An inhibitor of the NF-κB subunit c-Rel; inhibits NF-κB DNA binding (IC50 = 0.1 µM); reduces TNF-α-induced NF-κB activity (IC50 = 4 µM); decreases proliferation of ABC and GCB DLBCLL cells at 3 µM; increases HO-1 expression and ROS production in mitochondria of DLBCL cells but not normal leukocytes; increases survival in a mouse model of GVHD at 24 mg/kg every other day beginning eight days after HSCT; reduces tumor growth in mouse xenograft models of EBV-induced B cell lymphoma

IT-901 – 1 mg

Brand:
Cayman
CAS:
1584121-99-2
Storage:
-20
UN-No:
Non-Hazardous - /

IT-901 is an inhibitor of the NF-κB subunit c-Rel.{42097} It inhibits NF-κB DNA binding in HBL1 cells (IC50 = 0.1 µM) and reduces TNF-α-induced NF-κB activity in a reporter assay (IC50 = 4 µM). IT-901 decreases proliferation of activated B-like (ABC) and germinal center B-like (GCB) human diffuse large B cell lymphoma (DLBCL) cells when used at a concentration of 3 µM. It increases the expression of heme oxygenase-1 (HO-1; Item No. 22731) in DLBCL cells and increases the production of reactive oxygen species (ROS) in the mitochondria of DLBCL cells but not normal leukocytes. IT-901 increases survival in a mouse model of graft versus host disease (GVHD) when administered at a dose of 24 mg/kg every other day beginning eight days after hematopoietic stem cell transplantation (HSCT). It also reduces tumor growth in mouse xenograft models of B cell lymphoma induced by Epstein-Barr virus (EBV), chronic lymphocytic leukemia (CLL), and Richter syndrome.{42097,42098}  

 

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Description

An inhibitor of the NF-κB subunit c-Rel; inhibits NF-κB DNA binding (IC50 = 0.1 µM); reduces TNF-α-induced NF-κB activity (IC50 = 4 µM); decreases proliferation of ABC and GCB DLBCLL cells at 3 µM; increases HO-1 expression and ROS production in mitochondria of DLBCL cells but not normal leukocytes; increases survival in a mouse model of GVHD at 24 mg/kg every other day beginning eight days after HSCT; reduces tumor growth in mouse xenograft models of EBV-induced B cell lymphoma, CLL, and Richter syndrome

Formal name: 5-[(2,4-dimethoxy-1-naphthalenyl)methylene]dihydro-2-thioxo-4,6(1H,5H)-pyrimidinedione

Synonyms: 

Molecular weight: 342.4

CAS: 1584121-99-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ox Stress Reagents|Free Radical Generators||Product Type|Biochemicals|Small Molecule Inhibitors|TNF-α/NF-κB Signaling||Research Area|Cancer|Cell Signaling|NF-κB Signaling||Research Area|Cancer|Transcription Factors|NF-κB||Research Area|Cancer|Tumor Microenvironment||Research Area|Cell Biology|Cell Signaling|NF-κB Signaling||Research Area|Cell Biology|Stem Cell Research||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors||Research Area|Oxidative Stress & Reactive Species|Pro-oxidant Activity||Research Area|Oxidative Stress & Reactive Species|Reactive Oxygen

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