2. Apoptosis Metabolic Enzyme/Protease Autophagy
  3. Autophagy MDM-2/p53 Apoptosis E1/E2/E3 Enzyme
  4. (Rac)-Nutlin-3

(Rac)-Nutlin-3  (Synonyms: (Rac)-Rebemadlin)

目录号: HY-10029A
产品使用指南

摩尔计算器

(Rac)-Nutlin-3 (Rebemadlin) 是 Nutlin-3 的活性对映体，是一种有效的 MDM2 抑制剂。(Rac)-Nutlin-3 可抑制 MDM2-p53 相互作用，稳定 p53 蛋白，从而诱导细胞自噬 (autophagy) 和凋亡 (apoptosis)。(Rac)-Nutlin-3 有潜力用于 TP53 野生型卵巢癌的研究。

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(Rac)-Nutlin-3 Chemical Structure

(Rac)-Nutlin-3 Chemical Structure

CAS No. : 890090-75-2

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Other Forms of (Rac)-Nutlin-3:

(Rac)-Nutlin-3 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

(Rac)-Nutlin-3 (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). (Rac)-Nutlin-3 inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. (Rac)-Nutlin-3 has the potential for the study of TP53 wild-type ovarian carcinomas[1][2].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.41 μM
Compound: Nutlin-3
Cytotoxicity against human A549 cells after 72 hrs by SRB assay
Cytotoxicity against human A549 cells after 72 hrs by SRB assay
10.1039/C2MD20208E
HCT-116 IC50
4.63 μM
Compound: Nutlin-3
Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay
Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay
10.1039/C2MD20208E
MCF7 IC50
14.63 μM
Compound: Nutlin-3
Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 48 hrs by CCK8 assay
[PMID: 33725632]
MCF7 IC50
15.72 μM
Compound: Nutlin-3
Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 48 hrs in presence of Fer-1 by CCK8 assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 48 hrs in presence of Fer-1 by CCK8 assay
[PMID: 33725632]
MDA-MB-231 IC50
28.47 μM
Compound: nutlin-3
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay
[PMID: 36512711]
PC-3 IC50
6.37 μM
Compound: Nutlin-3
Cytotoxicity against human PC3 cells after 72 hrs by SRB assay
Cytotoxicity against human PC3 cells after 72 hrs by SRB assay
10.1039/C2MD20208E
SJSA-1 IC50
1.81 μM
Compound: Nutlin-3
Cytotoxicity against human SJSA1 cells after 72 hrs by SRB assay
Cytotoxicity against human SJSA1 cells after 72 hrs by SRB assay
10.1039/C2MD20208E
SW-620 IC50
0.38 μM
Compound: Nutlin-3
Cytotoxicity against human SW620 cells after 72 hrs by SRB assay
Cytotoxicity against human SW620 cells after 72 hrs by SRB assay
10.1039/C2MD20208E
U-87MG ATCC IC50
104.5 nM
Compound: 2
Binding affinity to MDM2 in human U87MG cells assessed as inhibition of MDM2/p53 protein interaction after 10 mins by quantitative sandwich immuno assay
Binding affinity to MDM2 in human U87MG cells assessed as inhibition of MDM2/p53 protein interaction after 10 mins by quantitative sandwich immuno assay
[PMID: 27050782]
U-87MG ATCC IC50
6.5 μM
Compound: 2
Antiproliferative activity against human U87MG cells expressing wild type p53 after 48 hrs by MTS assay
Antiproliferative activity against human U87MG cells expressing wild type p53 after 48 hrs by MTS assay
[PMID: 27050782]
体外研究
(In Vitro)

Nutlin-3a 是一种抑制 MDM2、激活野生型 p53 并诱导细胞凋亡的治疗剂，作为 TP53 野生型卵巢癌的抑制剂。具有野生型 TP53 的三种细胞系（HOC-7、OVCA429 和 A2780）对 Nutlin-3a 高度敏感（IC50=4-6 μM）。SKOV3 细胞对 Nutlin-3a 的 IC50 为 38 μM。其余两个卵巢透明细胞系（TOV21G 和 OVAS）均具有 TP53 野生型，对 Nutlin-3a 的生长抑制相对更敏感（IC50=14 和 25 μm）比 TP53 突变细胞系[1]。Nutlin-3a 是 Nutlin-3 的活性对映体。Nutlin-3a 是一种高度选择性的 MDM2 拮抗剂和 p53 诱导剂。与 10 μM Nutlin-3a 一起孵育 7 天，可抑制 NIH/3T3 细胞生长 90% 以上，但不影响 MEF 的增殖，其中药物的两个靶标均被消除。Nutlin-3a 可有效阻止所有细胞系的细胞周期进展，将 S 期间隔减少至 0.2-2%，并增加 G1- 和 G2/M 期，表明 G1 和 G2 停滞。添加 Nutlin-3a 后 3 小时，p53 靶标 p21 和 MDM2 显着升高，并在 8 小时时达到最高水平。40 小时后，Nutlin-3a 诱导约 60% 的 SJSA-1 和 MHM 细胞凋亡，60 小时后进一步增加（分别为 85% 和 65%）[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

(Rac)-Nutlin-3 相关抗体:
体内研究
(In Vivo)

Nutlin-3a 在所有模型中均有效，平均肿瘤生长抑制≥98%。Nutlin-3a 以剂量依赖性方式抑制异种移植物生长，最高剂量 (200 mg/kg) 显示肿瘤显着缩小（8 个部分消退和 1 个完全消退）。使用 Nutlin-3a 建立的 SJSA-1 和 MHM 骨肉瘤异种移植物可导致肿瘤广泛消退[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

581.49

Formula

C30H30Cl2N4O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

(Rac)-Nutlin-3 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(Rac)-Nutlin-3890090-75-2(Rac)-RebemadlinAutophagyMDM-2/p53ApoptosisE1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseInhibitorinhibitorinhibit

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