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2070014-93-4

中文名稱 PF-CBP1
英文名稱 PF-CBP1 (hydrochloride)
CAS 2070014-93-4
分子式 C29H37ClN4O3
分子量 525.09
MOL 文件 2070014-93-4.mol
更新日期 2023/03/20 15:41:27
2070014-93-4 結構式 2070014-93-4 結構式

基本信息

中文別名
化合物PF-CBP1 HYDROCHLORIDE
英文別名
PF-CBP1 (hydrochloride)
HFOZCHHWLMTUTP-UHFFFAOYSA-N
5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-[2-(morpholin-4-yl)ethyl]-2-[2-(4-propoxyphenyl)ethyl]-1H-1,3-benzodiazole
5-?(3,?5-Dimethyl-?4-?isoxazolyl)?-?1-?[2-?(4-?morpholinyl)?ethyl]?-?2-?[2-?(4-?propoxyphenyl)?ethyl]?-1H-?benzimidazole Hydrochloride

物理化學性質

儲存條件-20°C儲存
溶解度≥52.5 mg/mL in DMSO; insoluble in H2O; ≥40.6 mg/mL in EtOH
形態(tài)固體
顏色White to yellow
PF-CBP1價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-19999APF-CBP1
PF-CBP1 hydrochloride
2070014-93-45mg500元
2024/11/08HY-19999APF-CBP1
PF-CBP1 hydrochloride
2070014-93-410mg750元
2024/11/08HY-19999APF-CBP1
PF-CBP1 hydrochloride
2070014-93-410mM * 1mLin DMSO751元

常見問題列表

生物活性
PF-CBP1 hydrochloride 是 CREB 結合蛋白溴結構域 (CBP BRD) 的高選擇性抑制劑。PF-CBP1 抑制 CREBBP 和 EP300 溴結構域的 IC50 分別為 125 nM 和 363 nM。PF-CBP1 hydrochloride 降低 LPS 誘導的巨噬細胞中炎癥因子 (IL-1β、IL-6 和IFN-β) 的表達。PF-CBP1 hydrochloride 也可下調(diào)皮質神經(jīng)元 RGS4 的表達,可用于癲癇和帕金森病等多種神經(jīng)疾病的研究。
靶點

CREBBP

125 nM (IC 50 )

EP300

363 nM (IC 50 )

CBP

0.19 μM (Kd)

BRD4

20 μM (Kd)

體外研究

ITC is the label-free technique for determining K D values, PF-CBP1 is against CBP (K d =0.19 μM) and >105-fold selective over BRD4 (K d >20 μM) by ITC.PF-CBP1 displays greater than 100-fold selectivity for the bromodomain of CBP over those of BRD4 and a panel of other proteins, it against BRD2-1,BRD3-1, BRD3-2,BRD4-1, BRD4-2, BRDT-1, TAF1-2, and TAF1L-2 with IC 50 values of 1.24 μM, 1.38 μM, 4.22 μM, 1.54 μM, 9.75 μM, 2.44 μM, 3.39 μM and 7.29 μM, respectively.PF-CBP1 (3-10 μM; pretreatment 30 mins; 4 hours) moderately reduces LPS-induced IL-6 and IFN-b expression in the J774 cell at 10 μM. And it decreases IL-1b expression evidently at 3 μM.PF-CBP1 (100 nM-1000 nM;24 hours) significantly reduced RGS4 mRNA levels(49% reduction) relative to vehicle in cortical neuron cells.

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