NSC194598 

NSC194598 is a p53 DNA-binding inhibitor with an IC₅₀ value of 180 nM. NSC194598 inhibits p53 DNA binding and induction of target genesn when p53 is stabilized and activated by irradiation or chemotherapy. NSC194598 can interfere with transcriptional activation of mutated rearranged during transfection (RET) gene, induce apoptosis and G0/G1 phase arrest. NSC194598 can be used for the researches of acute radiation toxicity and medullary thyroid carcinoma^[1][2].

NSC194598 (1-2 μM; 35 min) inhibits p53, p63γ, and p73β DNA binding^[1].
NSC194598 inhibits the DNA-binding activity of p53-Cluc in a cell-free luciferase fragment competition assay with an IC₅₀ of 0.18 μM^[1].
NSC194598 inhibits a p53 quadruple mutant (p53-
M133L/V203A/N239Y/N268D) with an IC₅₀ of 0.06 μM^[1].
NSC194598 (2-40 μM; 4 h) inhibits IR-induced p53 DNA binding and target gene expression in U2OS cells^[1].
NSC194598 (2-40 μM; 8 h) inhibits p21 induction by activated p53^A138V in H1299-p53^A138V cells without altering p53 levels^[1].
NSC194598 (5-20 μM; 32 h) causes weak p53 accumulation and p21 induction in SJSA cells, and inhibits Nutlin-induced p21 expression^[1].
NSC194598 (0.5-20 μM) stabilizes the wild-type RET promoter G-quadruplex structure without altering its parallel folding pattern^[2].
NSC194598 (0.6-2.5 μg/mL; 24 h) inhibits wild-type RET promoter-driven luciferase activity in HEK293 WT cells by over 60% after 24 h treatment at 2.5 μg/mL, with concentration-dependent effects^[2].
NSC194598 (1.2-2.5 μg/mL; 24-48 h) reduces RET mRNA expression in TT cells^[2].
NSC194598 (2.5 μM; 24 h) inhibits recruitment of RNA polymerase II, Sp1, and nucleolin to the RET promoter at 2.5 μM for 24 h in TT cells^[2].
NSC194598 (0.3-2.5 μg/mL; 24 h) reduces TT cell growth and increases caspase 3 activity^[2].
NSC194598 (0.6-2.5 μg/mL; 24 h) induces dose-dependent increases in late apoptotic/necrotic TT cells, and induces G0/G1 phase arrest^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NSC194598 (80 μg; i.p.; single dose) administered immediately before 8 Gy gamma radiation produces a statistically significant improvement in mouse survival over a 40-day period^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

317.38

C₂₀H₁₉N₃O

5358-76-9

Solid

Light yellow to yellow

[O-][N+](C(CN1CCCCC1)=N2)=C3C4=C(C=CC=C4)C5=C3C2=CC=C5

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Li Q, et al. Inhibition of p53 DNA binding by a small molecule protects mice from radiation toxicity. Oncogene. 2020;39(29):5187-5200.  [Content Brief]

  [2]. Shin YJ, et al. Involvement of G-quadruplex structures in regulation of human RET gene expression by small molecules in human medullary thyroid carcinoma TT cells. Oncogene. 2015;34(10):1292-1299.  [Content Brief]