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Merck
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SML1272

Sigma-Aldrich

I-BET762

≥98% (HPLC)

同義詞:

(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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About This Item

經驗公式（希爾表示法）:
C22H22ClN5O2
CAS號碼:
1260907-17-2
分子量：:
423.90
MDL號碼:
MFCD22417091
分類程式碼代碼:
12352200
PubChem物質ID:
329825759
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

光學活性

[α]/D +80 to +90°, c = 0.3 in methanol

藥物控制

regulated under CDSA - not available from Sigma-Aldrich Canada

顏色

white to beige

溶解度

DMSO: 10 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

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 密鑰

AAAQFGUYHFJNHI-SFHVURJKSA-N

基因資訊

human ... BRD2(6046) , BRD3(8019) , BRD4(23476) , BRDT(676)

生化／生理作用

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 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。

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

分析證明 (COA)

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存取文件庫

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