p53

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研究领域

抑制剂选择性比较

p53产品

所有产品 p53抑制剂(9) p53激活剂(15)

目录号	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。Pifithrin-α也是一种有效的 aryl hydrocarbon receptor (AhR) 的兴奋剂。	Cancers (Basel), 2020, 20;12(2) pii: E493 J Steroid Biochem Mol Biol, 2020, 198:105537 J Biol Chem, 2020, 27;295(13):4237-4251	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.
S8059	Nutlin-3a Nutlin-3a 是Nutlin-3的活性对映体，抑制p53/MDM2相互作用，无细胞试验中IC50为90 nM。Nutlin-3a 可诱导p53依赖的自噬和细胞凋亡。	Oncogenesis, 2020, 1;9(5):57 Cell Discov, 2020, 21;6:21 Cell Stem Cell, 2019, 25(2):258-272	Nutlin-3a preserved p53 expression without influencing high glucose (HG)-induced podocyte impairment. A-D: cultured podocytes were pre-treated by nutlin-3a for 2 hrs before subjected to HG treatment. Western blotting gel documents (A) and summarized data (B) showing the expression of p53 and MDM2 in podocytes under HG exposure for 24 hrs. n = 4. Western blotting gel documents (C) and summarized data (D) showing the expression of Desmin in podocytes under HG exposure for 24 hrs. n = 3. *P < 0.05 vs. Ctrl, #P < 0.05 vs. Vehl + HG. Ctrl: control; Vehl: vehicle; nutlin-3a: nutlin-3a treatment.
S2176^New	Tenovin-3 Tenovin-3 是一种 SIRT2 的抑制剂。Tenovin-3 能够增加MCF-7细胞中的 p53 的水平。
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。	Radiat Res, 2020, 193(2):119-129 Theranostics, 2019, 9(2):554-572 Front Pharmacol, 2018, 9:92	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.
S7030	RG-7112 RG7112 (RO5045337)是一种口服具有活性的选择性p53-MDM2抑制剂，HTRF IC50为18 nM。	Eur J Cancer, 2020, 126:93-103 Nat Commun, 2019, 10(1):2189 Cancer Biother Radiopharm, 2019, 34(4):252-257
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.
S5791	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。
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。	Nat Commun, 2020, 3;11(1):1669 Cell Death Dis, 2019, 10(11):831
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）。	Genes Dev, 2020, 34(7-8):526-543 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 Br J Cancer, 2018, 119(4):450-461 Radiol Oncol, 2016, 50(2):168-74	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.
S2427^New	Triglycidyl Isocyanurate (Teroxirone) Triglycidyl Isocyanurate 又名 Teroxirone 是具有抗肿瘤活性的三氮杂三环氧化物。它通过激活 p53 抑制人非小细胞肺癌细胞的生长。Triglycidyl Isocyanurate 可以通过烷基化并交联DNA来抑制 DNA replication。Triglycidyl Isocyanurate 还用于金属精加工行业的各种聚酯粉末涂料中。
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 Int J Mol Med, 2019, 44(3):1091-1105	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.
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。	Cell Chem Biol, 2018, 25(5):585-594
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。	EMBO J, 2019, 38(20):e102096 Cell Chem Biol, 2018, 25(6):761-774 Oncotarget, 2017, 8(26):43008-43022	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。	Biomed Pharmacother, 2020, 125:109948 J Cell Sci, 2019, 132(6) 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。
S5811	Kevetrin hydrochloride Kevetrin hydrochloride是水溶性的p53激活剂，具有潜在的抗肿瘤活性。
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。	Micromachines (Basel), 2020, 11(2)
S8483	CBL0137 HCl (CBL-0137 HCl) 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。	Mol Cell, 2020, S1097-2765(20)30193-3
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。	J Biol Chem, 2020, 295(11):3576-3589 G3 (Bethesda), 2020, 4;10(5):1585-1597 Br J Haematol, 2019, 187(1):49-64	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	PK11000 PK11000通过共价半胱氨酸修饰稳定野生型和突变型p53的DBD，而又不影响DNA结合，并且能有效诱导细胞死亡。

目录号	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。Pifithrin-α也是一种有效的 aryl hydrocarbon receptor (AhR) 的兴奋剂。	Cancers (Basel),2020, 20;12(2) pii: E493 J Steroid Biochem Mol Biol,2020, 198:105537 J Biol Chem,2020, 27;295(13):4237-4251	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.
S8059	Nutlin-3a Nutlin-3a 是Nutlin-3的活性对映体，抑制p53/MDM2相互作用，无细胞试验中IC50为90 nM。Nutlin-3a 可诱导p53依赖的自噬和细胞凋亡。	Oncogenesis,2020, 1;9(5):57 Cell Discov,2020, 21;6:21 Cell Stem Cell,2019, 25(2):258-272	Nutlin-3a preserved p53 expression without influencing high glucose (HG)-induced podocyte impairment. A-D: cultured podocytes were pre-treated by nutlin-3a for 2 hrs before subjected to HG treatment. Western blotting gel documents (A) and summarized data (B) showing the expression of p53 and MDM2 in podocytes under HG exposure for 24 hrs. n = 4. Western blotting gel documents (C) and summarized data (D) showing the expression of Desmin in podocytes under HG exposure for 24 hrs. n = 3. *P < 0.05 vs. Ctrl, #P < 0.05 vs. Vehl + HG. Ctrl: control; Vehl: vehicle; nutlin-3a: nutlin-3a treatment.
S2176^New	Tenovin-3 Tenovin-3 是一种 SIRT2 的抑制剂。Tenovin-3 能够增加MCF-7细胞中的 p53 的水平。
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。	Radiat Res,2020, 193(2):119-129 Theranostics,2019, 9(2):554-572 Front Pharmacol,2018, 9:92	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.
S7030	RG-7112 RG7112 (RO5045337)是一种口服具有活性的选择性p53-MDM2抑制剂，HTRF IC50为18 nM。	Eur J Cancer,2020, 126:93-103 Nat Commun,2019, 10(1):2189 Cancer Biother Radiopharm,2019, 34(4):252-257
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.
S5791	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。
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。	Nat Commun,2020, 3;11(1):1669 Cell Death Dis,2019, 10(11):831
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。

目录号	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）。	Genes Dev, 2020, 34(7-8):526-543 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 Br J Cancer, 2018, 119(4):450-461 Radiol Oncol, 2016, 50(2):168-74	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.
S2427^New	Triglycidyl Isocyanurate (Teroxirone) Triglycidyl Isocyanurate 又名 Teroxirone 是具有抗肿瘤活性的三氮杂三环氧化物。它通过激活 p53 抑制人非小细胞肺癌细胞的生长。Triglycidyl Isocyanurate 可以通过烷基化并交联DNA来抑制 DNA replication。Triglycidyl Isocyanurate 还用于金属精加工行业的各种聚酯粉末涂料中。
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 Int J Mol Med, 2019, 44(3):1091-1105	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.
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。	Cell Chem Biol, 2018, 25(5):585-594
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。	EMBO J, 2019, 38(20):e102096 Cell Chem Biol, 2018, 25(6):761-774 Oncotarget, 2017, 8(26):43008-43022	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。	Biomed Pharmacother, 2020, 125:109948 J Cell Sci, 2019, 132(6) 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。
S5811	Kevetrin hydrochloride Kevetrin hydrochloride是水溶性的p53激活剂，具有潜在的抗肿瘤活性。
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。	Micromachines (Basel), 2020, 11(2)
S8483	CBL0137 HCl (CBL-0137 HCl) 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。	Mol Cell, 2020, S1097-2765(20)30193-3
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。	J Biol Chem, 2020, 295(11):3576-3589 G3 (Bethesda), 2020, 4;10(5):1585-1597 Br J Haematol, 2019, 187(1):49-64	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

目录号	产品描述	文献引用	实验数据
S8728	PK11000 PK11000通过共价半胱氨酸修饰稳定野生型和突变型p53的DBD，而又不影响DNA结合，并且能有效诱导细胞死亡。

目录号

产品描述

文献引用

实验数据

S8728

PK11000

PK11000通过共价半胱氨酸修饰稳定野生型和突变型p53的DBD，而又不影响DNA结合，并且能有效诱导细胞死亡。

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