p53

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抑制剂选择性比较

p53产品

所有产品 p53抑制剂(6) p53激活剂(15) 新p53产品

产品目录	产品描述	文献引用	实验数据
S2929	Pifithrin-α (PFTα) HBr Pifithrin-α (PFTα)是一种p53抑制剂，抑制p53依赖性的p53应答基因转录。	Redox Biol, 2019, 22:101157 Stem Cell Res Ther, 2019, 10(1):123 Cancer Med, 2019, 10.1002/cam4.2393	A, HAECs were per-incubated with PFTα (3 μmol/L) for 60 min followed by transfected with siB-myb or siNC in the presence of PFTα (3 μmol/L) for 7 d. The expression levels of B-myb, p-p53, p53 and p21 proteins were analysed by western blotting. GAPDH was used as a loading control. A typical group of blots is shown from one of three independent experiments.
S5791^New	Cyclic Pifithrin-α hydrobromide Cyclic 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。
S2930	Pifithrin-μ Pifithrin-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。	Front Pharmacol, 2018, 9:92 Oncogene, 2018, 37(8):1041-1048 Int J Mol Med, 2018, 42(4):2089-2097	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.
S9235	Didymin Didymin 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.
S8149	NSC348884 NSC348884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。
S8187	ReACp53 ReACp53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。
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。	Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193 BMC Pharmacol Toxicol, 2017, 18(1):40
S2678	NSC 207895 NSC 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）。	Oncol Lett, 2018, 15(2):1673-1679 Stem Cell Reports, 2016, 7(6):1140-1151	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).
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。	Cancer Cell, 2019, 35(2):191-203 Nat Chem Biol, 2015, 10.1038/nchembio.1986 Oncogene, 2014, 10.1038/onc.2014.37	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.
S8000	Tenovin-1 Tenovin-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。	J Transl Med, 2019, 17(1):76	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.
S5811^New	Kevetrin hydrochloride Kevetrin hydrochloride是水溶性的p53激活剂，具有潜在的抗肿瘤活性。
S7149	NSC 319726 NSC 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。
S8580	COTI-2 COTI-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。
S7649	MI-773 (SAR405838) MI-773 (SAR405838) 是一种口服生物有效的MDM2拮抗剂，K_i为0.88 nM。Phase 1。	Oncotarget, 2016, 7(50):82757-82769	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.
S4900	Tenovin-6 Tenovin-6是p53转录活性的小分子激活剂。	Nat Biotechnol, 2015, 10.1038/nbt.3130
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。
S8106	NSC59984 NSC59984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。
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。
S7723	PRIMA-1 PRIMA-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。
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。	Biochem Biophys Res Commun, 2018, 501(1):246-252 Oncol Rep, 2018, 39(3):1181-1190 J Neuroimmunol, 2017, 305:154-161	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
S8728	PK11007 PK11007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。

产品目录	产品描述	文献引用	实验数据
S2929	Pifithrin-α (PFTα) HBr Pifithrin-α (PFTα)是一种p53抑制剂，抑制p53依赖性的p53应答基因转录。	Redox Biol,2019, 22:101157 Stem Cell Res Ther,2019, 10(1):123 Cancer Med,2019, 10.1002/cam4.2393	A, HAECs were per-incubated with PFTα (3 μmol/L) for 60 min followed by transfected with siB-myb or siNC in the presence of PFTα (3 μmol/L) for 7 d. The expression levels of B-myb, p-p53, p53 and p21 proteins were analysed by western blotting. GAPDH was used as a loading control. A typical group of blots is shown from one of three independent experiments.
S5791^New	Cyclic Pifithrin-α hydrobromide Cyclic 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。
S2930	Pifithrin-μ Pifithrin-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。	Front Pharmacol,2018, 9:92 Oncogene,2018, 37(8):1041-1048 Int J Mol Med,2018, 42(4):2089-2097	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.
S9235	Didymin Didymin 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.
S8149	NSC348884 NSC348884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。
S8187	ReACp53 ReACp53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。

产品目录	产品描述	文献引用	实验数据
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。	Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193 BMC Pharmacol Toxicol, 2017, 18(1):40
S2678	NSC 207895 NSC 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）。	Oncol Lett, 2018, 15(2):1673-1679 Stem Cell Reports, 2016, 7(6):1140-1151	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).
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。	Cancer Cell, 2019, 35(2):191-203 Nat Chem Biol, 2015, 10.1038/nchembio.1986 Oncogene, 2014, 10.1038/onc.2014.37	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.
S8000	Tenovin-1 Tenovin-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。	J Transl Med, 2019, 17(1):76	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.
S5811^New	Kevetrin hydrochloride Kevetrin hydrochloride是水溶性的p53激活剂，具有潜在的抗肿瘤活性。
S7149	NSC 319726 NSC 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。
S8580	COTI-2 COTI-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。
S7649	MI-773 (SAR405838) MI-773 (SAR405838) 是一种口服生物有效的MDM2拮抗剂，K_i为0.88 nM。Phase 1。	Oncotarget, 2016, 7(50):82757-82769	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.
S4900	Tenovin-6 Tenovin-6是p53转录活性的小分子激活剂。	Nat Biotechnol, 2015, 10.1038/nbt.3130
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。
S8106	NSC59984 NSC59984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。
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。
S7723	PRIMA-1 PRIMA-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。
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。	Biochem Biophys Res Commun, 2018, 501(1):246-252 Oncol Rep, 2018, 39(3):1181-1190 J Neuroimmunol, 2017, 305:154-161	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
S8728	PK11007 PK11007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。

研究领域

产品类型

p53

信号通路图

研究领域

抑制剂选择性比较

p53产品