产品
编 号：F318781
分子式：C15H15NO5S
分子量：321.35
分子式：C15H15NO5S
分子量：321.35
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
100mg
询价
询价
结构图
CAS No: 321695-57-2
产品详情
生物活性：
L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an?IC50?of 1.98 μM. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment.
体内研究：
L002（腹膜内注射；20 μg/gm 体重；每 3 天；2 周）对诱发高血压两周后的小鼠进行治疗，可显着逆转高血压诱发的心脏肥大和纤维化。与未治疗的高血压小鼠相比，它还能降低心肌血管周围和间质胶原的水平。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.
体外研究：
L002 对 PCAF 和 GCN5 也有微弱的抑制作用 (IC50=35 和 34 μM) 并且对一组额外的乙酰转移酶、脱乙酰酶和甲基转移酶的 p300 具有特异性。
L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an?IC50?of 1.98 μM. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment.
体内研究：
L002（腹膜内注射；20 μg/gm 体重；每 3 天；2 周）对诱发高血压两周后的小鼠进行治疗，可显着逆转高血压诱发的心脏肥大和纤维化。与未治疗的高血压小鼠相比，它还能降低心肌血管周围和间质胶原的水平。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.
体外研究：
L002 对 PCAF 和 GCN5 也有微弱的抑制作用 (IC50=35 和 34 μM) 并且对一组额外的乙酰转移酶、脱乙酰酶和甲基转移酶的 p300 具有特异性。
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备