L 002;NSC 764414;L-002;NSC-764414
| 中文名稱 | L 002;NSC 764414;L-002;NSC-764414 |
|---|---|
| 中文同義詞 | 化合物L(fēng)002;4-[O-[(4-甲氧基苯基)磺酰基]肟] -2,6-二甲基-2,5-環(huán)己二烯-1,4-二酮;化合物L(fēng)002,10 MM DMSO 溶液;L-002 (NSC 764414;L002);L002 (NSC764414) ,E0405 |
| 英文名稱 | NSC764414 |
| 英文同義詞 | 4-[O-[(4-Methoxyphenyl)sulfonyl]oxime]-2,6-dimethyl-2,5-cyclohexadiene-1,4-dione;L002;NSC764414;p300/CBP Inhibitor VI, L002;[(3,5-dimethyl-4-oxo-cyclohexa-2,5-dien-1-ylidene)amino] 4-methoxybenzenesulfonate;L002(NSC764414);L 002;NSC 764414;L-002;NSC-764414;p300/CBP Inhibitor VI, L002 - CAS 321695-57-2 - Calbiochem |
| CAS號 | 321695-57-2 |
| 分子式 | C15H15NO5S |
| 分子量 | 321.35 |
| EINECS號 | |
| 相關(guān)類別 | |
| Mol文件 | 321695-57-2.mol |
| 結(jié)構(gòu)式 |  |
L 002;NSC 764414;L-002;NSC-764414 性質(zhì)
| 沸點(diǎn) | 459.8±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.28±0.1 g/cm3(Predicted) |
| 儲存條件 | 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 |
| InChI | 1S/C15H15NO5S/c1-10-8-12(9-11(2)15(10)17)16-21-22(18,19)14-6-4-13(20-3)5-7-14/h4-9H,1-3H3 |
| InChIKey | VEWFTYOFWIXCIO-UHFFFAOYSA-N |
| SMILES | [S](=O)(=O)(ON=C2C=C(C(=O)C(=C2)C)C)c1ccc(cc1)OC |
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 口袋并競爭性抑制 FATp300 催化結(jié)構(gòu)域，阻斷組蛋白乙酰化和 p53 乙?；乙种?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。
IC50: 1.98 uM (KAT3B); 35 μM (PCAF); 34 μM (GCN5) ;STAT3; p53
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.
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. |
安全信息
| WGK Germany | 3 |
|---|---|
| 存儲類別 | 11 - 可燃固體 |
| 更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價(jià)格 |
|---|---|---|---|---|---|
| 2026/06/05 | HY-100671 | L 002;NSC 764414;L-002;NSC-764414 L002 | 321695-57-2 | 5mg | 950元 |
| 2026/06/05 | HY-100671 | L 002;NSC 764414;L-002;NSC-764414 L002 | 321695-57-2 | 10mM * 1mLin DMSO | 1045元 |