Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T61369 |
p53 Activator 2
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p53 Activator 2 (compound 10ah) 插入DNA,导致显著的DNA双链断裂。该化合物通过增加p53、p-p53、CDK4、p21的表达,使细胞周期在G2/M期停滞,诱导细胞凋亡,并显著降低抗凋亡蛋白Bcl-2、Bcl-xL和cyclin B1的水平。此外,p53 Activator 2表现出对MGC-803细胞的抗增殖效果,其IC50为1.73 μM,且在MGC-803异种移植肿瘤模型中展示出有效的抗癌活性。 | |||
T67858 |
STIMA-1
2-Vinylquinazolin-4-ol,p53 Activator VII |
Others | Others |
STIMA-1 (2-Vinylquinazolin-4-ol) 是一种活性化合物,可以恢复 p63 的活性。STIMA-1 可以刺激角质形成细胞的增殖和分化。 | |||
T22980 |
MIRA-1
p53 Activator VIII,1-[(1-Oxopropoxy)methyl]-1H-pyrrole-2,5-dione,(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)methyl propionate,NSC 19630,WRN Helicase Inhibitor |
DNA/RNA Synthesis; p53 | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
MIRA-1 (WRN Helicase Inhibitor) 是马来酰亚胺类似物。它可以恢复p53依赖的转录转激活诱导 p53 突变细胞凋亡,具有抗肿瘤作用。 | |||
T72771 |
p53 Activator 7
|
Apoptosis | Apoptosis |
p53 Activator 7 是一种高效性和细胞渗透性的 p53 突变 Y220C (MDM-2/p53) 激活剂,可诱导细胞凋亡 。 | |||
T4325 |
COTI-2
COTI 2,COTI2 |
Apoptosis; p53 | Apoptosis |
COTI-2是一种具有口服活性的低毒性抗癌药物,是 p53 突变体激活剂。它通过激活突变型 p53 和抑制PI3K/AKT/mTOR 途径发挥作用,通过 p53 依赖和非依赖机制在 HNSCC 中具有抗肿瘤活性。它诱导多种人肿瘤细胞凋亡,可将突变型 p53 转化为野生型构象。 | |||
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。 | |||
T63748 | rel-MDM2/4-p53-IN-2 | ||
rel-MDM2/4-p53-IN-2 (2q) 是有效的双重 MDM2/MDM4 抑制剂和 p53 激活剂,能够作用于 MDM2-p53 复合物 (IC50: 70.7 nM) 和 MDM4-p53 复合物 (IC50: 81.4 nM)。rel-MDM2/4-p53-IN-2 能够调控细胞周期,诱导细胞凋亡(apoptosis),表现出抗癌效果。 | |||
T36465 |
Caylin-2
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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-2 is a nutlin-3 analog in which trifluoromethyl groups have been substituted for chlorine on the 2 phenyl rings. At high concentrations, caylin-2 inhibits the growth of HCT116 cells with an IC50 of approximately 8 μM, making it about 10-fold less potent than nutlin-3. Interestingly, at concentrations between 5-100 nM, caylin-2 promotes the growth of HCT116 c... | |||
TP1724 |
PUMA BH3
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PUMA BH3 is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.This is a PUMA BH3 domain peptide. PUMA proteins bind Bcl-2, localize to the mitochondria, and induce cytochrome C releas | |||
T35812 |
CAY10591
CAY10591 |
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Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. CAY10591 has been identified as an activator of the enzyme SIRT1. This com... |