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化學性質:
規格 | 10mg 50mg 100mg 500mg 1g |
CAS | 113104-25-9 |
別名 | N/A |
化學名 | 2-((7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)thio)pyridine 1-oxide |
分子式 | C11H6N4O4S |
分子量 | 290.25 |
溶解度 | ≥ 29mg/mL in DMSO |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述:
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.
特別提醒:
1. 本產品僅供科研使用。請勿用于醫藥、臨床診斷或治療,食品及化妝品等用途。請勿存放于普通住宅區。
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原創作者:上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業部
賬 號:2169 2341 6278