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).
For research use only. We do not sell to patients.
- Purity : 98.31%
- CAS No.: 2421141-51-5
- Formula: C27H31FN4O2
- Molecular Weight:462.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
ALK1 7 nM (IC50) |
ALK2 14 nM (IC50) |
ALK3 168 nM (IC50) |
ALK4 1660 nM (IC50) |
ALK5 1950 nM (IC50) |
ALK6 88 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>30 μM
Compound: 26b
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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
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[PMID: 32369358] |
| HEK293 | IC50 |
3900 nM
Compound: 26b
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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
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[PMID: 32369358] |
| HEK293 | IC50 |
52 nM
Compound: 26b
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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
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[PMID: 32369358] |
In Vitro
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.
Parmacokinetics
| Species | Dose | Route | T1/2 | Cmax | Vss |
|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 1.3 h | 0.3 μM | 3 |
In Vivo
| Mice PO 3 mg/kg |
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| 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.
Chemical Information
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CAS No. 2421141-51-5
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Appearance Solid
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Molecular Weight 462.56
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Formula C27H31FN4O2
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Color Light brown to brown
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro:
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)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (272 KB)
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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)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 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 Related Classifications
HY-148234 Related Classifications
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