Powder: -20°C for 3 years | In solvent: -80°C for 1 year
L002 是一种细胞可渗透的,可逆特定性乙酰转移酶 p300(KAT3B)抑制剂,IC50为 1.98 μM。 它结合乙酰辅酶 A 口袋并竞争性抑制 FATp300 催化结构域,阻断组蛋白乙酰化和 p53 乙酰化,且抑制 STAT3 激活,有用于高血压引起的心脏肥大和纤维化的研究潜力。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 329 | 现货 | ||
2 mg | ¥ 478 | 现货 | ||
5 mg | ¥ 763 | 现货 | ||
10 mg | ¥ 1,130 | 现货 | ||
25 mg | ¥ 2,590 | 现货 | ||
50 mg | ¥ 3,860 | 现货 | ||
100 mg | ¥ 5,530 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 857 | 现货 |
产品描述 | L002, a potent, cell-permeable, reversible, and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM, directly binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain. By blocking histone acetylation, p53 acetylation, and STAT3 activation, L002 shows potential in the treatment of hypertension‐induced cardiac hypertrophy and fibrogenesis. |
靶点活性 | PCAF:35 µM , KAT3B:1.98 uM , GCN5:34 µM |
体外活性 | 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 deacetylases, additional acetyltransferases, and methyltransferases. |
体内活性 | L002 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. |
分子量 | 321.35 |
分子式 | C15H15NO5S |
CAS No. | 321695-57-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 60 mg/mL (186.71 mM), Sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.1119 mL | 15.5594 mL | 31.1187 mL | 77.7968 mL |
5 mM | 0.6224 mL | 3.1119 mL | 6.2237 mL | 15.5594 mL | |
10 mM | 0.3112 mL | 1.5559 mL | 3.1119 mL | 7.7797 mL | |
20 mM | 0.1556 mL | 0.778 mL | 1.5559 mL | 3.8898 mL | |
50 mM | 0.0622 mL | 0.3112 mL | 0.6224 mL | 1.5559 mL | |
100 mM | 0.0311 mL | 0.1556 mL | 0.3112 mL | 0.778 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
L002 321695-57-2 Chromatin/Epigenetic JAK/STAT signaling Others Stem Cells STAT Histone Acetyltransferase p300 acetylation L 002 Inhibitor HATs HAT inhibit fibrosis cardiac L-002 histone inhibitor