CAS NO: | 321695-57-2 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | L002 is a potent, cell permeable, reversible and specificacetyltransferase p300 (KAT3B)inhibitor with an IC50 of 1.98 μM[1]. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibitsSTAT3activation[2]. L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment[3]. | ||||||||||||||||
IC50& Target | IC50: 1.98 uM (KAT3B); 35 μM (PCAF); 34 μM (GCN5)[1];STAT3; p53[2] | ||||||||||||||||
体外研究 (In Vitro) | L002 also has weak inhibitory effects against PCAF and GCN5 (IC50s =35 and 34 μM, respectively) and is specific for p300 over a panel of additional acetyltransferases, deacetylases, and methyltransferases[1]. | ||||||||||||||||
体内研究 (In Vivo) | L002 (intraperitoneal injection; 20 μg/gm body weight; every 3rd day; 2 weeks) reverses hypertension‐induced cardiac hypertrophy and fibrosis by treatment of mice after inducing hypertension for two weeks significantly.It also reduces the levels of perivascular and interstitial collagen in the myocardium compared to non-treated hypertensive mice[3].
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分子量 | 321.35 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C15H15NO5S | ||||||||||||||||
CAS 号 | 321695-57-2 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 62.5 mg/mL(194.49 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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