PF-CBP1 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PF-CBP1 是 CREB 结合蛋白溴结构域 (CREBBP) 的高选择性抑制剂。它抑制 CREBBP 和 p300 溴结构域，IC50 分别为 125 和 363 nM。

PF-CBP1 is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.

ITC is the label-free technique for determining KD values, PF-CBP1 is against CBP (Kd=0.19 μM) and >105-fold selective over BRD4 (Kd>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 IC50 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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Endocrinology/Hormones

Opioid Receptor

CREBBP| p300/CBP

Neurological Disease

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2070014-93-4

525.08

C29H37ClN4O3

>98% (HPLC)

DMSO : ≥ 34 mg/mL; 64.75 mM

CCCOc1ccc(cc1)CCc1nc2c(n1CCN1CCOCC1)ccc(c2)c1c(onc1C)C.Cl

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(-20℃)

With Ice Pack

≥ 2 years