NSC228155
An EGFR activator and inhibitor of KID-KIX interactions
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包装价格促销价数量
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10mg￥762.00610.00- +
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50mg￥3050.002440.00- +
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100mg￥5287.004230.00- +
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500mg￥0.000.00- +
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1g￥0.000.00- +
- 货号: ajci12448
- CAS: 113104-25-9
- 别名:
- 分子式: C11H6N4O4S
- 分子量: 290.25
- 纯度: ＞98%
- 溶解度: ≥ 29mg/mL in DMSO
- 储存: Store at -20°C
- 库存: 现货
Background
IC50: 0.36 μM for KIX-KID interaction
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].
In vivo: So far, there is no animal in vivo data reported.
Clinical trial: Up to now, NSC228155 is still in the preclinical development stage.
Reference:
[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.
