321695-57-2
中文名称
L 002;NSC 764414;L-002;NSC-764414
CAS
321695-57-2
分子式
C15H15NO5S
分子量
321.35
MOL 文件
321695-57-2.mol
321695-57-2 结构式
基本信息
英文别名
L002NSC764414
L002(NSC764414)
p300/CBP Inhibitor VI, L002
L 002
NSC 764414
L-002
NSC-764414
p300/CBP Inhibitor VI, L002 - CAS 321695-57-2 - Calbiochem
4-[O-[(4-Methoxyphenyl)sulfonyl]oxime]-2,6-dimethyl-2,5-cyclohexadiene-1,4-dione
[(3,5-dimethyl-4-oxo-cyclohexa-2,5-dien-1-ylidene)amino] 4-methoxybenzenesulfonate
L 002;NSC 764414;L-002;NSC-764414价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2024/04/30 | HY-100671 | L 002;NSC 764414;L-002;NSC-764414 L002 | 321695-57-2 | 5mg | 950元 |
| 2024/04/30 | HY-100671 | L 002;NSC 764414;L-002;NSC-764414 L002 | 321695-57-2 | 10mM * 1mLin DMSO | 1045元 |
| 2024/04/30 | HY-100671 | L 002;NSC 764414;L-002;NSC-764414 L002 | 321695-57-2 | 10mg | 1390元 |
常见问题列表
生物活性
L002 是一种有效的，细胞可渗透的，可逆的和特定的乙酰转移酶 p300(KAT3B) 抑制剂，IC50 为 1.98 μM。 L002 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。L002 有潜力用于高血压引起的心脏肥大和纤维化的研究。靶点
IC50: 1.98 uM (KAT3B); 35 µM (PCAF); 34 µM (GCN5) ;STAT3; p53
体外研究
L002 also has weak inhibitory effects against PCAF and GCN5 (IC 50 s =35 and 34 µM, respectively) and is specific for p300 over a panel of additional acetyltransferases, deacetylases, and methyltransferases.
体内研究
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.
| Animal Model: | Wild‐type C57BL/6 male mice planted with osmotic minipumps ( Angiotensin II 1500 ng/kg/min) for 4 weeks |
| Dosage: | 20 μg/gm body weight; every 3rd day; 2 weeks |
| Administration: | Intraperitoneal injection |
| Result: | Reversed hypertension-induced cardiac fibrosis in mice. |