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CCT020312

目录号: PL09425 纯度: ≥98%

CCT020312 是选择性的 EIF2AK3/PERK 的激活剂。CCT020312 可诱导细胞细胞中 EIF2A 的磷酸化。

CAS No. :324759-76-4

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中文名称	CCT020312
英文名称	CCT020312
英文别名	CCT020312;6-Bromo-3-[5-(4-bromo-phenyl)-1-(3-diethylamino-propionyl)-4,5-dihydro-1H-pyrazol-3-yl]-4-phenyl-1H-quinolin-2-one;BrC=1C=C2C(=C(C(NC2=CC=1)=O)C1=NN(C(C1)C1=CC=C(C=C1)Br)C(CCN(CC)CC)=O)C1=CC=CC=C1
Cas No.	324759-76-4
分子式	C₃₁H₃₀Br₂N₄O₂
分子量	650.40
包装储存	Powder -20°C 3 years；In solvent -80°C 6 months
详情描述	CCT020312 是选择性的 EIF2AK3/PERK 的激活剂。CCT020312 可诱导细胞细胞中 EIF2A 的磷酸化。

产品详情	CCT020312 是选择性的 EIF2AK3/PERK 的激活剂。CCT020312 可诱导细胞细胞中 EIF2A 的磷酸化。
生物活性	CCT020312 is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells.
性状	Solid
IC50 & Target[1][2]	EIF2AK3/PERK.
体外研究(In Vitro)	Treatment of HT29 cells with CCT020312 for 24 hours reveals a concentration-dependent loss of P-S608-pRB signal, with a linear response between 1.8 and 6.1 μM. CCT020312 treatment effectively inhibits cell proliferation (as measured at 96 hours) even if treatment is for 2 hours only with subsequent compound washout, indicating that CCT020312 is capable of eliciting durable rather than transient cytostasis. Treatment of HT29 cells with 10 μM CCT020312 for 24 hours reduces the amount of the G1/S cyclins D1, D2, E and A as well as the CDK catalytic subunit CDK2 and increased the level of the CDK inhibitor p27KIP1 present in such cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Treatment of 15-week-old wildtype mice with the PERK activator CCT020312 (1-5 mg/kg; i.p.; once daily for 3 days) leads to increased levels of phosphorylated PERK and NRF2 in brain homogenates. P301S transgenic mice treated with CCT020312 (2 mg/kg; i.p.; once daily for 6 weeks) performes significantly better in Morris water maze. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；In solvent -80°C 6 months
参考文献	[1]. Stockwell SR, et al.Mechanism-based screen for G1/S checkpoint activators identifies a selective activator of EIF2AK3/PERK signalling. PLoS One. 2012;7(1):e28568. [2]. Bruch J, et al. PERK activation mitigates tau pathology in vitro and in vivo. EMBO Mol Med. 2017 Mar;9(3):371-384.

溶解度数据	In Vitro: DMSO : 100 mg/mL (153.75 mM; Need ultrasonic)配制储备液

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[1]. Stockwell SR, et al.Mechanism-based screen for G1/S checkpoint activators identifies a selective activator of EIF2AK3/PERK signalling. PLoS One. 2012;7(1):e28568.
[2]. Bruch J, et al. PERK activation mitigates tau pathology in vitro and in vivo. EMBO Mol Med. 2017 Mar;9(3):371-384.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

CCT020312

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