Cat. No.: HY-124179

IT-901

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

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.

Purity: 99.32%
CAS No.: 1584121-99-2
Formula: C₁₇H₁₄N₂O₄S
Molecular Weight:342.37

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

IT-901 Chemical Structure

CAS No.: 1584121-99-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^{[1]

NF-κB
0.1 μM (IC₅₀)

c-Rel
3 μM (IC₅₀)

All NF-κB Isoforms :

NF-κB

NF-κB1/p50

RelA/p65

RelB

c-Rel}

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 T_1/2 and C_max^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Chemical Information

CAS No. 1584121-99-2
Appearance Solid
Molecular Weight 342.37
Formula C₁₇H₁₄N₂O₄S
Color Orange to red
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

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Cell Death Discov

The glycolytic enzyme PFKFB3 alleviates DNA damage and chondrocyte senescence in osteoarthritis. [Abstract]

2025 Dec 8. PMID: 41360766

Solvent & Solubility

In Vitro:

DMSO : 12.5 mg/mL (36.51 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9208 mL

14.6041 mL

29.2082 mL

5 mM

0.5842 mL

2.9208 mL

5.8416 mL

10 mM

0.2921 mL

1.4604 mL

2.9208 mL

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.

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Shono Y, et al. Characterization of a c-Rel Inhibitor That Mediates Anticancer Properties in HematologicMalignancies by Blocking NF-κB-Controlled Oxidative Stress Responses. Cancer Res. 2016 Jan 15;76(2):377-89. [Content Brief]

[2]. Vaisitti T, et al. Targeting metabolism and survival in chronic lymphocytic leukemia and Richter syndrome cellsby a novel NF-κB inhibitor. Haematologica. 2017 Nov;102(11):1878-1889. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.9208 mL	14.6041 mL	29.2082 mL	73.0204 mL
	5 mM	0.5842 mL	2.9208 mL	5.8416 mL	14.6041 mL
	10 mM	0.2921 mL	1.4604 mL	2.9208 mL	7.3020 mL
	15 mM	0.1947 mL	0.9736 mL	1.9472 mL	4.8680 mL
	20 mM	0.1460 mL	0.7302 mL	1.4604 mL	3.6510 mL
	25 mM	0.1168 mL	0.5842 mL	1.1683 mL	2.9208 mL
	30 mM	0.0974 mL	0.4868 mL	0.9736 mL	2.4340 mL

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IT-901

Immunology/Inflammation Compound Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Pyroptosis Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

Covalent Screening Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) IT-901

All NF-κB Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

IT-901 Related Classifications

Cat. No.: HY-124179