Merck

N6287

Sigma-Aldrich

核蛋白-3

≥98% (HPLC), powder

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别名:
(±)-4-[4,5-双(4-氯苯基)-2-(2-异丙氧-4-甲氧基-苯基)-4,5-二氢-咪唑-1-羰基]-哌嗪-2-酮
Empirical Formula (Hill Notation):
C30H30Cl2N4O4
分子量:
581.49
MDL编号:
PubChem化学物质编号:
NACRES:
NA.77

质量水平

检测方案

≥98% (HPLC)

形式

powder

reaction suitability

reagent type: ligand

溶解性

DMSO: 20 mg/mL
H2O: insoluble

创始人

Roche

运输

wet ice

储存温度

−20°C

SMILES string

O=C(N1CC(NCC1)=O)N2C(C3=CC=C(Cl)C=C3)C(C4=CC=C(Cl)C=C4)N=C2C5=C(OC(C)C)C=C(OC)C=C5

InChI

1S/C30H30Cl2N4O4/c1-18(2)40-25-16-23(39-3)12-13-24(25)29-34-27(19-4-8-21(31)9-5-19)28(20-6-10-22(32)11-7-20)36(29)30(38)35-15-14-33-26(37)17-35/h4-13,16,18,27-28H,14-15,17H2,1-3H3,(H,33,37)/t27-,28+/m1/s1

InChI key

BDUHCSBCVGXTJM-IZLXSDGUSA-N

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此商品
SML0580SML3406N6664
Nutlin-3 ≥98% (HPLC), powder

Sigma-Aldrich

N6287

核蛋白-3

Nutlin-3a ≥98% (HPLC)

Sigma-Aldrich

SML0580

Nutlin-3a

Nutlin-3b ≥98% (HPLC)

Sigma-Aldrich

SML3406

Nutlin-3b

Neurodazine ≥98% (HPLC)

Sigma-Aldrich

N6664

神经连氮

form

powder

form

powder

form

powder

form

powder

solubility

DMSO: 20 mg/mL, H2O: insoluble

solubility

DMSO: 5 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: >20 mg/mL

originator

Roche

originator

-

originator

-

originator

-

shipped in

wet ice

shipped in

wet ice

shipped in

-

shipped in

-

storage temp.

−20°C

storage temp.

−20°C

storage temp.

−20°C

storage temp.

−20°C

应用

Nutlin-3可用于:
  • 作为刺激 p53 基因的药物,用于基因转移实验
  • 注入蠕虫,验证翻译控制肿瘤蛋白(TCTP)对后截肢蠕虫EEugeniae的一般作用作为的一般作用
  • 作为 p53 基因激活剂用于循环疗法研究
  • 作为 mdm2 抑制剂,研究其对 p53 基因水平、裂解胱天蛋白酶 3和P聚(ADP-核糖)聚合酶(PARP)裂解的作用

生化/生理作用

Nutlin-3是小鼠双微体基因2人同源基因(HDM2)的拮抗剂,具有抑制 HDM2 介导 p53 基因降解的能力。Nutlin-3 还可以增强 p73 基因的转录活性。
Nutlin-3 是 Mdm2(小鼠双微体 2)拮抗剂、p53 通路激活剂和凋亡诱导剂。

特点和优势

该化合物由 Roche 开发。要浏览其他制药公司开发的化合物列表批准的药物/候选药物的列表, 点击这里
这种化合物是细胞凋亡研究的特色产品。点击此处发现更多特色细胞凋亡产品。在sigma.com/discover-bsm可了解更多关于生物活性小分子的其他研究领域。

其他说明

相对立体化学; (4R,5S)和(4S,5R)对映异构体的外消旋混合物。

分析说明

相对立体化学

法律信息

经 Hoffman-La Roche,Inc 许可销售,美国专利 6,734,302。

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

dust mask type N95 (US), Eyeshields, Gloves


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HDM2 antagonist Nutlin-3 disrupts p73-HDM2 binding and enhances p73 function
Lau LMS, et al.
Oncogene, 27(7), 997-997 (2008)
A Quintás-Cardama et al.
Leukemia, 31(6), 1296-1305 (2016-11-26)
TP53 mutations are associated with the lowest survival rates in acute myeloid leukemia (AML). In addition to mutations, loss of p53 function can arise via aberrant expression of proteins that regulate p53 stability and function. We examined a large AML
Nutlin-3 enhances the bortezomib sensitivity of p53-defective cancer cells by inducing paraptosis
Lee DM, et al.
Experimental & Molecular Medicine, 49(8), e365-e365 (2017)
Amine Bouafia et al.
PLoS genetics, 10(5), e1004309-e1004309 (2014-05-17)
Genomic instability is a major hallmark of cancer. To maintain genomic integrity, cells are equipped with dedicated sensors to monitor DNA repair or to force damaged cells into death programs. The tumor suppressor p53 is central in this process. Here
Activation of endogenous p53 by combined p19Arf gene transfer and nutlin-3 drug treatment modalities in the murine cell lines B16 and C6
Merkel CA, et al.
BMC Cancer, 10(1), 316-316 (2010)

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Apoptosis, or programmed cell death (PCD), is a selective process for the removal of unnecessary, infected or transformed cells in various biological systems. As it plays a role in the homeostasis of multicellular organisms, apoptosis is tightly regulated through two principal pathways by a number of regulatory and effector molecules.

n proliferating cells, the cell cycle consists of four phases. Gap 1 (G1) is the interval between mitosis and DNA replication that is characterized by cell growth. Replication of DNA occurs during the synthesis (S) phase, which is followed by a second gap phase (G2) during which growth and preparation for cell division occurs. Together, these three stages comprise the interphase phase of the cell cycle. Interphase is followed by the mitotic (M) phase.

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