Isatin
Based on 1 Customer Validation
Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 μM). Also acts as an antagonist of both atrial natriuretic peptide stimulated and nitric oxide-stimulated guanylate cyclase activity. Shows effect on the serotonergic system.
For research use only. We do not sell to patients.
- Purity: 99.89%
- CAS No.: 91-56-5
- Formula: C8H5NO2
- Molecular Weight:147.13
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
IC50: 3 μM (MAO B)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
13.5 μM
Compound: 1
|
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
|
[PMID: 22386528] |
| BTI-TN-5B1-4 | IC50 |
18.75 μM
Compound: Is
|
Inhibition of human MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate incubated for 15 mins prior to substrate addition measured for 15 mins by Amplex red assay
Inhibition of human MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate incubated for 15 mins prior to substrate addition measured for 15 mins by Amplex red assay
|
[PMID: 23153812] |
| BTI-TN-5B1-4 | IC50 |
18.75 μM
Compound: Is
|
Inhibition of human MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate assessed as hydrogen peroxide production by fluorimetric method
Inhibition of human MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate assessed as hydrogen peroxide production by fluorimetric method
|
10.1039/C0MD00014K |
| BTI-TN-5B1-4 | IC50 |
18.75 μM
Compound: Isatin
|
Inhibition of human recombinant MAOB expressed in baculovirus infected insect BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine by amplex red assay
Inhibition of human recombinant MAOB expressed in baculovirus infected insect BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine by amplex red assay
|
[PMID: 20715818] |
| BTI-TN-5B1-4 | IC50 |
18.75 μM
Compound: Isatin
|
Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine after 15 mins by microplate fluorescence assay
Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine after 15 mins by microplate fluorescence assay
|
[PMID: 21872365] |
| BTI-TN-5B1-4 | IC50 |
18.75 μM
Compound: Isatin
|
Inhibition of human recombinant MAO-B expressed in baculovirus-infected BTI-TN-5B1-4 cell microsomes assessed as decrease in H2O2 production using p-tyramine as substrate preincubated for 15 mins by Amplex Red reagent based fluorimetric method
Inhibition of human recombinant MAO-B expressed in baculovirus-infected BTI-TN-5B1-4 cell microsomes assessed as decrease in H2O2 production using p-tyramine as substrate preincubated for 15 mins by Amplex Red reagent based fluorimetric method
|
[PMID: 24746464] |
| BTI-TN-5B1-4 | IC50 |
18754 nM
Compound: isatin
|
Inhibition of human recombinant MAOB expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay
Inhibition of human recombinant MAOB expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay
|
[PMID: 20579890] |
| BTI-TN-5B1-4 | IC50 |
34.39 μM
Compound: Isatin
|
Inhibition of human recombinant microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as reduction in H2O2 production preincubated for 15 mins followed by substrate addition measured for 15 mins Ample
Inhibition of human recombinant microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as reduction in H2O2 production preincubated for 15 mins followed by substrate addition measured for 15 mins Ample
|
[PMID: 27135371] |
| BTI-TN-5B1-4 | IC50 |
40 μM
Compound: Isatin
|
Inhibition of human recombinant MAOA expressed in baculovirus infected insect BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine by amplex red assay
Inhibition of human recombinant MAOA expressed in baculovirus infected insect BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine by amplex red assay
|
[PMID: 20715818] |
| HepG2 | IC50 |
>10 μM
Compound: 1a
|
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
|
[PMID: 24360564] |
| HepG2 | IC50 |
>10 μM
Compound: 1a
|
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
|
[PMID: 30055465] |
| HT-29 | IC50 |
>10 μM
Compound: 1a
|
Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay
Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay
|
[PMID: 24360564] |
| Jurkat | IC50 |
>10 μM
Compound: 1a
|
Anticancer activity against human Jurkat cells after 48 hrs by MTT assay
Anticancer activity against human Jurkat cells after 48 hrs by MTT assay
|
[PMID: 26890120] |
| K562 | IC50 |
>10 μM
Compound: 1a
|
Cytotoxicity against human K562 cells after 48 hrs by MTT assay
Cytotoxicity against human K562 cells after 48 hrs by MTT assay
|
[PMID: 24360564] |
| K562 | IC50 |
>10 μM
Compound: 1a
|
Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
|
[PMID: 30055465] |
| KB 3-1 | IC50 |
>50 μM
Compound: 8
|
Cytotoxicity against human P-gp-negative KB-3-1 cells after 72 hrs by MTT assay
Cytotoxicity against human P-gp-negative KB-3-1 cells after 72 hrs by MTT assay
|
[PMID: 19397322] |
| KB-V1 | IC50 |
>50 μM
Compound: 8
|
Cytotoxicity against human P-glycoprotein-expressing KBV1 cells after 72 hrs by MTT assay
Cytotoxicity against human P-glycoprotein-expressing KBV1 cells after 72 hrs by MTT assay
|
[PMID: 19397322] |
| MDA-MB-231 | IC50 |
>100 μM
Compound: 1
|
Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay
|
[PMID: 22386528] |
| MRC5 | IC50 |
>100 μM
Compound: 1
|
Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay
Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay
|
[PMID: 22386528] |
| SK-N-SH | IC50 |
9.84 μM
Compound: 1
|
Cytotoxicity against human SK-N-SH cells after 48 hrs by MTT assay
Cytotoxicity against human SK-N-SH cells after 48 hrs by MTT assay
|
[PMID: 22386528] |
| U-937 | IC50 |
565 μM
Compound: 2a
|
Cytotoxicity against human U937 cells
Cytotoxicity against human U937 cells
|
[PMID: 17088067] |
| U-937 | IC50 |
565 μM
Compound: isatin
|
Cytotoxicity against human U937 cells
Cytotoxicity against human U937 cells
|
[PMID: 21306903] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 91-56-5
-
Appearance Solid
-
Molecular Weight 147.13
-
Formula C8H5NO2
-
Color Yellow to orange
-
SMILES
O=C1NC2=C(C=CC=C2)C1=O
-
Synonyms
Indoline-2,3-dione
-
Structure Classification
-
Initial Source
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (679.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (13.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (13.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Purity & Documentation
-
Data Sheet (276 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
[2]. Igosheva N, et al. Isatin, an endogenous monoamine oxidase inhibitor, triggers a dose- and time-dependent switch from apoptosis to necrosis in human neuroblastoma cells. Neurochem Int. 2005 Aug;47(3):216-24. [Content Brief]
[3]. McIntyre IM, et al. Serotonergic effects of isatin: an endogenous MAO inhibitor related to tribulin. J Neural Transm Gen Sect. 1990;79(1-2):35-40. [Content Brief]
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 | 6.7966 mL | 33.9829 mL | 67.9657 mL | 169.9143 mL |
| 5 mM | 1.3593 mL | 6.7966 mL | 13.5931 mL | 33.9829 mL | |
| 10 mM | 0.6797 mL | 3.3983 mL | 6.7966 mL | 16.9914 mL | |
| 15 mM | 0.4531 mL | 2.2655 mL | 4.5310 mL | 11.3276 mL | |
| 20 mM | 0.3398 mL | 1.6991 mL | 3.3983 mL | 8.4957 mL | |
| 25 mM | 0.2719 mL | 1.3593 mL | 2.7186 mL | 6.7966 mL | |
| 30 mM | 0.2266 mL | 1.1328 mL | 2.2655 mL | 5.6638 mL | |
| 40 mM | 0.1699 mL | 0.8496 mL | 1.6991 mL | 4.2479 mL | |
| 50 mM | 0.1359 mL | 0.6797 mL | 1.3593 mL | 3.3983 mL | |
| 60 mM | 0.1133 mL | 0.5664 mL | 1.1328 mL | 2.8319 mL | |
| 80 mM | 0.0850 mL | 0.4248 mL | 0.8496 mL | 2.1239 mL | |
| 100 mM | 0.0680 mL | 0.3398 mL | 0.6797 mL | 1.6991 mL |