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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

NSC194598

NSC194598 構造式

CAS 番号 : 5358-76-9

容量 価格（税別） 在庫状況 数量
1 mg $145 在庫あり
5 mg   お問い合わせ  
10 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 0 publication(s) in Google Scholar

NSC194598 関連抗体

Top Publications Citing Use of Products

DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

Caspase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

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

 

体外実験

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 関連抗体

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.
体内実験

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.
分子量

317.38

分子式

C20H19N3O
CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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
10 mM 0.3151 mL 1.5754 mL 3.1508 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
純度とドキュメンテーション

純度: 98.90%

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

取扱説明書 (2659 KB)
参考文献

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

NSC194598 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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

最近チェックした製品:

オンラインお問い合わせ

Your information is safe with us. * Required Fields.

製品名

  

カスタマ需要量 *

お名前 *

 

タイトル

メールアドレス *

 

電話番号 *

デパートメント

 

組纖名 *

市区町村

都道府県

国或いは地域 *

      

必ず会社名を記載ください。個人への返信は行いません。

備考

バルクお問い合わせ

Inquiry Information

製品名:
NSC194598
製品番号:
HY-156135
数量:
MCE 日本正規代理店:

カスタマーレビュー

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

製品名

  

Lot #

お名前 *

 

メールアドレス *

電話番号 *

 

部門 *

組纖名 *

 

国或いは地域 *

備考

Request for HNMR Report

We have received your request and will respond to you as soon as possible.