M4K2234
Based on 1 Customer Validation
M4K2234, a chemical probe, is an orally active, highly selective inhibitor of ALK1 and ALK2 with IC50 values of 7 nM and 14 nM, respectively. M4K2234 specifically blocks BMP signaling by inhibiting the phosphorylation of SMAD1/5/8. M4K2234 inhibits BMP7-stimulated reporter gene activity (IC50 = 16 nM). M4K2234 can be used for the investigation of ALK1/2-mediated biological processes and related diseases such as diffuse midline glioma (DMG) and fibrodysplasia ossificans progressiva (FOP).
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: 98.31%
- CAS 番号: 2421141-51-5
- 分子式: C27H31FN4O2
- 分子量:462.56
-
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
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Kinase Inhibitor Library
HY-L009
-
Protein Tyrosine Kinase Compound Library
HY-L016
-
Stem Cell Signaling Compound Library
HY-L017
-
TGF-beta/Smad Compound Library
HY-L018
-
Wnt/Hedgehog/Notch Compound Library
HY-L020
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Orally Active Compound Library
HY-L061
-
Angiogenesis-Related Compound Library
HY-L088
-
Transcription Factor-Targeted Library
HY-L090
-
Anti-Colorectal Cancer Compound Library
HY-L103
-
Anti-Prostate Cancer Compound Library
HY-L124
-
Anti-Pulmonary Fibrosis Compound Library
HY-L125
-
Osteogenesis Compound Library
HY-L131
-
Cancer Stem Cells Compound Library
HY-L135
-
Membrane Protein-targeted Compound Library
HY-L149
-
Highly Selective Inhibitors Library
HY-L158
-
Serine/Threonine Kinase Inhibitor Library
HY-L164
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Anti-Fibrosis Compound Library
HY-L185
-
Anti-Brain Cancer Compound Library
HY-L188
-
Protein Kinase Compound Library
HY-L196
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
生物活性
|
ALK1 7 nM (IC50) |
ALK2 14 nM (IC50) |
ALK3 168 nM (IC50) |
ALK4 1660 nM (IC50) |
ALK5 1950 nM (IC50) |
ALK6 88 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>30 μM
Compound: 26b
|
Inhibition of human ERG expressed in HEK293 cells measured after 5 mins by whole cell patch clamp method
Inhibition of human ERG expressed in HEK293 cells measured after 5 mins by whole cell patch clamp method
|
[PMID: 32369358] |
| HEK293 | IC50 |
3900 nM
Compound: 26b
|
Inhibition of ALK5 (unknown origin) expressed in HEK293 cells transfected with CAGA-luciferase and Renilla luciferase reporter measured after 24 hrs by dual luciferase reporter assay
Inhibition of ALK5 (unknown origin) expressed in HEK293 cells transfected with CAGA-luciferase and Renilla luciferase reporter measured after 24 hrs by dual luciferase reporter assay
|
[PMID: 32369358] |
| HEK293 | IC50 |
52 nM
Compound: 26b
|
Inhibition of C-terminal nanoluciferase-fused ALK2 (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition by NanoBRET assay
Inhibition of C-terminal nanoluciferase-fused ALK2 (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition by NanoBRET assay
|
[PMID: 32369358] |
M4K2234 (16 nM) potently inhibits BMP7-stimulated reporter gene activity in HEK293 cells, while showing 50-fold and 150-fold weaker inhibition on activin A and TGF-β1-induced CAGA-responsive reporter, respectively[1].
M4K2234 (0.5-1 μM) specifically inhibits phosphorylation of SMAD1/5/8 induced by BMP family ligands in HEK293T cells, without affecting SMAD2/3 phosphorylation induced by activin A or TGF-β1[1].
M4K2234 shows an IC50 of 7 nM for ALK1 and 14 nM for ALK2 in enzyme kinetic assays, with weak inhibition on ALK6 (88 nM) and negligible activity on ALK4/5 (>10,000 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Cmax | Vss |
|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 1.3 h | 0.3 μM | 3 |
| Mice PO 3 mg/kg |
|
| Cmax(ng/mL) | 1650 |
| AUCinf(ng·h/mL) | 4630 |
| t1/2(h) | 2.61 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
-
CAS 番号 2421141-51-5
-
性状 Solid
-
分子量 462.56
-
分子式 C27H31FN4O2
-
Color Light brown to brown
-
SMILES
O=C(C1=C(C=C(C2=CN=CC(C3=CC=C(N4CCN(C(C)C)CC4)C=C3)=C2C)C=C1OC)F)N
-
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
DMSO : 100 mg/mL (216.19 mM; Need ultrasonic; 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 (272 KB)
-
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
-
取扱説明書 (2659 KB)
参考文献
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 | 2.1619 mL | 10.8094 mL | 21.6188 mL | 54.0470 mL |
| 5 mM | 0.4324 mL | 2.1619 mL | 4.3238 mL | 10.8094 mL | |
| 10 mM | 0.2162 mL | 1.0809 mL | 2.1619 mL | 5.4047 mL | |
| 15 mM | 0.1441 mL | 0.7206 mL | 1.4413 mL | 3.6031 mL | |
| 20 mM | 0.1081 mL | 0.5405 mL | 1.0809 mL | 2.7024 mL | |
| 25 mM | 0.0865 mL | 0.4324 mL | 0.8648 mL | 2.1619 mL | |
| 30 mM | 0.0721 mL | 0.3603 mL | 0.7206 mL | 1.8016 mL | |
| 40 mM | 0.0540 mL | 0.2702 mL | 0.5405 mL | 1.3512 mL | |
| 50 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL | 1.0809 mL | |
| 60 mM | 0.0360 mL | 0.1802 mL | 0.3603 mL | 0.9008 mL | |
| 80 mM | 0.0270 mL | 0.1351 mL | 0.2702 mL | 0.6756 mL | |
| 100 mM | 0.0216 mL | 0.1081 mL | 0.2162 mL | 0.5405 mL |
M4K2234 関連分類
HY-148234 関連分類
Powered by Bioz