p53
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S2929 | Pifithrin-α (PFTα) HBr | <1 mg/mL | 67 mg/mL | <1 mg/mL |
| S5791 | Cyclic Pifithrin-α hydrobromide | <1 mg/mL | 27 mg/mL | 3 mg/mL |
| S9235 | Didymin | 100 mg/mL | ||
| S2930 | Pifithrin-μ | <1 mg/mL | 36 mg/mL | 36 mg/mL |
| S8149 | NSC348884 | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S8187 | ReACp53 | 100 mg/mL | -1 mg/mL | -1 mg/mL |
| S1172 | JNJ-26854165 (Serdemetan) | <1 mg/mL | 66 mg/mL | 2 mg/mL |
| S2678 | NSC 207895 | <1 mg/mL | 0.4 mg/mL | <1 mg/mL |
| S2781 | RITA (NSC 652287) | <1 mg/mL | 58 mg/mL | 8 mg/mL |
| S8000 | Tenovin-1 | <1 mg/mL | 74 mg/mL | <1 mg/mL |
| S5811 | Kevetrin hydrochloride | 36 mg/mL | 36 mg/mL | 21 mg/mL |
| S8728 | PK11007 | 47 mg/mL | 47 mg/mL | 23 mg/mL |
| S7149 | NSC 319726 | <1 mg/mL | 19 mg/mL | <1 mg/mL |
| S8580 | COTI-2 | <1 mg/mL | 73 mg/mL | <1 mg/mL |
| S7649 | MI-773 (SAR405838) | <1 mg/mL | 100 mg/mL | 31 mg/mL |
| S4900 | Tenovin-6 | 98 mg/mL | 98 mg/mL | <1 mg/mL |
| S7724 | APR-246 (PRIMA-1MET) | 40 mg/mL | ||
| S8106 | NSC59984 | <1 mg/mL | 53 mg/mL | 53 mg/mL |
| S8483 | CBL0137 (CBL-0137) | 24 mg/mL | 38 mg/mL | <1 mg/mL |
| S7723 | PRIMA-1 | 37 mg/mL | 37 mg/mL | 37 mg/mL |
| S2341 | (-)-Parthenolide | <1 mg/mL | 49 mg/mL | 49 mg/mL |
- p53抑制剂（21）
- 新p53产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2929 |
Pifithrin-α (PFTα) HBrPifithrin-α (PFTα)是一种p53抑制剂，抑制p53依赖性的p53应答基因转录。 |
(C) Cell viability was measured after TSA and PFTα co-treatment. MG63 were exposed to TSA and various concentrations of PFTα (1, 5, 10μM) co-treatment compared with TSA treatment alone for 24h. Data are presented as means ± S.E.M. from 3 independent experiments. *, P < 0.05 vs. MG63 cells without TSA or PFTα treatment; **, P < 0.01 vs. MG 63 cells without TSA or PFTα treatment; &&, P < 0.01 vs. MG63 cells with TSA treatment alone. (D) Flow cytometry analysis of ANXA5 and propidiumiodide staining of MG63 cells with TSA and various concentrations of PFTα (1, 5, 10μM) co-treatment, compared with TSA treatment alone.
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| S5791New |
Cyclic Pifithrin-α hydrobromideCyclic Pifithrin-α hydrobromide是Cyclic Pifithrin-α的氢溴酸盐形式，cyclic Pifithrin-α是p53的转录抑制剂。 |
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| S9235New |
DidyminDidymin is a citrus-derived natural compound that kills p53 wild-type as well as drug-resistant p53-mutant neuroblastoma cells in culture. It possesses antioxidant, anti-inflammation and anti-cancer properties. |
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| S2930 |
Pifithrin-μPifithrin-μ是一种特异性的p53抑制剂，通过降低其与Bcl-xL和Bcl-2的亲和力而发挥作用，也抑制HSP70功能和细胞自噬。 |
Effect of pifithrin-μ (the inhibitor of mitochondrial translocation of p53) on MEG3-induced apoptosis in TGF-β1-treated LX-2 cells. The inhibitor pifithrin-μ attenuated cleavage of caspase 3 which blocked apoptosis. The results are expressed as relative expression against control expression without treatment.
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| S8149 |
NSC348884NSC348884是核仁磷酸蛋白抑制剂。在多种肿瘤细胞系中，抑制细胞增殖以及诱导凋亡。IC50为1.4-4 μM。 |
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| S8187 |
ReACp53ReACp53是可穿透细胞的肽段，抑制p53淀粉体的形成，在癌细胞株和来源于HGSOC的细胞器中实现p53功能的再利用。 |
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| S1172 |
JNJ-26854165 (Serdemetan)JNJ-26854165 (Serdemetan)是一种HDM2泛素连接酶拮抗剂，作用于p53野生型细胞，诱导早期凋亡，在缺乏功能性p53的细胞中，抑制细胞增殖而延迟细胞凋亡。 |
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| S2678 |
NSC 207895NSC 207895抑制MDMX，IC50为2.5 μM，促进p53稳定/激活和DNA损伤，也调节MDM2（E3连接酶）。 |
Median overall survival of mice (n = 5 mice in vehicle and PYR-41; n = 4 mice in NSC group) inoculated with IOWA-1T xenografts were increased to 43 ± 0.5 and 39 ± 2 days with PYR-41 (PYR) and NSC-207895 (NSC), respectively, compared with a vehicle-treated control group 33 ± 1 days (*p < 0.05).
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| S2781 |
RITA (NSC 652287)RITA (NSC 652287)诱导DNA-蛋白质和DNA-DNA交联，检测不到DNA单链断裂，通过靶向作用于p53，也抑制MDM2-p53相互作用。 |
To determine the number of viable cells, cells were serum starved for 8 hours and treated with 25 nM RITA and stimulated with 1ug/mL SDF1α for 48 hours in serum-free media. After 48 hours, cells were harvested and counted by trypan blue exclusion, using standard methods.
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| S8000 |
Tenovin-1Tenovin-1防止MDM2介导的p53的降解，涉及泛素化途径，通过抑制SirT1和SirT2的蛋白脱乙酰活性。 |
The SIRT1 inhibitor (tenovin-1) partially blocked the protective effect of γ-man in L02 cells. The effect of tenovin-1 on expression and acetylation level of PGC-1α (B) in L02 cells treated with or without γ-man.
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| S5811New |
Kevetrin hydrochlorideKevetrin hydrochloride是水溶性的p53激活剂，具有潜在的抗肿瘤活性。 |
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| S8728New |
PK11007PK11007是一种抗p53化合物，能够稳定野生型和突变型p53。它不仅能通过重新激活p53发挥抗肿瘤活性，还能通过其他细胞机制，如增强细胞内ROS水平、激活UPR来抵御肿瘤。 |
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| S7149 |
NSC 319726NSC 319726是一种p53(R175)突变型活化剂，抑制表达突变型p53的细胞生长，作用于p53(R175)突变型，IC50为8 nM，对p53野生型细胞没有抑制作用。 |
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| S8580 |
COTI-2COTI-2是一种具有口服活性的第三代胺苯硫脲，是突变型p53的激活剂，具有潜在的抗肿瘤活性。 |
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| S7649 |
MI-773 (SAR405838)MI-773 (SAR405838) 是一种口服生物有效的MDM2拮抗剂，Ki为0.88 nM。Phase 1。 |
A panel of four NB cell lines were seeded in six-well plates with indicated concentrations of SAR405838 and agar, and grown for 2 to 3 weeks. Cells were stained with crystal violet for 4 hours. Colonies were counted and colony numbers were represented as % vehicle ± S.D. with P < 0.05 (*), P < 0.01 (**) or P < 0.001 (***) (Student's t-test, two-tailed) as indicated.
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| S4900 |
Tenovin-6Tenovin-6是p53转录活性的小分子激活剂。 |
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| S7724 |
APR-246 (PRIMA-1MET)APR-246，又名PRIMA-1MET， 是一种小分子有机化合物，可以恢复肿瘤抑制功能，主要靶向突变型p53，在多种癌细胞类型中诱导细胞死亡。 |
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| S8106 |
NSC59984NSC59984是一种p53通路激活剂，通过诱导突变型 p53 蛋白质降解和 p73 激活发挥作用。 |
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| S8483 |
CBL0137 (CBL-0137)CBL0137(CBL-0137)激活p53并抑制NF-kB，在细胞实验中，IC50分别为0.37 μM 和 0.47 μM。它还能抑制组蛋白分子伴侣FACT，FACT促进染色质转录复合体的形成。 |
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| S7723 |
PRIMA-1PRIMA-1是p53突变体的重活化剂。在携带p53突变的人类肿瘤中，引起细胞凋亡并抑制肿瘤生长。 |
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| S2341 |
(-)-Parthenolide(-)-Parthenolide, Nuclear Factor-κB抑制剂，可特异性地耗尽HDAC1蛋白，而不影响其他I/II类 HDACs。促进MDM2的泛素化并激活p53的细胞功能。 |
-Parthenolide-S234101W0220161110.gif)
-Parthenolide-S234101W0220161110.gif)
G. To evaluate effects of IKBKE/TBK1 inhibition on NF-κB signaling in Ewing, TC32 cells were incubated with CYT387 for six hours prior to stimulation with TNF-α (30 ng/mL). IκBα degradation was measured by harvesting TC32 cells thirty minutes after stimulation with TNF-α. TNF-α stimulation resulted in degradation of IκBα, and this effect was attenuated with CYT387 treatment. Parthenolide, an inhibitor of IκBα phosphorylation was used as a positive control. Similar effects of CYT387 activity were seen in HEK-293T cells which also express IKBKΕ. Nuclear extracts were prepared from TC32 cells harvested following forty-five minutes of TNF-α stimulation. Treatment with CYT387 resulted in decreased nuclear localization of NF-κB family proteins RelA/p65 and c-Rel. There was a modest impairment of p50 nuclear localization as compared to parthenolide and DMSO controls and no change in p52 nuclear localization. RelB (not shown) is not expressed in TC32 cells |
