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PhiKan-083
CAS No. 1050480-30-2
PhiKan-083 ( PK-083 )
产品货号. M10244 CAS No. 1050480-30-2
p53 突变体 Y220C 的小分子稳定剂，Kd 为 150 uM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 10MG | ￥5947 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称PhiKan-083
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注意事项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
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产品简述p53 突变体 Y220C 的小分子稳定剂，Kd 为 150 uM。
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产品描述A small-molecule stabilizer of p53 mutant Y220C with Kd of 150 uM; binds with high affinity to a crevice created by the Y220C mutation in p53 and stabilizes the mutant protein.
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体外实验PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM, shows a relative binding affinity (Kd) of 150 μM for p53Y220C in Ln229 cells.PhiKan 083 slows down its thermal denaturation rate.PhiKan 083 (125 μM, 48 hours) reduces the cell viability of engineered variants of Ln229 cells. PhiKan 083 (100 μM) in conbination with NSC 123127 (1 μM) enhances the pro-apoptotic activity in all variants of Ln229 cells (p53wt, p53Y220C, p53G245S, p53R282W). Cell Viability Assay Cell Line:Ln229, Ln229-p53-wt, Ln229-p53-Y220C, Ln229-p53-G245S, Ln229-p53-R282W cells Concentration:125 μM Incubation Time:48 hours Result:Caused ～70 ± 5% reduction in cell viability of variants of Ln229 cells.
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体内实验——
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同义词PK-083
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通路Apoptosis
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靶点MDM2-p53
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受体MDM2-p53
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研究领域——
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适应症——
化学信息
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CAS Number1050480-30-2
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分子量274.792
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分子式C16H18N2.HCl
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纯度>98% (HPLC)
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溶解度H2O : 2 mg/mL7.28 mM
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SMILESCCN1C2=C(C=C(C=C2)CNC)C3=CC=CC=C31.Cl
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化学全称1-(9-ethyl-9H-carbazol-3-yl)-N-methylmethanamine hydrochloride
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Bauer MR, et al. ACS Chem Biol. 2016 Aug 19;11(8):2265-74.
2. Boeckler FM, et al. Proc Natl Acad Sci U S A. 2008 Jul 29;105(30):10360-5.
3. Wiman KG. Oncogene. 2010 Jul 29;29(30):4245-52.
