2. Apoptosis Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage
  3. MDM-2/p53 RET DNA/RNA Synthesis Apoptosis Caspase
  4. 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.

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NSC194598

NSC194598 Estructura química

No. CAS : 5358-76-9

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Based on 1 publication(s) in Google Scholar

NSC194598 Related Antibodies

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Descripciòn

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].

IC50 & Target[2]

Caspase 3

 

In Vitro

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 p53A138V in H1299-p53A138V 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 Related Antibodies

Western Blot Analysis[1]

Cell Line: H1299-p53-A138V human lung cancer cells
Concentration: 2, 5, 10, 20, 40 μM
Incubation Time: 8 h
Result: Inhibited p21 protein expression without changing p53 protein levels.

RT-PCR[2]

Cell Line: Human medullary thyroid carcinoma TT cells
Concentration: 1.2, 2.5 μg/mL
Incubation Time: 24 h, 48 h
Result: Reduced RET mRNA expression by 90% at concentrations below 2.5 μg/mL after 24 and 48 h.

Western Blot Analysis[2]

Cell Line: Human medullary thyroid carcinoma TT cells
Concentration: 1.2, 2.5 μg/mL
Incubation Time: 24 h, 48 h
Result: Induced corresponding reductions in RET protein levels alongside reduced RET mRNA expression.

Cell Proliferation Assay[2]

Cell Line: Human medullary thyroid carcinoma TT cells
Concentration: 0.3, 0.6, 1.2, 2.5 μg/mL
Incubation Time: 24 h
Result: Reduced cell number to 70% of control at 2.5 μg/mL.

Apoptosis Analysis[2]

Cell Line: Human medullary thyroid carcinoma TT cells
Concentration: 0.6, 1.2, 2.5 μg/mL
Incubation Time: 24 h
Result: Induced dose-dependent increases in propidium iodide-stained unfixed cells.

Cell Cycle Analysis[2]

Cell Line: Human medullary thyroid carcinoma TT cells
Concentration: 0.6, 1.2, 2.5 μg/mL
Incubation Time: 24 h
Result: Induced a dose-dependent increase in sub-G0/G1 apoptotic cells.
In Vivo

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.

Animal Model: C57BL/6 (male and female, ~2 months old)[1]
Dosage: 80 μg
Administration: i.p.; single dose, before 8 Gy gamma radiation
Result: Produced a statistically significant improvement in survival over 40 days after irradiation.
Did not prevent initial body weight loss but increased the probability of weight recovery after the initial decrease.
Peso molecular

317.38

Fòrmula

C20H19N3O
No. CAS
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
In Vitro: 

DMSO : 8.3 mg/mL (26.15 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1508 mL 15.7540 mL 31.5080 mL
5 mM 0.6302 mL 3.1508 mL 6.3016 mL
View the Complete Stock Solution Preparation Table

* 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.

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In Vivo Dissolution Calculator
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Pureza y Documentación

Purity: 98.90%

SDS (251 KB)

COA (262 KB) Elemental Analysis Report (121 KB)

Instrucciones de manejo (2659 KB)
Referencias

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1508 mL 15.7540 mL 31.5080 mL 78.7699 mL
5 mM 0.6302 mL 3.1508 mL 6.3016 mL 15.7540 mL
10 mM 0.3151 mL 1.5754 mL 3.1508 mL 7.8770 mL
15 mM 0.2101 mL 1.0503 mL 2.1005 mL 5.2513 mL
20 mM 0.1575 mL 0.7877 mL 1.5754 mL 3.9385 mL
25 mM 0.1260 mL 0.6302 mL 1.2603 mL 3.1508 mL
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NSC194598 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NSC1945985358-76-9NSC 194598NSC-194598MDM-2/p53RETDNA/RNA SynthesisApoptosisCaspasep73U2OS cellsc-MycRET promoter G-quadruplexE2F1TCF1TT cellsp53p63MDM2Inhibitorinhibitorinhibit

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Nombre del producto:
NSC194598
Cat. No.:
HY-156135
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