Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2158 |
Nutlin-3
Nutlin3 |
E1/E2/E3 Enzyme | Ubiquitination |
Nutlin-3 是一种 MDM2 拮抗剂,抑制 MDM2-p53 相互作用 ,Ki 为 90 nM,并激活 p53。 | |||
T6023 |
Nutlin-3a
(-)-Nutlin-3,Nutlin-3a chiral,(−)-Nutlin-3 |
Apoptosis; E1/E2/E3 Enzyme; Autophagy | Apoptosis; Autophagy; Ubiquitination |
Nutlin-3a ((−)-Nutlin-3) 是 Nutlin-3 的活性对映体,是一种 MDM2抑制剂,可抑制 MDM2-p53相互作用,稳定 p53 蛋白,从而诱导细胞自噬和凋亡,有潜力研究 TP53野生型卵巢癌。 | |||
T6613 | (Rac)-Nutlin-3 | ||
T6614 |
Nutlin-3b
(+)-Nutlin-3,4-[[(4R,5S)-4,5-双(4-氯苯基)-4,5-二氢-2-[4-甲氧基-2-(1-甲基乙氧基)苯基]-1H-咪唑-1-基]羰基]-2-哌嗪酮 |
Mdm2; E1/E2/E3 Enzyme | Apoptosis; Ubiquitination |
Nutlin-3b ((+)-Nutlin-3) 是一种 p53/MDM2 拮抗剂或抑制剂,IC50为 13.6 μM。它与 MDM2 的结合活性比 Nutlin-3a 低 150 倍。 | |||
T1798 |
RITA
NSC 652287,RITA (NSC 652287) |
Mdm2; DNA Alkylator/Crosslinker; p53; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair |
RITA (NSC-652287) 是 p53-HDM-2相互作用抑制剂,可诱导 DNA-DNA 和 DNA-蛋白质的交联,可与 p53dN 结合,Kd 值为 1.5 nM。 | |||
T17873 |
(4R,5S)-nutlin carboxylic acid
E3 ligase Ligand 15,MDM2 ligand 2 |
Others | Others |
(4R,5S)-Nutlin Carboxylic Acid (MDM2 Ligand 2), a Nutlin 3-based MDM2 ligand, can be conjugated to a protein-binding ligand via a linker to create PROTACs[1]. | |||
T17874 |
Nutlin carboxylic acid
MDM2 ligand 1,E3 ligase Ligand 16 |
Others | Others |
Nutlin Carboxylic Acid (MDM2 ligand 1), derived from Nutlin 3, serves as an MDM2 ligand. It can be attached to a protein ligand via a linker to create PROTACs[1]. | |||
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... | |||
T36464 |
Caylin-1
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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-1 is a nutlin-3 analog which contains chlorine substituents at the 3 and 4 positions on two of the phenyl rings rather than a single 4-chloro as seen in nutlin-3. At high concentrations, caylin-1 inhibits the growth of HCT116 cells with an IC50 value of approximately 7 μM, making it about 7-fold less potent than nutlin-3 in the same assay. Interestingly, at ... | |||
T17902 |
Nutlin-C1-amido-PEG4-C2-N3
E3 ligase Ligand-Linker Conjugates 48,MDM2 Ligand-Linker Conjugates 1 |
Others | Others |
Nutlin-C1-amido-PEG4-C2-N3 is a novel compound that functions as a ligand-linker conjugate for the E3 ligase. It is a synthesized molecule incorporating the MDM2 ligand derived from Nutlin 3, and a 4-unit PEG linker. This compound is specifically designed for utilization in PROTAC technology. | |||
T36192 |
CAY10682
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(±)-Nutlin-3 blocks the interaction of p53 with its negative regulator Mdm2 (IC50 = 90 nM), inducing the expression of p53-regulated genes and blocking the growth of tumor xenografts in vivo. CAY10682 is a pyrrolo[3,4c]pyrazole derivative that inhibits the p53-Mdm2 interaction as potently as (±)-nutlin-3 (Ki = 83 nM) and also dose-dependently reduces activation of the NF-κB pathway. It specifically prevents phosphorylation of IκBα by the kinases IKKα, IKKβ, and IKK (IC50s = 80.5, 78.2, and 57.1... |