NSC228155 Usage And Synthesis |
| 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 | | 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. |
| | NSC228155 Preparation Products And Raw materials |
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