CAS NO: | 177355-84-9 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 |
DBeQ is a selective, potent, reversible, and ATP-competitivep97inhibitor, with anIC50value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibitsVps4with anIC50of 11.5 μM. |
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IC50& Target |
IC50: 1.5 μM (p97)[1], 11.5 μM (Vps4)[2] |
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体外研究 (In Vitro) |
DBeQ is a ATP-competitive p97 inhibitor, with an IC50value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively. DBeQ inhibits p97 competitively with respect to ATP, with a Kiof 3.2 ± 0.4 μM. DBeQ inhibits degradation of the p97-dependent substrate UbG76V-GFP, with IC50value of 2.6 μM. DBeQ (10 μM) also significantly suppresses degradation of TCRα-GFP, induces CHOP but does not increase p21 level. Moreover, DBeQ inhibits the viability of MRC-5, Hek293, HeLa and RPMI8226 cells, with GI50s of 6.6 ± 2.9, 4 ± 0.6, 3.1 ± 0.5 and 1.2 ± 0.3, respectively[1]. DBeQ potently inhibits the AAA ATPase p97 by specifically binding to the ATPase site of its D2 domain (p97D2). DBeQ also inhibits Vps4, with an IC50of 11.5 μM. Furthermore, DBeQ (30 μM) inhibits hyphal growth of the wild-type cell (strain YLZ0)[2].
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分子量 |
340.42 |
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性状 |
Solid |
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Formula |
C22H20N4 |
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CAS 号 |
177355-84-9 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 35.71 mg/mL(104.90 mM;Need ultrasonic)
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In Vivo:
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