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IT-901 

Cat. No.: HY-124179
Handling Instructions

IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with an IC50 of 0.1 µM, 3 μM for NF-κB DNA binding and c-Rel DNA binding, respectively. IT-901, a bioactive naphthalenethiobarbiturate derivative, has the potential for human lymphoid tumors and ameliorate graft-versus-host disease (GVHD).

For research use only. We do not sell to patients.

IT-901 Chemical Structure

IT-901 Chemical Structure

CAS No. : 1584121-99-2

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Description

IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with an IC50 of 0.1 µM, 3 μM for NF-κB DNA binding and c-Rel DNA binding, respectively. IT-901, a bioactive naphthalenethiobarbiturate derivative, has the potential for human lymphoid tumors and ameliorate graft-versus-host disease (GVHD)[1][2].

IC50 & Target[1]

NF-κB

0.1 μM (IC50)

c-Rel

3 μM (IC50)

In Vitro

IT-901 (1, 3, 5 μM; for 24 hours) results in decreased proliferation of viable ABC and GCB DLBCL cells[1].
IT-901 (3 μM; for 24 hours) decreases cell viability in a dose-dependent fashion, at least 60 percent of cells were still viable after 48 hours of IT-901 treatment (4μM) in all tested cell lines except HBL1[1].
IT-901 (1, 5, 10 μM; for 6 hours) documents Diminished expression of p65 and p50 in nuclear and cytosolic fractions and also decreases the expression of the inhibitory subunit IκBα both in the phosphorylated and non-phosphorylated forms in primary CLL cells and cell lines[2].
The IC50 of IT-901/GDM-12 is 2.9 μM for c-Rel whereas IL-2 secretion is successfully blocked at 5 μM[1].
The concentrations of IT-901 above 10 μM become increasingly toxic and may lead to apoptosis of healthy cells[1].
IT-901 inhibits cell growth of both activated B-like (ABC) and germinal center B-like (GCB) cell lines with the IC50 values between 3μM to 4μM[1].

Cell Proliferation Assay[1]

Cell Line: TMD8 and SU-DHL8 cells
Concentration: 1, 3, 5 μM
Incubation Time: For 24 hours
Result: Resulted in decreased proliferation of viable ABC and GCB DLBCL cells.

Cell Viability Assay[1]

Cell Line: SU-DHL8 and TMD8 cells
Concentration: 3 μM
Incubation Time: For 24 hours
Result: Decreased cell viability in a dose-dependent fashion.

Western Blot Analysis[2]

Cell Line: Primary chronic lymphocytic leukemia (CLL) cells and cell lines
Concentration: 1, 5, 10 μM
Incubation Time: For 6 hours
Result: Documented Diminished expression of p65 and p50 in nuclear and cytosolic fractions and also decreased the expression of the inhibitory subunit IκBα both in the phosphorylated and non-phosphorylated forms.
In Vivo

IT-901 (24 mg/kg; IP; every other day for 2 weeks) has an effective treatment of acute GVHD without impairing anti-tumor activity[1].
IT-901 (12-20 mg/kg; IP) improves the PK profile by increasing T1/2 and Cmax[1].

Animal Model: BALB/C-Tg (NFkB-RE-luc)-Xen mice with 6-9 weeks old[1]
Dosage: 24 mg/kg
Administration: IP; every other day for 2 weeks
Result: Had an effective treatment of acute GVHD without impairing anti-tumor activity.
Molecular Weight

342.37

Formula

C₁₇H₁₄N₂O₄S

CAS No.

1584121-99-2

SMILES

O=C(/C(C(N1)=O)=C\C2=C3C=CC=CC3=C(OC)C=C2OC)NC1=S

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

IT-901IT901IT 901NF-κBNuclear factor-κBNuclear factor-kappaBorallyDNAbindingnaphthalenethiobarbituratederivativehumanlymphoidtumorsameliorategraft-versus-hostdiseaseGVHDInhibitorinhibitorinhibit

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IT-901
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