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| 25mg |
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iFSP1 is a novel and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1) (AIFM2) with an EC50 of 103 nM. Moreover, it is a ferroptosis inducer.
| Targets |
FSP1 (EC50 = 103 nM)
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|---|---|
| ln Vitro |
iFSP1 (0.001-1 μM; 24 hours) inhibits the growth of Gpx4-knockout cells in a dose-dependent manner but not the growth of wild-type cells. Ferroptosis-inducing iFSP1 can be prevented in GPX4 knockout cells by treatment with the ferroptosis inhibitor Lip-1[1].
iFSP1 (0.001-1 μM; 24 hours) is less effective than genetic deletion of FSP1, whereas iFSP1 treatment in the FSP1-knockout background had no additive effect to RSL3-induced ferroptosis[1]. iFSP1 (3 μM; 24 hours) treatment results in an obvious toxicity of RSL3 in a panel of genetically engineered (FSP1-knockout) human cancer cell lines[1]. AIFM2: A previously unrecognized anti-ferroptotic gene is the flavoprotein apoptosis-inducing factor mitochondria-associated 2. Ironoptosis suppressor protein 1 (FSP1), also known as AIFM2, is a protein.[1] |
| Cell Assay |
After plating, cells are seeded on 96-well plates (2,500 cells per well) and given an iFSP-1 treatment. According to the manufacturer's instructions, cell viability is evaluated 24 h (unless otherwise specified) after treatment using AquaBluer as an indicator of viable cells.
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| References | |
| Additional Infomation |
IFSP1 is a member of the class of pyridobenzimidazoles that is pyrido[1,2-a]benzimidazole substituted by amino, cyano, 4-methylphenyl, and cyano groups at positions 1, 2, 3 and 4, respectively. It is a potent inhibitor of ferroptosis suppressor protein 1 (FSP1) with EC50 of 103 nM. It induces ferroptosis in GPX4 knockout cells that overexpress FSP1. It has a role as a ferroptosis inducer, an antineoplastic agent and a ferroptosis suppressor protein 1 inhibitor. It is a member of toluenes, a nitrile, a primary amino compound, an aromatic amine and a pyridobenzimidazole.
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| Molecular Formula |
C₂₀H₁₃N₅
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|---|---|
| Molecular Weight |
323.35
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| Exact Mass |
323.117
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| Elemental Analysis |
C, 74.29; H, 4.05; N, 21.66
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| CAS # |
150651-39-1
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| Related CAS # |
150651-39-1
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| PubChem CID |
699043
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.369
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
25
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| Complexity |
592
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
N12C(=C(C#N)C(C3C=CC(C)=CC=3)=C(C#N)C1=NC1C=CC=CC2=1)N
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| InChi Key |
FNESYDFRCQEEKA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H13N5/c1-12-6-8-13(9-7-12)18-14(10-21)19(23)25-17-5-3-2-4-16(17)24-20(25)15(18)11-22/h2-9H,23H2,1H3
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| Chemical Name |
1-amino-3-(4-methylphenyl)pyrido[1,2-a]benzimidazole-2,4-dicarbonitrile
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| Synonyms |
iFSP1; iFSP-1; iFSP 1
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~20 mg/mL (~61.9 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (6.19 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0926 mL | 15.4631 mL | 30.9262 mL | |
| 5 mM | 0.6185 mL | 3.0926 mL | 6.1852 mL | |
| 10 mM | 0.3093 mL | 1.5463 mL | 3.0926 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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