1-amino-3-(4-methylphenyl)pyrido[1,2-a]benzimidazole-2,4-dicarbonitrile Property

Density 

1.31±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO:30.0(Max Conc. mg/mL);92.78(Max Conc. mM)

form 

A crystalline solid

pka

2.90±0.50(Predicted)

color 

Light yellow to yellow

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H312Harmful in contact with skin

H315Causes skin irritation

H319Causes serious eye irritation

H332Harmful if inhaled

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P322Specific measures (see …on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P363Wash contaminated clothing before reuse.

P501Dispose of contents/container to..…

1-amino-3-(4-methylphenyl)pyrido[1,2-a]benzimidazole-2,4-dicarbonitrile Chemical Properties,Usage,Production

Definition

ChEBI: 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.

Biological Activity

iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1/AIFM2) with EC50 of 103 nM. It selectively induces ferroptosis in FSP1-overexpressing GPX4 knockout Pfa1 cells and HT1080 cells.

in vitro

iFSP1 (0.001-1 μM; 24 hours) inhibits the Gpx4-knockout cell growth as a dose-dependent manner, but does not inhibit the wild type cell growth. Treatment with the ferroptosis inhibitor Lip-1 protects GPX4 - knockout cells from iFSP1-induced ferroptosis. It (0.001-1 μM; 24 hours) is less efficient than genetic deletion of FSP1, whereas iFSP1 treatment in the FSP1-knockout background had no additive effect to RSL3-induced ferroptosis.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.

target

Target	Value
FSP1/AIFM2 (Cell-free assay)	103 nM(EC50)

storage

Store at -20°C