2. Metabolic Enzyme/Protease Stem Cell/Wnt JAK/STAT Signaling Immunology/Inflammation Apoptosis
  3. TNF Receptor Interleukin Related Pyruvate Kinase STAT HIF/HIF Prolyl-Hydroxylase NO Synthase COX
  4. Iminostilbene

Iminostilbene  (Synonyms: 5H-ジベンゾ[b,f]アゼピン)

製品番号: HY-N7064 純度: 99.34%
COA 取扱説明書 Technical Support

Iminostilbene is a chemical precursor of carbamazepine. Additionally, Iminostilbene is an orally active inhibitor of PKM2 (Pyruvate Kinase M2) and COX2 (Cyclooxygenase-2). Iminostilbene exerts its effects by inhibiting PKM2 and its interaction with HIF-1α and STAT3, reducing COX2 and iNOS expression, and decreasing LPS-induced release of IL-1β, IL-6, TNF-α, and MCP-1, thereby suppressing macrophage-mediated inflammatory responses and improving myocardial ischemia/reperfusion (MI/R) injury. Iminostilbene holds promise for research in inflammation regulation, cardiovascular diseases (such as MI/R injury), and macrophage-mediated immune-related diseases.

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Iminostilbene

Iminostilbene 構造式

CAS 番号 : 256-96-2

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 27 在庫あり
Solution
10 mM * 1 mL in DMSO USD 27 在庫あり
Solid
1 g $25 在庫あり
5 g $60 在庫あり
10 g $85 在庫あり
25 g $140 在庫あり
50 g $180 在庫あり
100 g $240 在庫あり
> 100 g   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

Other Forms of Iminostilbene:

Iminostilbene 関連抗体

Top Publications Citing Use of Products

TNF Receptor 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
TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

Interleukin Related 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
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

STAT 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
STAT3 STAT5 STAT6 STAT1

HIF/HIF Prolyl-Hydroxylase 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
HIF-1α HIF

NO Synthase 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
nNOS iNOS eNOS

COX 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
COX COX-1 COX-2 COX-3

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  • 純度とドキュメンテーション

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製品説明

Iminostilbene is a chemical precursor of carbamazepine. Additionally, Iminostilbene is an orally active inhibitor of PKM2 (Pyruvate Kinase M2) and COX2 (Cyclooxygenase-2). Iminostilbene exerts its effects by inhibiting PKM2 and its interaction with HIF-1α and STAT3, reducing COX2 and iNOS expression, and decreasing LPS-induced release of IL-1β, IL-6, TNF-α, and MCP-1, thereby suppressing macrophage-mediated inflammatory responses and improving myocardial ischemia/reperfusion (MI/R) injury. Iminostilbene holds promise for research in inflammation regulation, cardiovascular diseases (such as MI/R injury), and macrophage-mediated immune-related diseases[1][2].

IC50 & Target

COX-2

 

iNOS

 

STAT3

 

HIF-1α

 

Cellular Effect
Cell Line Type Value Description References
U-937 IC50
2.58 μM
Compound: 11
Cytotoxicity in UV-irradiated human U937 cells exposed to photosensitizer for 2 hrs before irradiation for 20 mins by WST-1 assay
Cytotoxicity in UV-irradiated human U937 cells exposed to photosensitizer for 2 hrs before irradiation for 20 mins by WST-1 assay
[PMID: 24900465]
体外実験

Iminostilbene (2.5-10 μM, 30 h) inhibits LPS-induced inflammatory response, reduces PKM2 expression, and suppresses its downstream signaling pathways in RAW264.7 macrophages[2].

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

Iminostilbene 関連抗体

Cell Viability Assay[2]

Cell Line: LPS (HY-D1056)-induced RAW264.7 macrophages (mouse-derived)
Concentration: 2.5 μM, 5 μM, 10 μM
Incubation Time: 30 h (6 h pre-treatment with Iminostilben, followed by LPS stimulation for 24 h)
Result: Showed no significant effect on cell viability at low doses, slight reduction at high dose (10 μM).

Real Time qPCR[2]

Cell Line: LPS (HY-D1056)-induced RAW264.7 macrophages (mouse-derived)
Concentration: 2.5 μM, 5 μM, 10 μM
Incubation Time: 30 h (6 h pre-treatment with Iminostilben, followed by LPS stimulation for 24 h)
Result: Suppressed IL-1β, IL-6, MCP-1, and TNF-α mRNA levels.

Western Blot Analysis[2]

Cell Line: LPS (HY-D1056)-induced RAW264.7 macrophages (mouse-derived)
Concentration: 2.5 μM, 5 μM, 10 μM
Incubation Time: 30 h (6 h pre-treatment with Iminostilben, followed by LPS stimulation for 24 h)
Result: Inhibited COX2, PKM2, and iNOS protein expression and reduced PKM2-HIF-1α-STAT3 interaction.
体内実験

Iminostilbene (0.625 mg/kg, 1.25 mg/kg, p.o., once daily for 5 days) improved cardiac function and suppressed inflammation in the myocardial ischemia/reperfusion (MI/R) injury SD rat model[2].

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

Animal Model: Myocardial ischemia/reperfusion (MI/R) injury Sprague-Dawley (SD) rat model[2]
Dosage: 0.625 mg/kg, 1.25 mg/kg
Administration: Oral gavage (p.o.), once daily for 5 days
Result: Improved cardiac function, reduced myocardial infarction area.
Decreased CK-MB, LDH, and cTnT levels.
Reduced inflammatory cell infiltration, inhibited COX2 and iNOS expression, and suppressed IL-1β and IL-6 RNA and protein levels.
分子量

193.25

分子式

C14H11N
CAS 番号
Appearance

Solid

Color

Yellow to orange

SMILES

C12=CC=CC=C1C=CC3=CC=CC=C3N2
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
体外: 

DMSO : 50 mg/mL (258.73 mM; Need ultrasonic; 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 5.1746 mL 25.8732 mL 51.7464 mL
5 mM 1.0349 mL 5.1746 mL 10.3493 mL
10 mM 0.5175 mL 2.5873 mL 5.1746 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 (protect from light). 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

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (12.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.34%

COA (254 KB) HNMR (94 KB) LCMS (232 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 (protect from light). 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 5.1746 mL 25.8732 mL 51.7464 mL 129.3661 mL
5 mM 1.0349 mL 5.1746 mL 10.3493 mL 25.8732 mL
10 mM 0.5175 mL 2.5873 mL 5.1746 mL 12.9366 mL
15 mM 0.3450 mL 1.7249 mL 3.4498 mL 8.6244 mL
20 mM 0.2587 mL 1.2937 mL 2.5873 mL 6.4683 mL
25 mM 0.2070 mL 1.0349 mL 2.0699 mL 5.1746 mL
30 mM 0.1725 mL 0.8624 mL 1.7249 mL 4.3122 mL
40 mM 0.1294 mL 0.6468 mL 1.2937 mL 3.2342 mL
50 mM 0.1035 mL 0.5175 mL 1.0349 mL 2.5873 mL
60 mM 0.0862 mL 0.4312 mL 0.8624 mL 2.1561 mL
80 mM 0.0647 mL 0.3234 mL 0.6468 mL 1.6171 mL
100 mM 0.0517 mL 0.2587 mL 0.5175 mL 1.2937 mL
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Iminostilbene 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:

Iminostilbene256-96-2TNF ReceptorInterleukin RelatedPyruvate KinaseSTATHIF/HIF Prolyl-HydroxylaseNO SynthaseCOXTumor Necrosis Factor ReceptorTNFRILHypoxia-inducible factorsHIFsHIF-PHNitric oxide synthasesNOSCyclooxygenaseinflammation regulationcardiovascular diseasesMI/R injurymacrophageInhibitorinhibitorinhibit

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