321695-57-2
中文名稱
L 002;NSC 764414;L-002;NSC-764414
英文名稱
NSC764414
CAS
321695-57-2
分子式
C15H15NO5S
分子量
321.35
MOL 文件
321695-57-2.mol
321695-57-2 結(jié)構(gòu)式
基本信息
中文別名
化合物L(fēng)002化合物L(fēng)002,10 MM DMSO 溶液
4-[O-[(4-甲氧基苯基)磺?；鵠肟] -2,6-二甲基-2,5-環(huán)己二烯-1,4-二酮
英文別名
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
物理化學(xué)性質(zhì)
沸點(diǎn)459.8±55.0 °C(Predicted)
密度1.28±0.1 g/cm3(Predicted)
儲(chǔ)存條件2-8°C
溶解度在DMSO中的溶解度為20mg/mL，澄清
形態(tài)粉末
顏色白色至米色
L 002;NSC 764414;L-002;NSC-764414價(jià)格(試劑級(jí))
| 報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
| 2024/11/08 | HY-100671 | L 002;NSC 764414;L-002;NSC-764414 L002 | 321695-57-2 | 5mg | 950元 |
| 2024/11/08 | HY-100671 | L 002;NSC 764414;L-002;NSC-764414 L002 | 321695-57-2 | 10mM * 1mLin DMSO | 1045元 |
| 2024/11/08 | HY-100671 | L 002;NSC 764414;L-002;NSC-764414 L002 | 321695-57-2 | 10mg | 1390元 |
常見問題列表
生物活性
L002 是一種有效的，細(xì)胞可滲透的，可逆的和特定的乙酰轉(zhuǎn)移酶 p300(KAT3B) 抑制劑，IC50 為 1.98 μM。 L002 結(jié)合乙酰輔酶 A 口袋并競(jìng)爭(zhēng)性抑制 FATp300 催化結(jié)構(gòu)域，阻斷組蛋白乙?；?p53 乙酰化，且抑制 STAT3 激活。L002 有潛力用于高血壓引起的心臟肥大和纖維化的研究。靶點(diǎn)
IC50: 1.98 uM (KAT3B); 35 μM (PCAF); 34 μM (GCN5) ;STAT3; p53
體外研究
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.
體內(nèi)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. |