Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T72026 |
p53-MDM2-IN-1
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Mdm2; p53 | Apoptosis |
p53-MDM2-IN-1 (Example 30) 是一种 p53-MDM2/X 蛋白相互作用的抑制剂,Ki 值为 23.35 µM。p53-MDM2-IN-1 能用于抗肿瘤研究。 | |||
T14303 |
Alrizomadlin
APG-115,AA-115 |
Mdm2 | Apoptosis |
Alrizomadlin (APG-115) 是一种具有口服活性的 MDM2 抑制剂,IC50 为 3.8 nM,Ki 分别为 1 nM[1]。 Alrizomadlin 阻断 MDM2 和 p53 的相互作用,并以 p53 依赖性方式诱导细胞周期停滞和细胞凋亡。 | |||
T11982 |
MDM2-IN-1
|
Others | Others |
MDM2-IN-1 is a synthetic MDM2-p53 interaction (MDM2) inhibitor and contains the trans (D-)configuration. | |||
T26610 |
AM-6761
AM 6761,AM6761 |
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AM-6761 is a potent inhibitor of the MDM2-p53 interaction. In the SJSA-1 osteosarcoma xenograft model, AM-6761 shows excellent antitumor activity with an ED50 of 11 mg/kg. | |||
T73895 | MI-1061 TFA | ||
MI-1061 TFA 是一种有效、口服生物可用、化学稳定性高的MDM2(MDM2-p53 互作) 抑制剂,具有低纳摩尔级别的抑制活性(IC50=4.4 nM;Ki=0.16 nM)。它能在小鼠SJSA-1 异种移植瘤组织中激活p53并诱导凋亡,展现出抗肿瘤活性。 | |||
T74936 | MDM2/4-p53-IN-3 | ||
MDM2/4-p53-IN-3,一种针对MDM2/4-p53蛋白-蛋白相互作用(PPI)的抑制剂,IC50s分别为18.5 nM(MDM2-p53)与14.8 nM(MDM4-p53)。该化合物主要应用于癌症研究领域,特别是结肠癌的研究。 | |||
T74935 | MDM2/4-p53-IN-2 | ||
MDM2/4-p53-IN-2 (2q) 是一种有效的双重 MDM2/ MDM4抑制剂和 p53激活剂,作用于 MDM2-p53 和 MDM4-p53 复合物的 IC50值分别是 70.7 nM 和 81.4 nM。MDM2/4-p53-IN-2 可以调控细胞周期,诱导细胞凋亡(apoptosis),具有抗癌活性。 | |||
T28108 |
MRT80
MRT-80,MRT00055778,MRT 80 |
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MRT80 is an inhibitor of GSK-3 in vitro. MRT80 de-stabilizes MDM2 and stabilizes p53 protein and E2F-1. | |||
T78699 |
MDMX/MDM2-IN-2
|
||
MDMX/MDM2-IN-2 是一款p53-MDM2/MDMX双重抑制剂,具有高效性,其对MDM2和MDMX的Ki值分别为0.23 μM和2.45 μM。该化合物阻断p53与MDM2蛋白的相互作用,从而恢复p53功能,诱导细胞周期停滞与细胞凋亡。同时,MDMX/MDM2-IN-2抑制细胞迁移和侵袭,显示出潜在的抗肿瘤活性。 | |||
T79483 | MDM2/XIAP-IN-3 | ||
MDM2/XIAP-IN-3(化合物 3e)为MDM2/XIAP双重抑制剂,能够下调MDM2与XIAP蛋白水平,提升p53表达,进而抑制癌细胞增殖并诱导细胞凋亡。 | |||
T78166 |
MEL24
|
Others | Others |
MEL24为Mdm2 E3连接酶抑制剂,通过p53依赖机制降低细胞存活率,增强对DNA损伤剂的敏感性,适用于体外抗肿瘤研究。 | |||
T14554 |
BI-0252
|
Others | Others |
BI-0252 is an inhibitor of MDM2-p53 (IC50:4 nM). BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft. And it concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis. | |||
T61116 |
NSC405640
|
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NSC405640 is a highly effective compound that inhibits the interaction between MDM2 and p53 proteins. Furthermore, it can restore the structural integrity of p53 molecules affected by mutations. Notably, NSC405640 exhibits selectivity in inhibiting the growth of cell lines that possess the normal, unmutated form of the p53 protein [1]. | |||
T60478 |
BTX161
|
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BTX161 是沙利度胺类似物。BTX161是有效的 CKIα降解剂。在人类 AML 细胞中,BTX161 比来那度胺更好地介导 CKIα 降解,激活 DNA 损伤反应 (DDR) 和 p53,并能稳定 p53 拮抗剂 MDM2。 | |||
T36464 |
Caylin-1
|
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Nutlin-3 is an activator of p53 that functions by inhibiting the interaction of p53 with MDM2, a negative regulator of p53 activity. Caylin-1 is a nutlin-3 analog which contains chlorine substituents at the 3 and 4 positions on two of the phenyl rings rather than a single 4-chloro as seen in nutlin-3. At high concentrations, caylin-1 inhibits the growth of HCT116 cells with an IC50 value of approximately 7 μM, making it about 7-fold less potent than nutlin-3 in the same assay. Interestingly, at ... |