SML1272
I-BET762
≥98% (HPLC)
别名:
(4S)-6-（4-氯苯基）-N-乙基-8-甲氧基-1-甲基-4H-[1,2,4] 三唑 [4,3-a] [1,4] 苯二氮卓-4-乙酰胺, GSK525762, GSK525762A, I-BET
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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)
Bromodomains: are readers right for epigenetic therapy?.
Conway S J.
ACS Medicinal Chemistry Letters, 3(9), 691?694-691?694 (2012)
Laura Helminen et al.
Nucleic acids research, 52(2), 625-642 (2023-11-28)
Treatment of prostate cancer relies predominantly on the inhibition of androgen receptor (AR) signaling. Despite the initial effectiveness of the antiandrogen therapies, the cancer often develops resistance to the AR blockade. One mechanism of the resistance is glucocorticoid receptor (GR)-mediated
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| SML1272-25MG | 04061832825557 |
| SML1272-5MG | 04061838356932 |