PF-CBP1 HCl

製品コードS8180 バッチS818001

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₉H₃₆N₄O₃.HCl
	分子量	525.08	CAS No.	2070014-93-4
Solubility (25°C)*	体外	DMSO	100 mg/mL (190.44 mM)
		Ethanol	100 mg/mL (190.44 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	PF-CBP1 HCl 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.
in vitro	PF-CBP1 modulates key inflammatory genes in primary macrophages. PF-CBP1 down regulates RGS4 in neurons, a target linked to Parkinson's disease.It is 139-fold selective over BRD4 in the biochemical assays and >105-fold selective by ITC.PF-CBP1 is also a potent inhibitor of EP300 and possesses no cytotoxicity in macrophages, and hepatotoxicity in cell-based models as long as the concentration is not very high^[1].

製品説明

PF-CBP1 HCl 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.

in vitro

PF-CBP1 modulates key inflammatory genes in primary macrophages. PF-CBP1 down regulates RGS4 in neurons, a target linked to Parkinson's disease.It is 139-fold selective over BRD4 in the biochemical assays and >105-fold selective by ITC.PF-CBP1 is also a potent inhibitor of EP300 and possesses no cytotoxicity in macrophages, and hepatotoxicity in cell-based models as long as the concentration is not very high^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	mouse J774 macrophage-like cell line
	濃度	0.1-10 μM
	反応時間	30min
	実験の流れ	Cells are pretreated with the probes PF-CBP1, ISOX-INACT, or ISOX-DUAL starting at 10 μM concentrations, and then serially diluted to 0.1 μM. After 30 min, the cells are treated with LPS to induce gene transcription and the expression levels of interleukin-6 (IL-6), IL-1β, and interferon-β (IFN-β)(which are known to be induced after 4 h of LPS exposure) are analyzed by RT-PCR. Probe PF-CBP1 moderately reduces LPS-induced IL-6 and IFN-β expression at 10 μM, and a decrease in IL-1β expression is evident at 3 μM.

参考

[1] Eugene L, et al. Chem Biol. 2015, 22(12):1588-1596.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Brain milieu induces early microglial maturation through the BAX-Notch axis [ Nat Commun, 2022, 13-1:6117]	PubMed: 36253375
The transcriptional coactivator CBP/p300 is an evolutionarily conserved node that promotes longevity in response to mitochondrial stress [ Nat Aging, 2021, 1(2):165-178]	PubMed: 33718883
Interferon-γ Signaling in Melanocytes and Melanoma Cells Regulates Expression of CTLA-4 [ Cancer Res, 2018, 78(2):436-450]	PubMed: 29150430
Interferon-γ Signaling in Melanocytes and Melanoma Cells Regulates Expression of CTLA-4 [ Cancer Res, 2018, 78(2):436-450]	PubMed: 29150430
Epigenetic Reprogramming with Antisense Oligonucleotides Enhances the Effectiveness of Androgen Receptor Inhibition in Castration-Resistant Prostate Cancer [ Cancer Res, 2018, 78(20):5731-5740]	PubMed: 30135193

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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