BI-4659
Based on 1 Customer Validation
BI-4659 is a TGFβRI and PDGFRα inhibitor with IC50 values of 19 nM and 99 nM, respectively. BI-4659 inhibits the kinase activities of TGFβRI and PDGFRα, blocks the downstream TGFβRI signaling pathway, and reduces the phosphorylation level of Smad2/3 without altering the expression of TGF-β1. BI-4659 is applicable to research related to pulmonary fibrosis, cancer, and renal ischemia-reperfusion injury.
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。
The BI-4659 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- 純度 : 99.78%
- CAS 番号: 894784-05-5
- 分子式: C27H28N4O2
- 分子量:440.54
-
保管条件:Powder -20°C, 3 years , 4°C, 2 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
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
TGFBR1 19 nM (IC50) |
PDGFRα 99 nM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HaCaT | EC50 |
185 nM
Compound: 47i
|
Inhibition of TGFbeta receptor in human HaCaT cells assessed as Smad phosphorylation by ELISA
Inhibition of TGFbeta receptor in human HaCaT cells assessed as Smad phosphorylation by ELISA
|
[PMID: 20919678] |
| HaCaT | IC50 |
>1 μM
Compound: 47i
|
Cytotoxicity against human HaCaT cells
Cytotoxicity against human HaCaT cells
|
[PMID: 20919678] |
体外実験
BI-4659 (75 min) inhibits TGFβRI-mediated phosphorylation of Smad2/3 in HaCaT cells with an EC50 of 185 nM[1].
BI-4659 (up to 1 μM; 24 h) shows no significant cytotoxicity in HaCaT cells at concentrations as high as 1 μM following a 24 h incubation[1].
BI-4659 (1 μM; 24 h) inhibits the TGF-β-Smad2/3 pathway in mouse bone marrow-derived neutrophils, thereby blocking sFgl2-MSC-induced transformation of neutrophils into an anti-inflammatory N2-like phenotype, inhibition of neutrophil extracellular trap formation, and regulation of inflammatory cytokine secretion[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HaCaT cells
-
Concentration:up to 1 μM
-
Incubation Time:24 h
-
Result:Exhibited no significant cytotoxicity (IC50 > 1 μM).
化学情報
-
CAS 番号 894784-05-5
-
性状 Solid
-
分子量 440.54
-
分子式 C27H28N4O2
-
Color Off-white to yellow
-
SMILES
CN(C)CC(C=C1)=CC=C1N/C(C2=CC=CC=C2)=C3C4=CC=C(C(NCC)=O)C=C4NC/3=O
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 5 mg/mL (11.35 mM; Need warming; 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 (278 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Roth GJ, et al. Design, synthesis, and evaluation of indolinones as inhibitors of the transforming growth factor β receptor I (TGFβRI). J Med Chem. 2010;53(20):7287-7295. [Content Brief]
[2]. Chen GS, et al. Overexpression of Soluble Fibrinogen-like Protein 2 in MSCs Ameliorates Renal Ischemia-Reperfusion Injury in Mice by Modulating Neutrophils. Balkan Med J. 2026;43(3):136-150. [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 | 2.2699 mL | 11.3497 mL | 22.6994 mL | 56.7485 mL |
| 5 mM | 0.4540 mL | 2.2699 mL | 4.5399 mL | 11.3497 mL | |
| 10 mM | 0.2270 mL | 1.1350 mL | 2.2699 mL | 5.6749 mL |
BI-4659 関連分類
HY-171878 関連分類
Powered by Bioz