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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PERK-CCT020312
CCT020312

Chemical Structure : CCT020312

CAS No.: 324759-76-4

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CCT020312 (CCT-020312;CCT 020312)

货号: PC-35976Not For Human Use, Lab Use Only.

CCT020312 (CCT-020312) is a small molecule PERK activator, inhibits pRB phosphorylation in HT29 colon carcinoma cells with EC50 of 5.1 uM.

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5 mg ￥1580 In stock
10 mg ￥2480 In stock
25 mg ￥3980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CCT020312 (CCT-020312) is a small molecule PERK activator, inhibits pRB phosphorylation in HT29 colon carcinoma cells with EC50 of 5.1 uM.
CCT020312 shows no effect on the activity on CDK4/cyclin D or CDK1/cyclin B, effectively inhibits cell proliferation of HT29 colon carcinoma cells with IC50 of 3.1 uM (96 h).
CCT020312 elicits EIF2A phosphorylation in cells, does not induce full ER stress signalling; also reduced tau phosphorylation, tau conformational change and 4-repeat tau isoforms, and increased cell viability in cultured human neurons.
CCT020312  significantly improved memory and locomotor function, reduced tau pathology, and prevented dendritic spine and motoneuron loss in P301S tau mice.

物理化学性质&存储条件

分子量 650.415
分子式 C31H30Br2N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

6-Bromo-3-[5-(4-bromo-phenyl)-1-(3-diethylamino-propionyl)-4,5-dihydro-1H-pyrazol-3-yl]-4-phenyl-1H-quinolin-2-one

参考文献

1. Stockwell SR, et al. PLoS One. 2012;7(1):e28568. doi: 10.1371/journal.pone.0028568.

2. Bruch J, et al. EMBO Mol Med. 2017 Mar;9(3):371-384.

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