IT-901
Based on 2 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).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.32%
- CAS 番号: 1584121-99-2
- 分子式: C17H14N2O4S
- 分子量:342.37
-
保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 IT-901
More
生物活性
|
NF-κB 0.1 μM (IC50) |
c-Rel 3 μM (IC50) |
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 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 Line:SU-DHL8 and TMD8 cells
-
Concentration:3 μM
-
Incubation Time:For 24 hours
-
Result:Decreased cell viability in a dose-dependent fashion.
-
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.
IT-901 (12-20 mg/kg; IP) improves the PK profile by increasing T1/2 and Cmax[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.
化学情報
-
CAS 番号 1584121-99-2
-
性状 Solid
-
分子量 342.37
-
分子式 C17H14N2O4S
-
Color Orange to red
-
SMILES
O=C(/C(C(N1)=O)=C\C2=C3C=CC=CC3=C(OC)C=C2OC)NC1=S
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
Cell Death Discov
The glycolytic enzyme PFKFB3 alleviates DNA damage and chondrocyte senescence in osteoarthritis. [Abstract]2025 Dec 8. PMID: 41360766 -
Int J Mol Sci
Activated Macrophages Promote TNF-α-Associated Tumor Cell Necroptosis in Pituitary Apoplexy Through the PIEZO1-NFATC2/REL Axis. [Abstract]2026 Jun 22;27(12):5635. PMID: 42353349
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (281 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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
取扱説明書 (2659 KB)
参考文献
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
IT-901 関連分類
HY-124179 関連分類
Powered by Bioz