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MDM-2, p53

 Activation of the p53 protein protects the organism against the propagation of cells that carry damaged DNA with potentially oncogenic mutations. MDM2, a p53-specific E3 ubiquitin ligase, is the principal cellular antagonist of p53, acting to limit the p53 growth-suppressive function in unstressed cells. In unstressed cells, MDM2 constantly monoubiquitinates p53 and thus is the critical step in mediating its degradation by nuclear and cytoplasmic proteasomes. The interaction between p53 and MDM2 is conformation-based and is tightly regulated on multiple levels. Disruption of the p53-MDM2 complex by multiple routes is the pivotal event for p53 activation, leading to p53 induction and its biological response. Because the p53-MDM2 interaction is structurally and biologically well understood, the design of small lipophilic molecules that disrupt or prevent it has become an important target for cancer therapy. 

MDM-2, p53 (28)
产品名称 目录号 简述
AMG 232 HY-12296

AMG 232 is a highly potent, selective and orally bioavailable piperidinone inhibitor of the MDM2-p53 interaction((SPR KD= 0.045 nM, SJSA-1 EdU IC50=9.1 nM).

Kevetrin hydrochloride HY-16271

Kevetrin hydrochloride is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.

MI-773 HY-17493

MI-773 是人双微体2(HDM2)口服拮抗剂,有抗肿瘤活性。

MX69 HY-100892

MX69 is the MDM2/XIAP inhibitor, used for cancer treatment.

NSC319726 HY-18634

NSC319726是突变型p53R175再活化剂,能抑制表达p53R175的成纤维细胞增殖,IC50值为8nM,对野生型p53细胞无抑制作用。

NSC59984 HY-19726

NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway.

Nutlin 3 HY-50696

Nutlin-3是MDM2拮抗剂,能抑制MDM2和p53的相互作用,IC50为90nM,并激活p53。

Nutlin 3a HY-10029

Nutlin-3是MDM2拮抗剂,能抑制MDM2和p53的相互作用,IC50为90nM,并激活p53。

Nutlin 3b HY-15335

Nutlin-3b是MDM2/p53抑制剂,IC50为13.6 _mu_M。

NVP-CGM097 HY-15954

NVP-CGM097(CGM-097)能阻断P53与MDM2相互结合,具有抗肿瘤活性。

NVP-CGM097 sulfate HY-15954B

NVP-CGM097 sulfate is a potent and selective MDM2 inhibitor with IC50 of 1.7±0.1 nM for hMDM2.

p53 and MDM2 proteins-interaction-inhibitor chiral HY-70027

手性p53 and MDM2 proteins-interaction-inhibitor是p53和MDM2相互作用的抑制剂。

p53 and MDM2 proteins-interaction-inhibitor dihydrochloride HY-70027A

p53 and MDM2 proteins-interaction-inhibitor双盐酸盐是p53与MDM2相互作用抑制剂。

p53 and MDM2 proteins-interaction-inhibitor racemic HY-70028

外消旋p53 and MDM2 proteins-interaction-inhibitor是p53与MDM2相互作用抑制剂。

Pifithrin-α hydrobromide HY-15484

Pifithrin-_alpha_是p53抑制剂,能抑制p53依赖的p53应答基因反式激活。

Pifithrin-β HY-16702

Pifithrin-_beta_)(Cyclic Pifithrin-_alpha_)是p53蛋白的有效抑制剂,在宫颈癌细胞株IGROV-1中的IC50值为23uM。

Pifithrin-β hydrobromide HY-16702A

Pifithrin-_beta_) HBr(Cyclic Pifithrin-_alpha_ HBr)是p53蛋白的有效抑制剂,在宫颈癌细胞株IGROV-1中的IC50值为23uM。

PRIMA-1 HY-19980A

PRIMA-1 is a mutant p53 reactivator, restores the sensitivity of TP53 mutant-type thyroid cancer cells to the histone methylation inhibitor 3-Deazaneplanocin A.

RG7112 HY-10959

RG7112是第一个进入临床的MDM2抑制剂,能占据MDM2上与p53结合的活性口袋。

RG7388 HY-15676

RG7388是口服的MDM2拮抗剂,能抑制MDM2与p53的结合。

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