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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- CAS No.: 2421140-72-7
- 화학식: C24H26N4O2
- 분자량:402.50
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
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. Further protocols information, click here.
Chemical Information
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CAS No. 2421140-72-7
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분자량 402.50
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
M4K2149 Related Classifications
HY-184317 Related Classifications
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