NSC228155
- CAS NO.:113104-25-9
- Empirical Formula: C11H6N4O4S
- Molecular Weight: 290.25
- MDL number: MFCD30742994
- Update Date: 2024-10-30 18:52:02
What is NSC228155?
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].
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.
Properties of NSC228155
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) |
color | Light yellow to orange |
Safety information for NSC228155
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for NSC228155
New Products
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