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.
For research use only. We do not sell to patients.
- CAS No.: 2421140-72-7
- Formula: C24H26N4O2
- Molecular Weight:402.50
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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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CAS No. 2421140-72-7
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Molecular Weight 402.50
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Formula 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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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
M4K2149 Related Classifications
HY-184317 Related Classifications
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