p53
p53产品
目录号 | 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。Pifithrin-α也是一种有效的 aryl hydrocarbon receptor (AhR) 的兴奋剂。 |
![]() ![]() 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. |
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S8059 |
Nutlin-3aNutlin-3a ((-)-Nutlin-3)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。 |
![]() ![]() 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. |
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S2930 |
Pifithrin-μPifithrin-μ (NSC 303580, PFTμ) 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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S7030 |
RG-7112RG7112 (RO5045337)是一种口服具有活性的选择性p53-MDM2抑制剂,HTRF IC50为18 nM。 |
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S9235 |
DidyminDidymin (Neoponcirin, Isosakuranetin-7-O-rutinoside) 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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S5791 |
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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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 (XI-006) 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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S2176New |
Tenovin-3Tenovin-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。 |
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S0507New |
CBL0137CBL0137 (Curaxin-137)是一种 histone chaperone FACT (facilitates chromatin transcription) 的抑制剂,可同时抑制 NF-κB 并激活 p53,对应的EC50值分别为0.47 μM和0.37 μM。 |
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S2427New |
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。 |
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S8000 |
Tenovin-1Tenovin-1 可防止MDM2介导的p53的降解,涉及泛素化途径,并通过导致SirT1和SirT2蛋白脱乙酰基活性的降低而发挥作用。Tenovin-1 也是 dihydroorotate dehydrogenase (DHODH) 的抑制剂。 |
![]() ![]() 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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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并可抑制 dihydroorotate dehydrogenase (DHODH)。Tenovin-6 也是 SirT1 和 SirT2 的抑制剂。 |
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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。APR-246 可诱导凋亡和自噬。 |
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S5811 |
Kevetrin hydrochlorideKevetrin hydrochloride (Thioureidobutyronitrile)是水溶性的p53激活剂,具有潜在的抗肿瘤活性。 |
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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 HClCBL0137 (CBLC137, Curaxin 137) HCl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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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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S7723 |
PRIMA-1PRIMA-1 (2,2-Bis(hydroxymethyl)-3-quinuclidinone)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。 |
![]() ![]() 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 |
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S6882New |
HI-TOPK-032HI-TOPK-032 是一种有效的、特异性的 TOPK 的抑制剂。HI-TOPK-032 还可以降低 ERK-RSK 磷酸化,调节 p53、裂化的 caspase-7 和裂化的 PARP 的丰度,并在癌细胞中诱导凋亡。 |
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S6851New |
RA-190RA190 是一种双亚苄基哌啶,一种有效的、选择性的和口服活性的 proteasome ubiquitin receptor RPN13/ADRM1 抑制剂,具有抗癌活性。 RA190 可触发多发性骨髓瘤细胞的内质网应激反应、p53/p21 信号轴和自噬。 |
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S8728 |
PK11000PK11000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) HBrPifithrin-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。 |
![]() ![]() 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-3aNutlin-3a ((-)-Nutlin-3)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。 |
![]() ![]() 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. |
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S2930 |
Pifithrin-μPifithrin-μ (NSC 303580, PFTμ) 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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S7030 |
RG-7112RG7112 (RO5045337)是一种口服具有活性的选择性p53-MDM2抑制剂,HTRF IC50为18 nM。 |
||
S9235 |
DidyminDidymin (Neoponcirin, Isosakuranetin-7-O-rutinoside) 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 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。 |
||
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。 |
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。 |
![]() ![]() |
|
S2678 |
NSC 207895NSC 207895 (XI-006) 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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S2176New |
Tenovin-3Tenovin-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。 |
||
S0507New |
CBL0137CBL0137 (Curaxin-137)是一种 histone chaperone FACT (facilitates chromatin transcription) 的抑制剂,可同时抑制 NF-κB 并激活 p53,对应的EC50值分别为0.47 μM和0.37 μM。 |
||
S2427New |
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-1Tenovin-1 可防止MDM2介导的p53的降解,涉及泛素化途径,并通过导致SirT1和SirT2蛋白脱乙酰基活性的降低而发挥作用。Tenovin-1 也是 dihydroorotate dehydrogenase (DHODH) 的抑制剂。 |
![]() ![]() 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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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。 |
||
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。 |
||
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并可抑制 dihydroorotate dehydrogenase (DHODH)。Tenovin-6 也是 SirT1 和 SirT2 的抑制剂。 |
||
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。APR-246 可诱导凋亡和自噬。 |
||
S5811 |
Kevetrin hydrochlorideKevetrin hydrochloride (Thioureidobutyronitrile)是水溶性的p53激活剂,具有潜在的抗肿瘤活性。 |
||
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。 |
||
S8483 |
CBL0137 HClCBL0137 (CBLC137, Curaxin 137) HCl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。 |
||
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。 |
||
S7723 |
PRIMA-1PRIMA-1 (2,2-Bis(hydroxymethyl)-3-quinuclidinone)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。 |
![]() ![]() 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 |
---|---|---|---|
S6882New |
HI-TOPK-032HI-TOPK-032 是一种有效的、特异性的 TOPK 的抑制剂。HI-TOPK-032 还可以降低 ERK-RSK 磷酸化,调节 p53、裂化的 caspase-7 和裂化的 PARP 的丰度,并在癌细胞中诱导凋亡。 |
||
S6851New |
RA-190RA190 是一种双亚苄基哌啶,一种有效的、选择性的和口服活性的 proteasome ubiquitin receptor RPN13/ADRM1 抑制剂,具有抗癌活性。 RA190 可触发多发性骨髓瘤细胞的内质网应激反应、p53/p21 信号轴和自噬。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S8728 |
PK11000PK11000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。 |