M4K2149
M4K2149 is a selective ALK2 inhibitor with an IC50 value of 17 nM. M4K2149 is applicable to research related to diffuse intrinsic pontine glioma.
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- No. CAS: 2421140-72-7
- Fòrmula: C24H26N4O2
- Peso molecular:402.50
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
ALK2 17 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
55 nM
Compound: M4K2149
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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] |
| HEK293 | IC50 |
704 nM
Compound: M4K2149
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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] |
In Vitro
M4K2149 potently inhibits WT ALK2 with an IC50 of 17 nM, shows comparable potency against DIPG-linked ALK2 mutants (ALK2G328V, ALK2R206H, ALK2R258G), and exhibits 34-fold selectivity for ALK2 over ALK5 in a radioactive in vitro biochemical kinase assay[1].
M4K2149 inhibits ALK2 binding in HEK293 cells with an IC50 of 55 nM in a NanoBRET assay and exhibits 13-fold cell-based selectivity for ALK2 over ALK5[1].
M4K2149 has reduced off-target activity against the hERG potassium channel in HEK293 cells, with an IC50 of >50 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2421140-72-7
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Peso molecular 402.50
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Fòrmula C24H26N4O2
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SMILES
O=C(N)C1=CC=C(C=C1OC)C2=CN=CC(C3=CC=C(C=C3)N4CCNCC4)=C2C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
M4K2149 Related Classifications
HY-184317 Related Classifications
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