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关于此项目
经验公式(希尔记法):
C22H22ClN5O2
化学文摘社编号:
分子量:
423.90
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Quality Level
assay
≥98% (HPLC)
form
powder
optical activity
[α]/D +80 to +90°, c = 0.3 in methanol
drug control
regulated under CDSA - not available from Sigma-Aldrich Canada
color
white to beige
solubility
DMSO: 10 mg/mL, clear
storage temp.
2-8°C
SMILES string
CCNC(C[C@@H]1N=C(C2=CC=C(Cl)C=C2)C3=CC(OC)=CC=C3N4C1=NN=C4C)=O
InChI
1S/C22H22ClN5O2/c1-4-24-20(29)12-18-22-27-26-13(2)28(22)19-10-9-16(30-3)11-17(19)21(25-18)14-5-7-15(23)8-6-14/h5-11,18H,4,12H2,1-3H3,(H,24,29)/t18-/m0/s1
InChI key
AAAQFGUYHFJNHI-SFHVURJKSA-N
Gene Information
human ... BRD2(6046), BRD3(8019), BRD4(23476), BRDT(676)
Biochem/physiol Actions
I-BET762 通过控制促炎基因表达具有抗炎属性。I-BET762 在细胞模型中阻碍 MYC(原癌基因)的表达。I-BET762 的这一作用可作为治疗前列腺癌的有效疗法。
I-BET762 (GSK525762) 是溴结构域和末端外 (BET) 结构域蛋白 BRD2、BRD3 和 BRD4 的选择性抑制剂,IC 50 值为 32.5–42.5 nM,与其他含溴结构域蛋白无相互作用。I-BET 模拟乙酰化组蛋白,阻止乙酰化赖氨酸和 BET reader 蛋白之间的蛋白-蛋白相互作用。这表明阻断炎症基因在活化的巨噬细胞中的表达,并对内毒素性休克和细菌性败血症具有保护作用。I-BET762 在体外和体内也显示出强效的抗骨髓瘤活性 。
I-BET762 是溴结构域和末端外 (BET) 结构域蛋白的选择性抑制剂;合成组蛋白模拟物。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer.
Wyce A, et al.
Oncotarget, 4(12), 2419-2419 (2013)
Francesco Paolo Fiorentino et al.
International journal of molecular sciences, 21(24) (2020-12-20)
Small cell lung cancer (SCLC) is an aggressive type of lung cancer with high mortality that is caused by frequent relapses and acquired resistance. Despite that several target-based approaches with potential therapeutic impact on SCLC have been identified, numerous targeted
Bromodomains: are readers right for epigenetic therapy?.
Conway S J.
ACS Medicinal Chemistry Letters, 3(9), 691?694-691?694 (2012)
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| SML1272-25MG | 04061832825557 |
| SML1272-5MG | 04061838356932 |